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ABT-737

Catalog No. A10255
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Bcl-2 抑制剂

ABT-737是一种类BH3抑制剂，能同时抑制Bcl-xL，Bcl-2和Bcl-w，EC50分别为78.7 nM，30.3 nM和197.8 nM;但对Mcl-1，Bcl-B及Bfl-1没有抑制作用。了解更多

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- Jung Mo Lee, .et al. ABT-737, a BH3 Mimetic, Enhances the Therapeutic Effects of Ionizing Radiation in K-ras Mutant Non-Small Cell Lung Cancer Preclinical Model, Yonsei Med J, 2022, Jan;63(1):16-25 PMID: 34913280
- AidaVarela-Moreira, .et al. Utilizing in vitro drug release assays to predict in vivo drug retention in micelles, Int J Pharm, 2022, Apr 25;618:121638 PMID: 35257802
- Daniel F R Boehmer, .et al. OAS1/RNase L executes RIG-I ligand-dependent tumor cell apoptosis, Sci Immunol, 2021, Jul 16;6(61) PMID: 34272227
- Shivani Arora, .et al. Invariant natural killer T cells coordinate removal of senescent cells, Med, 2021, 2,1-13
- Ying Ji, .et al. Use of ratiometrically designed nanocarrier targeting CDK4/6 and autophagy pathways for effective pancreatic cancer treatment, Nat Commun, 2020, Aug 25;11(1):4249 PMID: 32843618
- Birgit Ritschka, .et al. The senotherapeutic drug ABT-737 disrupts aberrant p21 expression to restore liver regeneration in adult mice, Genes Dev, 2020, Apr 1;34(7-8):489-494 PMID: 32139422
- Hiroki Akiyama, .et al. Inhibition of USP9X Downregulates JAK2-V617F and Induces Apoptosis Synergistically With BH3 Mimetics Preferentially in Ruxolitinib-Persistent JAK2-V617F-Positive Leukemic Cells, Cancers, 2020, 12 (2) PMID: 32050632
- Hsu CC, .et al. α7-Nicotine acetylcholine receptor mediated nicotine induced cell survival and cisplatin resistance in oral cancer, Arch Oral Biol, 2020, Mar;111:104653 PMID: 31935534
- Gupta VK, .et al. Lysophosphatidic acid promotes survival of T lymphoma cells by altering apoptosis and glucose metabolism, Apoptosis, 2020, Feb;25(1-2):135-150 PMID: 31867678
- Meikle V, .et al. A protein complex from human milk enhances the activity of antibiotics and drugs against Mycobacterium tuberculosis, Antimicrob Agents Chemother, 2018, Nov 12. pii: AAC.01846-18 PMID: 30420480
- Chauhan D, .et al. BAX/BAK-Induced Apoptosis Results in Caspase-8-Dependent IL-1β Maturation in Macrophages, Cell Rep, 2018, Nov 27;25(9):2354-2368.e5 PMID: 30485805
- Jose Mario Gonzalez-Meljem, .et al. Stem cell senescence drives age-attenuated induction of pituitary tumours in mouse models of paediatric craniopharyngioma, Nat Commun, 2017, 8: 1819 PMID: 29180744
- Zhang C, .et al. Sorafenib targets the mitochondrial electron transport chain complexes and ATP synthase to activate the PINK1-Parkin pathway and modulate cellular drug response, J Biol Chem, 2017, Sep 8;292(36):15105-15120 PMID: 28673964
- Eun Young Kim, .et al. ABT-737 Synergizes with Cisplatin Bypassing Aberration of Apoptotic Pathway in Non-small Cell Lung Cancer, Neoplasia, 2017, Apr; 19(4): 354-363 PMID: 28319809
- Masayoshi Toge, .et al. Critical contribution of MCL-1 in EMT-associated chemo-resistance in A549 non-small cell lung cancer, Int J Oncol., 2015, Apr;46(4):1844-8 PMID: 25647738
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ABT-263 (Navitoclax)

Catalog No. A10022
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Bcl-2 抑制剂

ABT-263 (Navitoclax)是一种有效的Bcl-2家族抑制剂 (Bcl-2，Bcl-xL和Bcl-w的Ki <1 nmol/L)。ABT-263对Bcl- xL，Bcl-2和Bcl-w，( Ki≤1nmol/ L) 维持高亲和力，但与Mcl-1和A1的结合更弱。了解更多

Product Citations (20)

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- Rindert Missiaen, .et al. GCN2 inhibition sensitizes arginine-deprived hepatocellular carcinoma cells to senolytic treatment, Cell Metab, 2022, Aug 2;34(8):1151-1167 PMID: 35839757
- Ashlyn Parkhurst, .et al. Dual mTORC1/2 inhibition compromises cell defenses against exogenous stress potentiating Obatoclax-induced cytotoxicity in atypical teratoid/rhabdoid tumors, Cell Death Dis, 2022, Apr 28;13(4):410 PMID: 35484114
- Suzuki, Keiji, .et al. Characterization of radiation-induced micronuclei associated with premature senescence, and their selective removal by senolytic drug, ABT-263, Mutat Res Genet Toxicol Environ Mutagen, 2022, 876-877. 503448
- Rotem Ben-Hamo, .et al. Predicting and affecting response to cancer therapy based on pathway-level biomarkers, Nat Commun, 2020, 11: 3296
- Hua Xu, .et al. Preclinical Study Using ABT263 to Increase Enzalutamide Sensitivity to Suppress Prostate Cancer Progression Via Targeting BCL2/ROS/USP26 Axis Through Altering ARv7 Protein Degradation, Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
- Hiroki Akiyama, .et al. Inhibition of USP9X Downregulates JAK2-V617F and Induces Apoptosis Synergistically With BH3 Mimetics Preferentially in Ruxolitinib-Persistent JAK2-V617F-Positive Leukemic Cells, Cancers, 2020, 12 (2) PMID: 32050632
- Stephanie Ketterer, .et al. Cathepsin D deficiency in mammary epithelium transiently stalls breast cancer by interference with mTORC1 signaling, Nat Commun, 2020, Oct 12;11(1):5133 PMID: 33046706
- Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
- Min Li, .et al. Clearance of HIV infection by selective elimination of host cells capable of producing HIV, Nat Commun, 2020, 11: 4051 PMID: 32792548
- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Momeny M, .et al. The ERBB receptor inhibitor dacomitinib suppresses proliferation and invasion of pancreatic ductal adenocarcinoma cells, Cell Oncol (Dordr), 2019, Apr 25 PMID: 31025257
- Anderson R, .et al. Length-independent telomere damage drives postmitotic cardiomyocyte senescence, EMBO J, 2019, Feb 8. pii: e100492 PMID: 30737259
- Shinya Ishida, .et al. Mechanisms for mTORC1 activation and synergistic induction of apoptosis by ruxolitinib and BH3 mimetics or autophagy inhibitors in JAK2-V617F-expressing leukemic cells including newly established PVTL-2, Oncotarget, 2018, Jun 1; 9(42): 26834-26851 PMID: 29928488
- Rhys Anderson, .et al. Length-independent telomere damage drives cardiomyocyte senescence, bioRxiv, 2018, 2018
- Ryuta Mikawa, .et al. Elimination of p19ARF?\expressing cells protects against pulmonary emphysema in mice, Aging Cell, 2018, Oct; 17(5): e12827 PMID: 30058137
- Joo Sang Lee, .et al. Harnessing synthetic lethality to predict the response to cancer treatment, Nat Commun, 2018, 9: 2546 PMID: 29959327
- Toshiyuki Sumi, .et al. Survivin knockdown induces senescence in TTF-1-expressing, KRAS-mutant lung adenocarcinomas, Int J Oncol, 2018, Jul; 53(1): 33-46 PMID: 29658609
- Wei TW, .et al. Aurora A and NF-κB Survival Pathway Drive Chemoresistance in Acute Myeloid Leukemia via the TRAF-Interacting Protein TIFA, Cancer Res, 2017, Jan 15;77(2):494-508 PMID: 28069801
- Yusuke Takagi, .et al. SPIB is a novel prognostic factor in diffuse large B?\cell lymphoma that mediates apoptosis via the PI3K-AKT pathway, Cancer Sci, 2016, Sep; 107(9): 1270-1280 PMID: 27348272
- Matsumoto M, .et al. Cisplatin-induced apoptosis in non-small-cell lung cancer cells is dependent on Bax- and Bak-induction pathway and synergistically activated by BH3-mimetic ABT-263 in p53 wild-type and mutant cells, Biochem Biophys Res Commun, 2016, Apr 29;473(2):490-6 PMID: 26996126
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XL184 free base (Cabozantinib)

Catalog No. A10996
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VEGFR 抑制剂

XL184 free base (Cabozantinib)是设计用来抑制多种受体酪氨酸激酶（特别是MET和VEGFR2）的小分子。了解更多

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- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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ABT-888 (Veliparib)

Catalog No. A10026
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PARP 抑制剂

ABT-888 (Veliparib)是一种潜在的抗癌药物，可作为PARP抑制剂。了解更多

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- Subhajit Chatterjee, .et al. PARP inhibitor Veliparib (ABT-888) enhances the anti-angiogenic potentiality of Curcumin through deregulation of NECTIN-4 in oral cancer: Role of nitric oxide (NO), Cell Signal, 2021, Apr;80:109902 PMID: 33373686
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Saracatinib (AZD0530)

Catalog No. A10108
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Src/Abl 抑制剂

Saracatinib (AZD0530)是一种高选择性，双特异性Src/Abl激酶抑制剂，对c-Src和Abl激酶的IC50分别为2.7和30 nM。了解更多

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- Andromachi Lambrianidou, .et al. mTORC2 deploys the mRNA binding protein IGF2BP1 to regulate c-MYC expression and promote cell survival, Cell Signal, 2021, Apr;80:109912 PMID: 33388443
- Chisato Naito, .et al. Facilitatory effects of fetuin-A on atherosclerosis, Atherosclerosis, 2016, Mar;246:344-51 PMID: 26828753
- Kenta Maruyama, .et al. 5-Azacytidine-induced Protein 2 (AZI2) Regulates Bone Mass by Fine-tuning Osteoclast Survival, J Biol Chem, 2015, Apr 10; 290(15): 9377-9386 PMID: 25691576
- Amanda L Jackson, .et al. Emerging therapies: angiogenesis inhibitors for ovarian cancer, Expert Opin Emerg Drugs, 2015, Jun;20(2):331-46 PMID: 26001052
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Masitinib ( AB1010)

Catalog No. A10558
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c-Kit 抑制剂

Masitinib (AB1010)是一种蛋白质酪氨酸激酶抑制剂。了解更多

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- S Masson ,etc. Inhibition of Cell Signalling in Neoplastic Canine Mast Cells. , 2014, .
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Apixaban (BMS-562247-01)

Catalog No. A10082
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Factor Xa 抑制剂

Apixaban (BMS-562247-01)是一种抗凝剂，用于预防静脉血栓栓塞和静脉血栓栓塞事件。了解更多

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- Daniël Verhoef, .et al. Engineered factor Xa variants retain procoagulant activity independent of direct factor Xa inhibitors, Nat Commun, 2017, 8: 528 PMID: 28904343
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AP24534 (Ponatinib)

Catalog No. A10080
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BCR-ABL 抑制剂

AP24534 (Ponatinib)是有效的多激酶和pan-BCR-ABL抑制剂。了解更多

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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Yamamoto Y, .et al. Development of a sandwich enzyme-linked immunosorbent assay for the quantification of ponatinib in serum, Anal Biochem, 2019, Feb 13. pii: S0003-2697(18)31083-2 PMID: 30771339
- N Naganna, .et al. Amino alkynylisoquinoline and alkynylnaphthyridine compounds potently inhibit acute myeloid leukemia proliferation in mice, EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
- Takuya Hirao, .et al. Altered intracellular signaling by imatinib increases the anti-cancer effects of tyrosine kinase inhibitors in chronic myelogenous leukemia cells, Cancer Sci, 2018, Jan; 109(1): 121-131 PMID: 29121435
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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WP1130 (Degrasyn)

Catalog No. A10988
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DUB/Bcr/ABL 抑制剂

WP1130 (Degrasyn)是一种新型的选择性小分子去泛素酶抑制剂和Bcr/Abl破坏途径激活剂，可特异性和快速下调野生型和突变型Bcr/Abl蛋白，而不会影响慢性粒细胞性白血病（CML）中的bcr/abl基因表达细胞。了解更多

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Tianeptine sodium

Catalog No. A10931
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5-HT Receptor 激动剂

Tianeptine钠是体内和体外的选择性5-羟色胺再摄取促进剂（SSRE）。了解更多

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Danusertib (PHA-739358)

Catalog No. A10715
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Aurora 抑制剂

Danusertib (PHA-739358)是Aurora A/B/C的Aurora激酶抑制剂，在无细胞分析中的IC50为13 nM/79nM/61 nM，对Abl，TrkA，c-RET和FGFR1以及更低的浓度具有中等效力对Lck，VEGFR2/3，c-Kit，CDK2等有效。了解更多

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- Samuel Q. Li, etc. Targeting Wild-Type and Mutationally Activated FGFR4 in Rhabdomyosarcoma with the Inhibitor Ponatinib (AP24534). PLoS One. 2013; 8(10): e76551.
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Acarbose

Catalog No. A10029
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Anti-Diabetic Agent

Acarbose是一种肠道alpha-glucosidase抑制剂，用于治疗2型糖尿病以及某些国家的前驱糖尿病。了解更多

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3-Aminobenzamide

Catalog No. A10475
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PARP 抑制剂

3-Aminobenzamide是一种新型PARP抑制剂，已知它通过抑制DNA损伤的修复使细胞在体外对辐射敏感。了解更多

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- Kamada Y, .et al. Castalagin and vescalagin purified from leaves of Syzygium samarangense (Blume) Merrill & L.M. Perry: Dual inhibitory activity against PARP1 and DNA topoisomerase II, Fitoterapia, 2018, Sep;129:94-101 PMID: 29928967
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TSU-68 (Orantinib, SU6668)

Catalog No. A10953
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PDFGRβ 抑制剂

TSU-68 (Orantinib,SU6668)在无细胞试验中具有8 nM的Ki对PDGFR自磷酸化的最大效力，但也强烈抑制Flk-1和FGFR1反磷酸化，对IGF-1R，Met，Src， Lck，Zap70，Abl和CDK2；不抑制EGFR。了解更多

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- Aaron Y. Lai, .et al. Venular degeneration leads to vascular dysfunction in a transgenic model of Alzheimer's disease., Brain, 2015, Apr;138(Pt 4):1046-58 PMID: 25688079
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TAK-733

Catalog No. A11040
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MEK 抑制剂

TAK-733是一种有效的，选择性的MEK变构抑制剂，作用于MEK1，IC50为3.2 nM，抑制Abl1，AKT3，c-RAF，CamK1，CDK2及c-Met等活性。了解更多

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Baicalin

Catalog No. A10121
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HIV-1 production 抑制剂

Baicalin是已知的脯氨酰内肽酶抑制剂，并且影响GABA受体。了解更多

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- Shoichi Ozawa, .et al. Uremic serum residue decreases SN-38 sensitivity through suppression of organic anion transporter polypeptide 2B1 in LS-180 colon cancer cells, Sci Rep, 2019, 9: 15464
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PCI-24781 (Abexinostat)

Catalog No. A10700
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HDAC 抑制剂

PCI-24781 (Abexinostat)是一种广谱苯基异羟肟酸HDAC抑制剂。了解更多

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Decitabine

Catalog No. A10292
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DNA Methyltransferase 抑制剂

Decitabine是一种次甲基化剂，它通过抑制DNA甲基转移酶来使DNA次甲基化。了解更多

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- Borbala Szabo, .et al. Aspirin mediates its antitumoral effect through inhibiting PTTG1 in pituitary adenoma, J Clin Endocrinol Metab, 2022, Sep 5;dgac496 PMID: 36059148
- Sangni Qian, .et al. Hypermethylation of tumor suppressor lncRNA MEF2C-AS1 frequently happened in patients at all stages of colorectal carcinogenesis, Clin Epigenetics, 2022, Sep 5;14(1):111 PMID: 36064442
- Borb??la Szab??, .et al. Demethylation status of somatic DNA extracted from pituitary neuroendocrine tumors indicates proliferative behavior, J Clin Endocrinol Metab, 2020, Jun 1;105(6):dgaa156 PMID: 32232382
- Bracha Shraibman, .et al. Human Leukocyte Antigen (HLA) Peptides Derived from Tumor Antigens Induced by Inhibition of DNA Methylation for Development of Drug-facilitated Immunotherapy, Mol Cell Proteomics, 2016, Sep; 15(9): 3058-3070 PMID: 27412690
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Bafetinib (INNO-406)

Catalog No. A10119
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Bcr-Abl 抑制剂

Bafetinib (INNO-406)是一种双重Bcr-Abl/Lyn酪氨酸激酶抑制剂。了解更多

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- Li T, .et al. Bruton's tyrosine kinase potentiates ALK signaling and serves as a potential therapeutic target of neuroblastoma, Oncogene, 2018, Nov;37(47):6180-6194 PMID: 30013190
- S. Dallari, .et al. Src family kinases Fyn and Lyn are constitutively activated and mediate plasmacytoid dendritic cell responses, Nat Commun, 2017, 8: 14830 PMID: 28368000
- Andrea Haerzschel, .et al. BCR and chemokine responses upon anti-IgM and anti-IgD stimulation in chronic lymphocytic leukaemia, Ann Hematol, 2016, 95(12): 1979-1988 PMID: 27542958
- Magdalena Winiarska, .et al. Inhibitors of SRC kinases impair antitumor activity of anti-CD20 monoclonal antibodies, MAbs., 2014, 6(5): 1300-1313. PMID: 25517315
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OSI-906

Catalog No. A11053
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IGF-1R 抑制剂

OSI-906是一种选择性IGF-1R抑制剂，在无细胞试验中IC50为35 nM；对InsR抑制作用适中，IC50为75 nM，对Abl，ALK，BTK，EGFR， FGFR1/2，PKA等没有抑制活性。了解更多

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- Masao Kakoki, .et al. Cyanocobalamin prevents cardiomyopathy in type 1 diabetes by modulating oxidative stress and DNMT-SOCS1/3-IGF-1 signaling, Communications Biology, 2021, 4:775
- Nakamura T, .et al. Naturally Occurring Hair Growth Peptide: Water-Soluble Chicken Egg Yolk Peptides Stimulate Hair Growth Through Induction of Vascular Endothelial Growth Factor Production, J Med Food, 2018, Jul;21(7):701-708 PMID: 29583066
- Tzeng SF, .et al. O-Glycosylation-mediated signaling circuit drives metastatic castration-resistant prostate cancer, FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- Takata N, .et al. IGF-2/IGF-1R signaling has distinct effects on Sox1, Irx3, and Six3 expressions during ES cell derived-neuroectoderm development in vitro, In Vitro Cell Dev Biol Anim., 2016, May;52(5):607-15 PMID: 26956358
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Linifanib (ABT-869)

Catalog No. A10025
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VEGFR/PDGFR 抑制剂

Linifanib (ABT-869)是一种结构新颖的有效RTK，VEGF和PDGF抑制剂，对人内皮细胞，PDGFR-β，KDR和CSF-1R的IC50分别为0.2、2、4和7 nM。了解更多

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- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
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Dasatinib (BMS-354825)

Catalog No. A10290
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Abl-Src 抑制剂

Dasatinib (BMS-354825)是一种口服多BCR/ABL和Src家族酪氨酸激酶抑制剂。Dasatinib (BMS-354825)的主要靶标是BCR/ABL，Src，c-Kit，ephrin受体和其他几种酪氨酸激酶，但不是erbB激酶，例如EGFR或Her2。了解更多

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- Chihiro Motozono, .et al. The SARS-CoV-2 Omicron BA.1 spike G446S mutation potentiates antiviral T-cell recognition, Nat Commun, 2022, Sep 21;13(1):5440 PMID: 36130929
- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- David E J Klawon, .et al. Altered selection on a single self-ligand promotes susceptibility to organ-specific T cell infiltration, J Exp Med, 2021, Jun 7;218(6) PMID: 33914024
- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Sano T, .et al. Gliding Basal Cell Migration of the Urothelium during Wound Healing, Am J Pathol, 2018, Nov;188(11):2564-2573 PMID: 30121259
- Ines Peschel, .et al. FLT3 and FLT3-ITD phosphorylate and inactivate the cyclin-dependent kinase inhibitor p27Kip1 in acute myeloid leukemia, Haematologica, 2017, Aug; 102(8): 1378-1389 PMID: 28522571
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- John D. Leonard, .et al. Identification of natural regulatory T cell epitopes reveals convergence on a dominant autoantigen, Immunity, 2017, Jul 18; 47(1): 107-117.e8 PMID: 28709804
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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KW-2449

Catalog No. A10508
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FLT3/FGFR/Bcr-Abl/Aurora 抑制剂

KW-2449是FLT3、ABl、ABl-T315I和Aurora激酶的多激酶抑制剂。了解更多

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TAK-901

Catalog No. A11067
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Aurora Kinase A/B 抑制剂

TAK-901是一种新型Aurora A/B抑制剂，IC50为21 nM/15 nM。它不是细胞JAK2，c-Src或Abl的有效抑制剂。了解更多

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BIBR-1048 (Dabigatran etexilate)

Catalog No. A10139
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Thrombin 抑制剂

BIBR-1048 (Dabigatran etexilate)是dabigatran的前体药物，dabigatran是一种有效的、非肽类小分子化合物，可特异地、可逆性地抑制游离的和结合了血凝块的凝血酶。了解更多

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Methotrexate (Abitrexate)

Catalog No. A10021
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DHFR 抑制剂

Methotrexate (Abitrexate)是一种抑制胸苷酸合成酶和从头嘌呤合成的细胞毒剂。了解更多

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Imatinib Mesylate

Catalog No. A10468
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Bcr-Abl 抑制剂

Imatinib mesylate是一种选择性酪氨酸激酶抑制剂，通过抑制KIT信号转导途径，在治疗胃肠间质瘤中诱导了持续的客观反应。了解更多

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- Inge Govaerts, .et al. PSEN1-selective gamma-secretase inhibition in combination with kinase or XPO-1 inhibitors effectively targets T cell acute lymphoblastic leukemia, J Hematol Oncol, 2021, 14: 97 PMID: 34167562
- Genevra Kuziel, .et al. Stromal CCL2 Signaling Promotes Mammary Tumor Fibrosis through Recruitment of Myeloid-Lineage Cells, Cancers (Basel), 2020, Jul 28;12(8):E2083 PMID: 32731354
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NVP-BHG712

Catalog No. A10661
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EphB4 抑制剂

NVP-BHG712是EphB4激酶的选择性抑制剂，在体外对EphB4的选择性超过40多种其他激酶（包括FGFR3）。了解更多

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- Y Kaibori, .et al. EphA2 phosphorylation at Ser897 by the Cdk1/MEK/ERK/RSK pathway regulates M-phase progression via maintenance of cortical rigidity, the FASEB Journal, 2019, Jan 22:fj201801519RR PMID: 30668924
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ABT-751 (E-7010)

Catalog No. A10024
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Microtubule Associated 抑制剂

ABT-751 (E-7010)是一种抗有丝分裂剂，可抑制微管聚合，并在秋水仙碱位点与β-微管蛋白结合。在G2M期阻断细胞周期并诱导凋亡。了解更多

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Capecitabine (Xeloda)

Catalog No. A10177
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Capecitabine (Xeloda)是一种治疗肿瘤选择性的氟嘧啶氨基甲酸酯，具有较高的瘤内5-FU水平，且毒性比5-FU低。了解更多

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- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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DCC-2036 (Rebastinib)

Catalog No. A11200
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Bcr-Abl 抑制剂

DCC-2036 (Rebastinib)是一种Bcr-Abl抑制剂，作用于Abl1(WT)和Abl1(T315I)，IC50分别为0.8 nM和4 nM，也抑制SRC， LYN， FGR， HCK， KDR， FLT3，和Tie-2，对c-Kit具有低的抑制活性。了解更多

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- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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PP121

Catalog No. A11207
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PI3K 抑制剂

PP121是一种作用于PDGFR，Hck，mTOR，VEGFR2，Src和Abl的多靶点抑制剂，IC50分别为2 nM，8 nM，10 nM，12 nM，14 nM和18 nM，也抑制DNA-PK，IC50为60 nM。了解更多

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Myricetin (Cannabiscetin)

Catalog No. A10615
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Myricetin (Cannabiscetin)是一种具有抗氧化和抗肿瘤活性的天然黄酮，是新型的MEK1抑制剂，抑制JB6 P+小鼠表皮细胞的转化。它还能抑制PI3Kγ，Kd=0.17 μM。了解更多

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Nefiracetam (Translon)

Catalog No. A10631
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Nefiracetam (Translon)是认知增强剂。它激活L/N型钙通道，胆碱能，单胺能和GABA能系统。了解更多

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Nelarabine (Arranon)

Catalog No. A10632
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Nelarabine是一种嘌呤核苷类似物，可转化为其相应的阿拉伯糖基鸟嘌呤核苷酸三磷酸（araGTP），从而抑制DNA合成和细胞毒性，IC50为0.067-2.15 μM。了解更多

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Nilotinib (AMN-107)

Catalog No. A10644
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Bcr-Abl 抑制剂

Nilotinib (AMN-107)是一种Bcr-Abl抑制剂，IC50小于30 nM。了解更多

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- Rami Shinnawi, .et al. Monitoring Human-Induced Pluripotent Stem Cell-Derived Cardiomyocytes with Genetically Encoded Calcium and Voltage Fluorescent Reporters, Stem Cell Reports, 2015, Oct 13; 5(4): 582-596 PMID: 26372632
- Tetsuya Saita, .et al. Preparation of Antibodies and Development of an Enzyme-Linked Immunosorbent Assay for the Tyrosine Kinase Inhibitors Lapatinib and Nilotinib., Biol Pharm Bull. , 2015, 38(10):1652-7 PMID: 26424026
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NPI-2358 (Plinabulin)

Catalog No. A10654
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Microtubule 抑制剂

NPI-2358 (Plinabulin)是NPI-2350的合成类似物，NPI-2350是从曲霉属（Aspergillus sp.）分离的天然产物，可解聚A549人肺癌细胞中的微管。了解更多

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Sinomenine (Cucoline)

Catalog No. A10846
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Sinomenine (Cucoline)在传统上用于草药，以治疗风湿病和关节炎。了解更多

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- Zheng Sun, .et al. Sinomenine inhibits the growth of melanoma by enhancement of autophagy via PI3K/AKT/mTOR inhibition, Drug Des Devel Ther, 2018, 12: 2413-2421 PMID: 30122899
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Tropisetron (ICS 205930)

Catalog No. A11226
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5-HT3 拮抗剂

Tropisetron (ICS 205930)是5-羟色胺5-HT3受体拮抗剂，主要用作止吐药，用于治疗化疗后的恶心和呕吐。了解更多

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Rivaroxaban (Xarelto)

Catalog No. A10800
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Factor Xa 抑制剂

Rivaroxaban (Xarelto)是一种Factor Xa的直接抑制剂，无细胞试验中Ki和IC50分别为0.4 nM和0.7 nM。了解更多

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- Stefan Bittmann, .et al. TMPRSS2-Inhibitors Play a role in Cell Entry Mechanism of COVID-19: An Insight into Camostat and Nafamostat, J Regen Biol Med, 2020, 2(2):1-3
- Daniël Verhoef, .et al. Engineered factor Xa variants retain procoagulant activity independent of direct factor Xa inhibitors, Nat Commun, 2017, 8: 528 PMID: 28904343
- Mizuki Yamamoto, .et al. Identification of Nafamostat as a Potent Inhibitor of Middle East Respiratory Syndrome Coronavirus S Protein-Mediated Membrane Fusion Using the Split-Protein-Based Cell-Cell Fusion Assay, Antimicrob Agents Chemother, 2016, Nov; 60(11): 6532-6539 PMID: 27550352
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Clofarabine

Catalog No. A10228
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DNA/RNA Synthesis 抑制剂

Clofarabine具有抗肿瘤活性的第二代嘌呤核苷类似物。了解更多

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- Xie J, .et al. Optimization of a clofarabine-based drug combination regimen for the preclinical evaluation of pediatric acute lymphoblastic leukemia, Pediatr Blood Cancer, 2019, Dec 25:e28133 PMID: 31876116
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Fludarabine Phosphate (Fludara)

Catalog No. A10395
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Fludarabine Phosphate (Fludara)是一种用于治疗血液恶性肿瘤(血细胞癌，如白血病和淋巴瘤)的化疗药物。氟达拉滨通过干扰核糖核苷酸还原酶和dna聚合酶来抑制DNA合成。它对分裂细胞和静止细胞都有活性。了解更多

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Fludarabine (Fludara)

Catalog No. A10396
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STAT 抑制剂

Fludarabine或fludarabine(fludara)是一种用于治疗血液恶性肿瘤(血细胞癌，如白血病和淋巴瘤)的化疗药物。Fludarabine通过干扰核糖核苷酸还原酶和DNA聚合酶来抑制DNA合成。它对分裂细胞和静止细胞都有活性。了解更多

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- Irene Dell'Anno, .et al. Drug-repositioning screening identified fludarabine and risedronic acid as potential therapeutic compounds for malignant pleural mesothelioma, Invest New Drugs, 2020, Dec 9 PMID: 33300108
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Lopinavir (ABT-378)

Catalog No. A10537
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HIV Protease 抑制剂

Lopinavir (ABT-378)是HIV蛋白酶的抑制剂。了解更多

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Rifabutin

Catalog No. A10790
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RNA polymerase 抑制剂

Rifabutin是一种主要用于治疗肺结核的杀菌抗生素。它的作用是基于阻断细菌的DNA依赖性RNA聚合酶。了解更多

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- Matt D Johansen, .et al. Rifabutin is bactericidal against intracellular and extracellular forms of Mycobacterium abscessus, Antimicrob Agents Chemother, 2020, Aug 17;AAC.00363-20 PMID: 32816730
- Meikle V, .et al. A protein complex from human milk enhances the activity of antibiotics and drugs against Mycobacterium tuberculosis, Antimicrob Agents Chemother, 2018, Nov 12. pii: AAC.01846-18 PMID: 30420480
- Dinah Binte Aziz, .et al. Rifabutin Is Active against Mycobacterium abscessus Complex, Antimicrob Agents Chemother, 2017, Jun; 61(6): e00155-17 PMID: 28396540
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Chlormezanone (Trancopal)

Catalog No. A10201
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Chlormezanone (Trancopal)是一种非苯二氮卓类药物，用于治疗焦虑症。已经建议将其用于治疗肌肉痉挛。氯甲酮与中央苯并二氮杂receptor受体结合，后者与GABA受体发生变构作用。这增强了抑制性神经递质GABA的作用，增强了对网状激活系统的抑制作用，并阻断了在刺激网状通路后发生的皮质和边缘觉醒。了解更多

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Dabrafenib (GSK2118436A)

Catalog No. A11381
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Raf 抑制剂

Dabrafenib (GSK2118436A)是一种有效且选择性的B-RAF蛋白激酶抑制剂，具有V600E突变，目前正在临床试验中。了解更多

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- Yuki Shimizu, .et al. Acquired resistance to BRAF inhibitors is mediated by BRAF splicing variants in BRAF V600E mutation-positive colorectal neuroendocrine carcinoma, Cancer Lett, 2022, Sep 1;543 PMID: 35724767
- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Chenyang He, .et al. Detection of Dabrafenib using Optical Fibre Long Period Grating Sensor Modified with Surface Imprinted Polymers for Dose Detection and Prevention of Cancer Resistance, Clinical and Translational Biophotonics, 2020, TTh3B.2
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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GNF 2

Catalog No. A11439
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Bcr-Abl 抑制剂

GNF 2是一种Bcr-abl抑制剂，在表达Bcr-abl的细胞中抑制增殖并诱导凋亡。了解更多

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Ginkgolide A

Catalog No. A11739
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Ginkgolide A是银杏的提取物，是γ-氨基丁酸(GABA)拮抗剂，Ki为14.5 μM。了解更多

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Emtricitabine

Catalog No. A10349
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NRT 抑制剂

Emtricitabine是一种用于治疗HIV感染的核苷逆转录酶抑制剂 (NRTI) 。了解更多

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