Sitravatinib

Research use only, not for human use.

A novel, broad spectrum small molecule inhibitor that blocks a wide array of RTKs known to be amplified/overexpressed in sarcomas, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl (IC50=1.5-30 nM).

A novel, broad spectrum small molecule inhibitor that blocks a wide array of RTKs known to be amplified/overexpressed in sarcomas, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl (IC50=1.5-30 nM); significantly blocks the phosphorylation of potential driver RTKs and induces potent anti-proliferative effects in vitro; suppresses tumor growth in tumor xenografts in vivo.Lung Cancer Phase 2 Clinical(In Vitro):Sitravatinib (0.01 nM-10 μM; 14 days) reduces colony formation in a dose-dependent manner in KLN205 and E0771 cell lines.Sitravatinib (0.001-10 μM; 5 days) inhibits tumor cell viability with IC50s of approximately 1 μM in KLN205, E0771 and CT1B-A5 cell lines.(In Vivo):Sitravatinib (20 mg/kg; p.o.; once per day for 6 days) significantly inhibits tumor progression and induces tumor regression in C57BL/6 mice bearing CT1B-A5 cells model.

——

Animal Model:6-week-old C57BL/6 mice (bearing CT1B-A5 cells) Dosage:20 mg/kg Administration:Oral administration; once per day for 6 days Result:Significantly inhibited tumor progression and induced tumor regression.

MGCD-516 | MG-516

Angiogenesis

c-Kit

DDR2|EPHA3|Axl|Mer|VEGFR3(FLT4)

Cancer

Lung Cancer

1123837-84-2

629.6763

C33H29F2N5O4S

>98% (HPLC)

DMSO: ≥ 32 mg/mL

O=C(C1(C(NC2=CC=C(F)C=C2)=O)CC1)NC3=CC=C(OC4=C5C(C=C(C6=NC=C(CNCCOC)C=C6)S5)=NC=C4)C(F)=C3

1,1-Cyclopropanedicarboxamide, N-[3-fluoro-4-[[2-[5-[[(2-methoxyethyl)amino]methyl]-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxy]phenyl]-N'-(4-fluorophenyl)-

(-20℃)

With Ice Pack

≥ 2 years