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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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PLX4032 (Vemurafenib)

Catalog No. A10739
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Raf 抑制剂

PLX4032(Vemurafenib)也称为RG7204，Vemurafenib，R7204，RO5185426。PLX4032是B-raf抑制剂，IC50为44 nM。了解更多

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- Lee YJ, .et al. Overexpression of Dock180 and Elmo1 in melanoma is associated with cell survival and migration, Research Square, 2022, April 27th
- 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
- Guixin Zhu, .et al. TRIM15 and CYLD regulate ERK activation via lysine-63-linked polyubiquitination, Nat Cell Biol, 2021, Sep;23(9):978-991 PMID: 34497368
- 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
- Kudo K, .et al. Cell surface CD63 increased by up-regulated polylactosamine modification sensitizes human melanoma cells to the BRAF inhibitor PLX4032, FASEB J, 2018, Dec 3:fj201800664RR PMID: 30508500
- Min Ho Choe, .et al. miR-550a-3-5p acts as a tumor suppressor and reverses BRAF inhibitor resistance through the direct targeting of YAP, Cell Death Dis, 2018, Jun; 9(6): 640 PMID: 29844307
- Jan Dorrie, .et al. BRAF and MEK Inhibitors Influence the Function of Reprogrammed T Cells: Consequences for Adoptive T-Cell Therapy, Int J Mol Sci, 2018, Jan; 19(1): 289 PMID: 29346301
- Aishwarya Kundu, .et al. Inhibition of Oncogenic BRAF Activity by Indole-3-Carbinol Disrupts Microphthalmia-Associated Transcription Factor Expression and Arrests Melanoma Cell Proliferation, Mol Carcinog, 2017, Jan; 56(1): 49-61 PMID: 26878440
- 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
- Toshinori Sueda, .et al. BRAFV600E inhibition stimulates AMP-activated protein kinase-mediated autophagy in colorectal cancer cells, Sci Rep, 2016, 6: 18949 PMID: 26750638
- Yanling Li, .et al. Tyrphostin AG1296, a platelet-derived growth factor receptor inhibitor, induces apoptosis, and reduces viability and migration of PLX4032-resistant melanoma cells, Onco Targets Ther, 2015, 8: 1043-1051 PMID: 25999739
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PIK-93

Catalog No. A10731
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PI3K 抑制剂

PIK-93是第一个有效的，人工合成的PI4K(PI4KIIIβ)抑制剂，IC50为19 nM；抑制PI3Kα，IC50为39 nM。了解更多

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- Gavin Ka Yu Siu, .et al. Hepatitis C virus NS5A protein cooperates with phosphatidylinositol 4-kinase IIIα to induce mitochondrial fragmentation, Sci Rep, 2016, 6: 23464 PMID: 27010100
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CP-690550 (Tofacitinib citrate)

Catalog No. A10241
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JAK3 抑制剂

CP-690550 (Tofacitinib citrate)是口服的高选择性Janus激酶（JAK）酶抑制剂。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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Pimobendan (Vetmedin)

Catalog No. A10733
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PDE 抑制剂

Pimobendan (Vetmedin)是一种钙增敏剂，具有正性肌力和血管舒张作用。它也是磷酸二酯酶III（PDE3）的选择性抑制剂。了解更多

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Safinamide Mesylate (FCE28073)

Catalog No. A10818
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MAO 抑制剂

Safinamide Mesylate是沙芬酰胺的甲磺酸盐，可选择性和可逆地抑制MAO-B，IC50为0.45μM。了解更多

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GDC-0349

Catalog No. A11443
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mTOR 抑制剂

GDC-0349是一种有效的，选择性的，ATP竞争性的mTOR抑制剂，Ki为3.8 nM，比作用于PI3Kα和其他266种激酶的抑制效果高790倍。了解更多

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Piroxicam (Feldene)

Catalog No. A10736
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COX 抑制剂

Piroxicam (Feldene)是前列腺素合成的有效抑制剂，并且是Cox-1和Cox-2抑制剂。了解更多

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Pitavastatin calcium (Livalo)

Catalog No. A10737
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HMG-CoA reductase 抑制剂

Pitavastatin calcium (Livalo)是HMGCR（HMG-CoA还原酶）酶的竞争性抑制剂，可降低LDL胆固醇的合成。了解更多

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- Weizhen Chen, .et al. An improved osseointegration of metal implants by pitavastatin loaded multilayer films with osteogenic and angiogenic properties, Biomaterials, 2021, 280:121260 PMID: 34823885
- Karis Tutuska, .et al. Statin as anti-cancer therapy in autochthonous T-lymphomas expressing stabilized gain-of-function mutant p53 proteins, Cell Death Dis, 2020, Apr; 11(4): 274 PMID: 32332697
- D Jarmuzek, .et al. Phototransformations of pitavastatin - The inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase, J Photochem Photobiol A Chem, 2019, November
- Marwan Ibrahim Abdullah, .et al. Inhibition of the mevalonate pathway augments the activity of pitavastatin against ovarian cancer cells, Sci Rep, 2017, 7: 8090 PMID: 28808351