Famitinib - CAS 945380-27-8
Catalog number: 945380-27-8
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C23H27FN4O2
Molecular Weight:
410.493
COA:
Inquire
Description:
Famitinib is a novel multi-targeted receptor tyrosine kinase inhibitor under development for cancer treatment.  Famitinib is a structural analogue ofsunitinib, 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.
Synonyms:
Famitinib; SHR1020; SHR 1020; SHR-1020
MSDS:
Inquire
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-
Canonical SMILES:
CCN(CC)CCN1CCC2=C(C1=O)C(=C(N2)C=C3C4=C(C=CC(=C4)F)NC3=O)C
Current Developer:
Jiangsu Hengrui Medicine Co. Ltd. China
1.Famitinib enhances nasopharyngeal cancer cell radiosensitivity by attenuating radiation-induced phosphorylation of platelet-derived growth factor receptor and c-kit and inhibiting microvessel formation.
Mu X1,2, Ma J1, Zhang Z1, Zhou H1, Xu S1, Qin Y1, Huang J1, Yang K1, Wu G1. Int J Radiat Biol. 2015;91(9):771-6. doi: 10.3109/09553002.2015.1062574. Epub 2015 Sep 21.
PURPOSE: Famitinib is a novel tyrosine kinase inhibitor. We investigated the effects of famitinib on the radiosensitivity of human nasopharyngeal carcinoma (NPC) cell radiosensitivity in vitro and in vivo, and explored its possible mechanisms.
2.Hypothyroidism as a potential biomarker of efficacy of famitinib, a novel VEGFR-2 inhibitor in metastatic breast cancer.
Cao J1, Zhang J, Wang Z, Wang B, Lv F, Wang L, Hu X. Cancer Chemother Pharmacol. 2014 Aug;74(2):389-98. doi: 10.1007/s00280-014-2505-x. Epub 2014 Jun 18.
PURPOSE: Hypothyroidism is a common adverse event in patients treated with anti-VEGFR-2 targeting agents and may be a valuable predictive factor of efficacy. Famitinib is an inhibitor of multiple tyrosine kinases mainly targeting VEGFR-2. The objectives of this study were to assess the efficacy and safety of famitinib in patients with pretreated HER2-negative metastatic breast cancer (MBC) and to explore potential of famitinib-induced hypothyroidism and serum vascular endothelial growth factor (VEGF) level for efficacy prediction.
3.[Predicting pharmacokinetics of anti-cancer drug, famitinib in human using physiologically based pharmacokinetic model].
Yu MM, Gao ZW, Chen XY, Zhong DF. Yao Xue Xue Bao. 2014 Dec;49(12):1684-8.
This study is to establish physiologically based pharmacokinetic (PBPK) models of famitinib in rat and monkey, and then to predict the pharmacokinetics and tissue distribution of famitinib in human based on the PBPK models. According to published paper, previous studies and the chemical properties of famitinib predicted by ACD/ADME suite and SimCYP, the PBPK models of rat and monkey were established and optimized using GastroPlus. And then, the PBPK models were applied to predict the pharmacokinetic and tissue distribution of famitinib in human. The results showed that the PBPK models of rat and monkey can fit the observed data well, and the AUC0-∞, ratios of observed and calculated data in rat and monkey were 1.00 and 0.97, respectively. The AUC0-∞, ratios of observed and predicted data in human were 1.63 (rat to human) and 1.57 (monkey to human), respectively. The rat and monkey PBPK models of famitinib were well established, and the PBPK models were applied in predicting pharmacokinetic of famitinib in human successfully.
4.Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients.
Xie C1, Zhou J, Guo Z, Diao X, Gao Z, Zhong D, Jiang H, Zhang L, Chen X. Br J Pharmacol. 2013 Apr;168(7):1687-706. doi: 10.1111/bph.12047.
BACKGROUND AND PURPOSE: Famitinib is a novel multi-targeted receptor tyrosine kinase inhibitor under development for cancer treatment. This study aims to characterize the metabolic and bioactivation pathways of famitinib.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Products


CAS 60525-15-7 Zimelidine dihydrochloride

Zimelidine dihydrochloride
(CAS: 60525-15-7)

Zimelidine dihydrochloride is a 5-HT reuptake inhibitor with selectivity over noradrenalin and dopamine uptake (IC50 = 0.33, 8.2 and 12 μM, respectively). Zimel...

CH100
(CAS: 51346-20-4)

CH100 is a Chinese herbal medicine. It is previously used in the treatment of human hepatitis C.

CDK2

CDK2, a member of the eukaryotic S/T protein kinase family, catalyzes the phosphoryl transfer of ATP γ-phosphate to serine or threonine hydroxyl (denoted as S0/...

CAS 16941-32-5 Glucagon (swine)

Glucagon (swine)
(CAS: 16941-32-5)

Glucagon, a peptide compound, is effective in increasing the glucose concentration in bloodstream and could be released by pancrea α cells.

CAS 566203-88-1 AZD 2098

AZD 2098
(CAS: 566203-88-1)

AZD 2098 is a potent and selective CCR4 receptor antagonist (pIC50 = 7.8) used for the treatment of allergic rhinitis. CCR4 is a molecule that can drive the imm...

CAS 10163-15-2 Sodium Monofluorophosphate

Sodium Monofluorophosphate
(CAS: 10163-15-2)

Sodium Monofluorophosphate is a competitive inhibitor of pyruvate kinase and alkaline phosphatase with Ki of 3.4 mM and 69 μM, respectively, which also irrevers...

Ribuvaptan
(CAS: 1245620-47-6)

Ribuvaptan is a vasopressin receptor antagonist originated by Bayer HealthCare Pharmaceuticals. Now, Ribuvaptan is still in phase I development for the treatmen...

CAS 864070-44-0 Empagliflozin

Empagliflozin
(CAS: 864070-44-0)

Empagliflozin is a potent and selective SGLT-2 inhibitor with IC50 of 3.1 nM, exhibits >300-fold selectivity over SGLT-1, 4, 5 and 6.

Chemical Structure

CAS 945380-27-8 Famitinib

Quick Inquiry

Verification code

Featured Items