1044040-56-3

1044040-56-3 structure

Name: Famitinib (SHR1020)
Chemical Name: FAMITINIB
CAS Number: 1044040-56-3
Molecular Formula: C₂₃H₂₇FN₄O₂
Molecular Weight: 410.48
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2018-07-10 03:10:49
Modify Date: 2024-01-22 16:16:22
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[1]. Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts.Famitinib triggers apoptosis[2].

Name	FAMITINIB
Synonyms	768FW21J3L 4H-Pyrrolo[3,2-c]pyridin-4-one, 5-[2-(diethylamino)ethyl]-2-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-1,5,6,7-tetrahydro-3-methyl- 5-[2-(Diethylamino)ethyl]-2-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-3-methyl-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one FAMITINIB Famitinib (SHR1020)

Description	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[1]. Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts.Famitinib triggers apoptosis[2].
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PDGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR
Target	VEGFR-2:4.2 nM (IC50) PDGFRβ:6.6 nM (IC50) c-kit:2.3 nM (IC50)
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[1]. 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[2]." Cell Proliferation Assay[3] Cell Line: Human gastric cancer cells BGC-823 and MGC-803 Concentration: 0, 0.6, 1.25, 2.5, 5.0, 10.0 and 20.0 µM Incubation Time: 24, 48 and 72 hours Result: Inhibited cell growth in a dose-dependent manner. The IC50 values in BGC-823 and MGC-803 cells were 3.6 and 3.1 µM, respectively.
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 [1]. 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[2]." Animal Model: 18-20 g female BALB/c athymic nu/nu mice (age, 6–8 weeks) bearing BGC-823 xenografts[4] Dosage: 50 and 100 mg/kg Administration: Gavage, once daily for 3 weeks Result: Both doses exerted a similar inhibitory power, but greater toxicity was observed. Inhibited BGC-823 xenograft growth (tumor volume, 395.2 vs. 2,690.5 mm3), and animal weights were similar between groups (21.6 vs. 18.7 g).
References	[1]. Liguang Lou, et al. Abstract 3604: Preclinical antitumor study of famitinib, an orally available multi-targeted kinase inhibitor of VEGFR/PDGFR/c-Kit in phase I clinical trials. [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.

Density	1.3±0.1 g/cm3
Boiling Point	677.1±55.0 °C at 760 mmHg
Molecular Formula	C₂₃H₂₇FN₄O₂
Molecular Weight	410.48
Flash Point	363.3±31.5 °C
Exact Mass	410.211792
LogP	2.61
Vapour Pressure	0.0±2.1 mmHg at 25°C
Index of Refraction	1.628