Famitinib

Famitinib (SHR1020), an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively. Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts. Famitinib triggers apoptosis. Famitinib is a novel multi-targeted receptor tyrosine kinase inhibitor under development for cancer treatment. Famitinib is a structural analogue of sunitinib, is a novel and potent multi-targeted RTK inhibitor that is currently undergoing phase II clinical trials in China for the treatment of renal cell carcinoma, gastrointestinal stromal tumours, pancreatic cancer, and nasopharyngeal carcinoma. Compared with sunitinib, famitinib exhibits superior inhibition activities against multiple RTKs.

Product information

CAS Number: 1044040-56-3

Molecular Weight: 410.48

Formula: C23H27FN4O2

Chemical Name: (3Z)-3-({5-[2-(diethylamino)ethyl]-3-methyl-4-oxo-1H, 4H, 5H, 6H, 7H-pyrrolo[3, 2-c]pyridin-2-yl}methylidene)-5-fluoro-2, 3-dihydro-1H-indol-2-one

Smiles: CC1C2C(=O)N(CCC=2NC=1/C=C1\C(=O)NC2=CC=C(F)C=C\12)CCN(CC)CC

InChiKey: GKEYKDOLBLYGRB-LGMDPLHJSA-N

InChi: InChI=1S/C23H27FN4O2/c1-4-27(5-2)10-11-28-9-8-19-21(23(28)30)14(3)20(25-19)13-17-16-12-15(24)6-7-18(16)26-22(17)29/h6-7,12-13,25H,4-5,8-11H2,1-3H3,(H,26,29)/b17-13-

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: To be determined

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Famitinib inhibits the VEGF-induced proliferation, migration and tubule formation of human umbilical vein endothelial cells, and micro-vessel spouting from matrigel-embedded rat aortic rings. Famitinib inhibits cell proliferation by inducing cell cycle arrest at the G2/M phase and causes cell apoptosis in a dose-dependent manner in gastric cancer cell lines. Famitinib (0.6-20.0 µM) inhibits gastric cancer cell growth in a dose-dependent manner.

In Vivo:

Famitinib exhibits broad and potent anti-tumor activity, leading to regression or growth arrest of various established xenografts derived from human tumor cell lines . Famitinib significantly slows tumor growth in vivo via inhibition of angiogenesis in BGC-823 xenograft models. Famitinib (50 and 100 mg/kg;gavage) reduces xenograft growth in vivo via inhibition of angiogenesis.

References:

1. Xie C, Zhou J, Guo Z, Diao X, Gao Z, Zhong D, Jiang H, Zhang L, Chen X. Metabolism and Bioactivation of Famitinib, a Novel Inhibitor of Receptor Tyrosine Kinase, in Cancer Patients. Br J Pharmacol. 2012 Nov 6. doi: 10.1111/bph.12047. [Epub ahead of print] PubMed PMID: 23126373.
2. Sai Ge, et al. Famitinib exerted powerful antitumor activity in human gastric cancer cells and xenografts. Oncol Lett. 2016 Sep;12(3):1763-1768.

Products are for research use only. Not for human use.