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搜索结果：“azd”

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AZD1480

Catalog No. A10110
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JAK 抑制剂

AZD1480是一种新型有效的小型JAK2抑制剂，IC50为0.26 nM。了解更多

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- Simona Moravcova, .et al. The Circadian Rhythms of STAT3 in the Rat Pineal Gland and Its Involvement in Arylalkylamine-N-Acetyltransferase Regulation, Life (Basel), 2021, Oct 18;11(10):1105 PMID: 34685476
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Cediranib (AZD2171)

Catalog No. A10185
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VEGFR 抑制剂

Cediranib (AZD2171)是一种高效的VEGFR(KDR)抑制剂，此外对c-Kit和PDGFRβ也具有相似的抑制活性，对VEGFR的选择性比PDGFR-α，CSF-1R和Flt3分别高36倍，110倍和1000倍以上。了解更多

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- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
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Olaparib (AZD2281)

Catalog No. A10111
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PARP 抑制剂

Olaparib (AZD2281)是聚ADP核糖聚合酶（PARP）的抑制剂，该酶是一种与DNA修复有关的酶。了解更多

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- Saptarshi Sinha, .et al. Olaparib enhances the Resveratrol-mediated apoptosis in breast cancer cells by inhibiting the homologous recombination repair pathway, Exp Cell Res, 2022, Nov 1;420(1):113338 PMID: 36075449
- Subhajit Chatterjee, .et al. Combination of talazoparib and olaparib enhanced the curcumin-mediated apoptosis in oral cancer cells by PARP-1 trapping, J Cancer Res Clin Oncol, 2022, Dec;148(12):3521-3535 PMID: 35962813
- Yuki Uchihara, .et al. DNA damage promotes HLA class I presentation by stimulating a pioneer round of translation-associated antigen production, Mol Cell, 2022, Jul 21;82(14):2557-2570 PMID: 35594857
- Ji-Ye Kim, .et al. ARL6IP5 reduces cisplatin-resistance by suppressing DNA repair and promoting apoptosis pathways in ovarian carcinoma, Cell Death Dis, 2022, Mar 15;13(3):239 PMID: 35293383
- Emad Matanes, .et al. Inhibition of Poly ADP-Ribose Glycohydrolase Sensitizes Ovarian Cancer Cells to Poly ADP-Ribose Polymerase Inhibitors and Platinum Agents, Front Oncol, 2021, Oct 27;11:745981 PMID: 34778062
- Shino Endo, .et al. BRCA1/ATF1-Mediated Transactivation is Involved in Resistance to PARP Inhibitors and Cisplatin, Cancer Res Commun, 2021, 1(2): 90-105
- Yan Baglo, .et al. Evolutionary dynamics of cancer multidrug resistance in response to olaparib and photodynamic therapy, Transl Oncol, 2021, Nov;14(11):101198 PMID: 34418731
- Joseph M Gozgit, .et al. PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity, Cancer cell, 2021, Jul 22;S1535-6108(21)00340-8 PMID: 34375612
- Sefinew Molla, .et al. Olaparib enhances curcumin-mediated apoptosis in oral cancer cells by inducing PARP trapping through modulation of BER and chromatin assembly, DNA Repair (Amst), 2021, Jun 10;105:103157 PMID: 34144488
- Jianming Wang, .et al. Persistence of RNA transcription during DNA replication delays duplication of transcription start sites until G2/M, Cell Rep, 2021, Feb 16;34(7):108759 PMID: 33596418
- Ai Ito, .et al. Metolazone upregulates mitochondrial chaperones and extends lifespan in Caenorhabditis elegans, Biogerontology, 2021, Feb;22(1):119-131 PMID: 33216250
- Tim J Wigle, .et al. In Vitro and Cellular Probes to Study PARP Enzyme Target Engagement, Cell Chem Biol, 2020, Jul 16;27(7):877-887 PMID: 32679093
- Ali Divan, .et al. Structurally unique PARP-1 inhibitors for the treatment of prostate cancer, Pharmacol Res Perspect, 2020, Apr; 8(2): e00586 PMID: 32342655
- Jianwei Dou, .et al. Development and evaluation of poly adenosine 5'-diphosphate-ribose polymerase 1 immobilization-based receptor chromatography, J Sep Sci, 2020, Dec 4 PMID: 33275824
- Sai Dimple Manavitha Gullipalli, .et al. Development and Validation of Bioanalytical Method for Estimation of Niraparib in Rat Plasma Using High Performance LC-MS/MS And Its Application to Pharmacokinetic Study, Int. J. Adv. Pharm. Biotech, 2020, 6(2) 01-08
- Chao Zhang, .et al. Phenotypic Switching of Atherosclerotic Smooth Muscle Cells is Regulated by Activated PARP1-Dependent TET1 Expression, J Atheroscler Thromb, 2020, Sep 25 PMID: 32981917
- Wigle TJ, .et al. Forced Self-Modification Assays as a Strategy to Screen MonoPARP Enzymes, SLAS Discov, 2019, Dec 19:2472555219883623 PMID: 31855104
- Wang Q, .et al. Biguanides in combination with olaparib limits tumorigenesis of drug-resistant ovarian cancer cells through inhibition of Snail, Cancer Med, 2019, Dec 21 PMID: 31863638
- Molla S, .et al. PARP inhibitor Olaparib Enhances the Apoptotic Potentiality of Curcumin by Increasing the DNA Damage in Oral Cancer Cells through Inhibition of BER Cascade, Pathol Oncol Res, 2019, Nov 25 PMID: 31768967
- Alvin Z.Lu, .et al. Enabling drug discovery for the PARP protein family through the detection of mono-ADP-ribosylation, Biochem Pharmacol, 2019, May 7. pii: S0006-2952(19)30171-6 PMID: 31075269
- Bian C, .et al. NADP+ is an endogenous PARP inhibitor in DNA damage response and tumor suppression, Nat Commun, 2019, Feb 11;10(1):693 PMID: 30741937
- HC de Silva, .et al. IGFBP-3 interacts with NONO and SFPQ in PARP-dependent DNA damage repair in triple-negative breast cancer, Cell Mol Life Sci, 2019, 1-16 PMID: 30725116
- 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
- 2018, .et al. Augmentation of the therapeutic efficacy of WEE1 kinase inhibitor AZD1775 by inhibiting the YAP-E2F1-DNA damage response pathway axis, FEBS Open Bio, 2018, Jun; 8(6): 1001-1012 PMID: 29928579
- 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
- Hiro Sato, .et al. DNA double-strand break repair pathway regulates PD-L1 expression in cancer cells, Nat Commun, 2017, 8: 1751 PMID: 29170499
- Charles-André Philip, .et al. Inhibition of PI3K-AKT-mTOR pathway sensitizes endometrial cancer cell lines to PARP inhibitors, BMC Cancer, 2017, 17: 638 PMID: 28886696
- Rulina AV, .et al. Distinct outcomes of CRL-Nedd8 pathway inhibition reveal cancer cell plasticity, Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189
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AZD1152-HQPA (Barasertib)

Catalog No. A10109
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Aurora Kinase B 抑制剂

AZD1152-HQPA (Barasertib)是Aurora B的高效抑制剂，Ki值分别为0.36（Aurora B）和1369 nM（Aurora A），与一组其他50种激酶相比具有很高的特异性。了解更多

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- Sakamoto K, .et al. Recurrent 8q24 rearrangement in blastic plasmacytoid dendritic cell neoplasm: association with immunoblastoid cytomorphology, MYC expression, and drug response, Leukemia, 2018, May 23 PMID: 29795241
- Jennifer M. Sahni, .et al. Bromodomain and Extraterminal Protein Inhibition Blocks Growth of Triple-negative Breast Cancers through the Suppression of Aurora Kinases, J Biol Chem, 2016, Nov 4; 291(45): 23756-23768 PMID: 27650498
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AZD8055

Catalog No. A10114
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mTOR 抑制剂

AZD8055是一种有效的，选择性的ATP竞争性mTOR激酶抑制剂，IC50为0.8 nM。了解更多

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- L. M. C. Koene, .et al. Effects of antiepileptic drugs in a new TSC/mTOR-dependent epilepsy mouse model, ACTN, 2019, June PMID: 31353861
- Helga Weber, .et al. Rapamycin and WYE-354 suppress human gallbladder cancer xenografts in mice, Oncotarget, 2015, Oct 13; 6(31): 31877–31888 PMID: 26397134
- Kentaro Hirose, .et al. Mechanistic target of rapamycin complex 1 signaling regulates cell proliferation, cell survival, and differentiation in regenerating zebrafish fins, BMC Dev Biol, 2014, 14: 42. PMID: 25480380
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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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AZD6482

Catalog No. A10112
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PI3K 抑制剂

AZD6482是一种PI3Kβ抑制剂，(IC50 = 0.021M)。了解更多

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AZD8931 (Sapitinib)

Catalog No. A10116
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pan-EGFR/pan-erbB 抑制剂

AZD8931 (Sapitinib)是ErbB1，ErbB2和ErbB3受体信号传导的等效抑制剂。了解更多

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- Takeshi Ito, .et al. Mathematical analysis of gefitinib resistance of lung adenocarcinoma caused by MET amplification, Biochem Biophys Res Commun, 2019, in Press
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AZD7762

Catalog No. A10113
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Chk1 & Chk2 抑制剂

AZD7762是一种有效的ATP竞争性检查点激酶抑制剂，可促进检查点废止并增强DNA靶向疗法。了解更多

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MK-1775

Catalog No. A10599
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WEE1 抑制剂

MK-1775是一种有效的体外和体内Wee1激酶抑制剂。了解更多

Product Citations (3)

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- Ting-Yu Chang, .et al. A novel histone deacetylase inhibitor MPT0L184 dysregulates cell-cycle checkpoints and initiates unscheduled mitotic signaling, Biomed Pharmacother, 2021, Jun;138:111485 PMID: 33740521
- 2018, .et al. Augmentation of the therapeutic efficacy of WEE1 kinase inhibitor AZD1775 by inhibiting the YAP-E2F1-DNA damage response pathway axis, FEBS Open Bio, 2018, Jun; 8(6): 1001-1012 PMID: 29928579
- Rulina AV, .et al. Distinct outcomes of CRL-Nedd8 pathway inhibition reveal cancer cell plasticity, Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189
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AZD4547

Catalog No. A11075
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FGFR 抑制剂

AZD4547是一种有效，选择性和口服活性的pan-FGFR抑制剂，对于FGFR1、2、3和4的IC50分别为0.2、2.5、1.8和165 nM。了解更多

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- Ryuma Tokunaga, .et al. Fibroblast growth factor receptor 2 expression, but not its genetic amplification, is associated with tumor growth and worse survival in esophagogastric junction adenocarcinoma, Oncotarget, 2016, Apr 12; 7(15): 19748-19761 PMID: 26933914
- Mitsuko Kawano, .et al. FGF18 signaling in the hair cycle resting phase determines radioresistance of hair follicles by arresting hair cycling, Adv Radiat Oncol, 2016, Jul-Sep; 1(3): 170-181 PMID: 28740887
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AZD2014 (Vistusertib)

Catalog No. A11303
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mTORC1/2 抑制剂

Vistusertib (AZD2014)是一种新型mTOR抑制剂，无细胞试验中IC50为2.8 nM；对多种PI3K亚型(α/β/γ/δ)具有较高选择性。浓度为1 μM时，对大多数激酶无或有微弱结合力。了解更多

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- Shuhang Dai, .et al. Calcium/calmodulin-dependent protein kinase kinase 2 mediates pleiotropic effects of epidermal growth factor in cancer cells, Biochim Biophys Acta Mol Cell Res, 2022, Jul;1869(7):119252 PMID: 35271909
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AZD5363

Catalog No. A11759
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AKT 抑制剂

AZD5363是有效的AKT抑制剂，在体内具有药效学活性，有潜力作为单一疗法或联合用药来治疗一系列实体瘤和血液肿瘤。了解更多

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- Giri R. Gnawali, .et al. Synthesis of 2-oxoquinoline derivatives as dual pim and mTORC protein kinase inhibitors, Medicinal Chemistry Research, 2022, 31: 1154-1175
- Jeremiah J Bearss, .et al. EDC3 phosphorylation regulates growth and invasion through controlling P-body formation and dynamics, EMBO Rep, 2021, Apr 7;22(4):e50835 PMID: 33586867
- Jin H. Song, .et al. Mechanisms Behind Resistance to PI3K Inhibitor Treatment Induced by the PIM Kinase, Mol Cancer Ther, 2018, Dec;17(12):2710-2721 PMID: 30190422
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AZD1080

Catalog No. A12819
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GSK3 抑制剂

AZD1080是一种新型GSK3抑制剂，可消除啮齿动物大脑中的突触可塑性缺陷，并在人类中表现出外周靶标参与。了解更多

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- Shengzhong Liu, .et al. STAT1-avtiviated LINC00961 regulates myocardial infarction by the PI3K/AKT/GSK3?? signaling pathway, J Cell Biochem, 2019, 2019
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AZD3514

Catalog No. A12396
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AR 抑制剂 downregulator

AZD3514是一种有效的雄激素受体下调剂，具有潜在的抗癌活性。了解更多

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AZD1208

Catalog No. A13203
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pan-Pim kinase 抑制剂

AZD1208是PIM激酶的小分子抑制剂，具有潜在的抗肿瘤活性。了解更多

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- Remy J, .et al. Inhibition of PIM1 blocks the autophagic flux to sensitize glioblastoma cells to ABT-737-induced apoptosis, Biochim Biophys Acta Mol Cell Res, 2019, Feb;1866(2):175-189 PMID: 30389373
- Andrea L. Casillas, .et al. Hypoxia-inducible PIM kinase expression promotes resistance to anti-angiogenic agents, Clin Cancer Res, 2018, Jan 1; 24(1): 169-180 PMID: 29084916
- Jin H. Song, .et al. Mechanisms Behind Resistance to PI3K Inhibitor Treatment Induced by the PIM Kinase, Mol Cancer Ther, 2018, Dec;17(12):2710-2721 PMID: 30190422
- Sathish K.R. Padi, .et al. Targeting the PIM protein kinases for the treatment of a T-cell acute lymphoblastic leukemia subset, Oncotarget, 2017, May 2; 8(18): 30199-30216 PMID: 28415816
- Lim R, .et al. Inhibition of PIM1 kinase attenuates inflammation-induced pro-labour mediators in human foetal membranes in vitro, Mol Hum Reprod, 2017, Jun 1;23(6):428-440 PMID: 28333279
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AZD2858

Catalog No. A13060
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GSK-3β 抑制剂

AZD2858是一种选择性GSK-3抑制剂，IC50为68 nM，激活Wnt信号，增加大鼠的骨量。了解更多

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AZD1981

Catalog No. A13186
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CRTH2 receptor 拮抗剂

AZD1981作为疾病相关细胞系统的有效拮抗剂，可抑制DK-PGD2诱导的人嗜酸性粒细胞CD11b表达，IC50为10 nM。了解更多

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Alvelestat

Catalog No. A12779
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neutrophil elastase 抑制剂

Avelestat，也称为AZD9668，是可口服的,高度选择性neutrophil elastase (NE)抑制剂，IC50和Ki分别为12 nM和9.4 nM,其选择性超过其他丝氨酸蛋白酶至少600倍。了解更多

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AZD8186

Catalog No. A14164
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PI3K 抑制剂

AZD8186是磷酸肌醇-3激酶(PI3K)β亚型的抑制剂，具有潜在的抗肿瘤活性。了解更多

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AZD8186

Catalog No. A15759
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PI3K 抑制剂

AZD8186是一种同工型特异性小分子PI3K抑制剂，有效抑制PI3Kβ（IC50 = 4 nM）和PI3Kδ（IC50 = 12 nM），选择性高于PI3Kα（IC50 = 35 nM）和PI3Kγ（IC50 = 675 nM）。了解更多

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AZD6738 (Ceralasertib)

Catalog No. A15794
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ATR 抑制剂

AZD6738是一种有效的ATR激酶抑制剂，对分离的酶的IC50为1 nM，对细胞中ATR激酶依赖性CHK1磷酸化的IC50为74 nM。了解更多

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- Brian F Kiesel, .et al. Dose-dependent bioavailability and tissue distribution of the ATR inhibitor AZD6738 (ceralasertib) in mice, Cancer Chemother Pharmacol, 2022, Feb;89(2):231-242 PMID: 35066692
- Albert Job, .et al. The POLD1 R689W variant increases the sensitivity of colorectal cancer cells to ATR and CHK1 inhibitors, Sci Rep, 2020, Nov 3;10(1):18924 PMID: 33144657
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AZD1283

Catalog No. A15443
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P2Y12 receptor 拮抗剂

AZD1283是P2Y12受体的有效拮抗剂，EC50为3.0 ug/kg/min，TI> 10；结合IC50为11 nM。了解更多

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AZD 7545

Catalog No. A14157
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PDHK 抑制剂

AZD7545是PDHK2的新型选择性小分子抑制剂（PDH激酶2），对PDHK1和PDHK2的IC50分别为36.8 nM和6.4 nM。了解更多

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AZD-3965

Catalog No. A14186
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MCT1 抑制剂

AZD-3965（AZD3965）是具有1.6 nM结合亲和力的单羧酸盐转运蛋白1（MCT1）的选择性抑制剂，是MCT2的6倍选择性，在10μM时不抑制MCT4。了解更多

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- Lu Gao, .et al. Trophoblast-derived Lactic Acid Orchestrates Decidual Macrophage Differentiation via SRC/LDHA Signaling in Early Pregnancy, Int J Biol Sci, 2022, Jan 1;18(2):599-616 PMID: 35002512
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AZD-2461

Catalog No. A12393
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PARP 抑制剂

AZD2461是新型有效的PARP抑制剂，对P-糖蛋白的亲和力较低。了解更多

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AZD-9291 (Osimertinib)

Catalog No. A13681
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EGFR 抑制剂

AZD-9291 (Osimertinib)是第三代EGFR抑制剂，在临床前研究中显示出希望，并为已对现有EGFR抑制剂产生耐药性的晚期肺癌患者提供了希望。了解更多

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- Liu YN, .et al. Acquired resistance to EGFR tyrosine kinase inhibitors is mediated by the reactivation of STC2/JUN/AXL signaling in lung cancer, Int J Cancer, 2019, Jun 4 PMID: 31162839

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