Sitravatinib (MGCD516)

Names

[ Name ]:
Sitravatinib (MGCD516)

[Synonym ]:
UNII:CWG62Q1VTB
CWG62Q1VTB
MGCD516
Sitravatinib
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

Biological Activity

[Description]:

Sitravatinib is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth with IC50 of 3980 nmol/Lin vitro: MGCD516 is superior to other multi-kinase inhibitors in inhibiting cell proliferation, RTK phosphorylation, and phosphorylation of downstream effectors. MGCD516 is unique in a way that it has broad spectrum activity against many RTKs including c-Met, c-Kit, Axl, PDGFR, and Eph receptors that are known to play a role in driving sarcoma cell growthIn vivo: MGCD516 induces significant tumor growth suppression than imatinib and crizotinib.

[Related Catalog]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Kit

Research Areas >> Cancer

[References]

[1]. Patwardhan PP et al. Significant blockade of multiple receptor tyrosine kinases by MGCD516 (Sitravatinib), a novel small molecule inhibitor, shows potent anti-tumor activity in preclinical models of sarcoma. Oncotarget, 2016 Jan 26;7(4):4093-109.

[Related Small Molecules]

Pexidartinib | Masitinib (AB1010) | SU14813 | Dovitinib (TKI-258, CHIR-258) | DCC-2618 | BLU-285 | Motesanib | OSI-930 | AST 487 | DCC-2618 | Telatinib | Amuvatinib (MP-470) | Flumatinib | AC 710 | AZD2932

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
833.5±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₃₃H₂₉F₂N₅O₄S

[ Molecular Weight ]:
629.676

[ Flash Point ]:
457.9±34.3 °C

[ Exact Mass ]:
629.190857

[ LogP ]:
6.00

[ Vapour Pressure ]:
0.0±3.1 mmHg at 25°C

[ Index of Refraction ]:
1.685

[ Storage condition ]:
-20℃

Related Compounds

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