[CAS NO. 1123837-84-2] Sitravatinib (MGCD516)

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Catalog:	SLK-S8573
Brand:	Selleck
CAS:	1123837-84-2

Overview

MDL	-
Molecular Weight	629.68
Molecular Formula	C33H29F2N5O4S
SMILES	C(NC1=CC(F)=C(OC2=C3C(C=C(S3)C4=CC=C(CNCCOC)C=N4)=NC=C2)C=C1)(=O)C5(C(NC6=CC=C(F)C=C6)=O)CC5

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

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Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.5881 mL	7.9405 mL	15.8811 mL
5 mM	0.3176 mL	1.5881 mL	3.1762 mL
10 mM	0.1588 mL	0.7941 mL	1.5881 mL
50 mM	0.0318 mL	0.1588 mL	0.3176 mL

Description

Sitravatinib (MGCD516, MG-516) is a novel small molecule inhibitor targeting multiple involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.

Targets

In vitro

MGCD516 (Sitravatinib), is an oral, potent small molecule inhibitor of a closely related spectrum of RTKs including RET, the split RTKs (VEGFR, PDGFR and KIT), TRK family, DDR2, MET and AXL. MGCD516 treatment resulted in significant blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects in vitro.

In vivo

Sitravatinib has demonstrated antitumor activity in nonclinical cancer models harboring genetic alterations of sitravatinib targets, including rearrangement of RET, NTRK, or CHR4q12 amplification. MGCD516 treatment of tumor xenografts in vivo resulted in significant suppression of tumor growth. Efficacy of MGCD516 was superior to imatinib and crizotinib, two other well-studied multi-kinase inhibitors with overlapping target specificities, both in vitro and in vivo.

References

[1] Theresa Werner, et al. Journal of Thoracic Oncology. 2017, 12(1S):S1068-S1069.
[2] Patwardhan PP, et al. Oncotarget. 2016, 7(4):4093-109.

Synonyms

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)-

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

Sitravatinib

MGCD 516

N-(3-fluoro-4-{[2-(5-{[(2-methoxyethyl)amino]methyl}pyridin-2-yl)thieno[3,2-b]pyridin-7-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

1-N′-[3-Fluoro-4-[2-[5-[(2-methoxyethylamino)methyl]pyridin-2-yl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

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