| Identification | Back Directory | [Name]
Sitravatinib | [CAS]
1123837-84-2 | [Synonyms]
MG516
CS-2638
MGCD-516
Sitravatinib
Sitravatinib (MGCD516)
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
1,1-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)- | [Molecular Formula]
C33H29F2N5O4S | [MDL Number]
MFCD28502181 | [MOL File]
1123837-84-2.mol | [Molecular Weight]
629.68 |
| Chemical Properties | Back Directory | [Boiling point ]
833.5±65.0 °C(Predicted) | [density ]
1.417±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO (up to at least 25 mg/ml), or in Ethanol (up to at least 25 mg/ml) | [form ]
solid | [pka]
13.17±0.70(Predicted) | [color ]
Off-white | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month. |
| Hazard Information | Back Directory | [Description]
Sitravatinib, known as MGCD516, is a multikinase (MET, RET, AXL, NTRK1, or NTRK3 genes) inhibitor used in a phase 1/1b clinical trial (NCT02219711) for patients with advanced cancers (NCT02219711). | [Uses]
MGCD 516 is an intermediate used to prepare substituted thienopyridines as inhibitors of protein tyrosine kinase activity. | [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[2]. | Animal Model: | 6-week-old C57BL/6 mice (bearing CT1B-A5 cells) [2] | | Dosage: | 20 mg/kg | | Administration: | Oral administration; once per day for 6 days | | Result: | Significantly inhibited tumor progression and induced tumor regression. |
| [IC 50]
Axl: 1.5 nM (IC50); MER: 2 nM (IC50); VEGFR3: 2 nM (IC50); VEGFR2: 5 nM (IC50); VEGFR1: 6 nM (IC50); TrkA: 5 nM (IC50); TrkB: 9 nM (IC50); KIT: 6 nM (IC50); FLT3: 8 nM (IC50); DDR2: 0.5 nM (IC50); DDR1: 29 nM (IC50) | [storage]
Store at -20°C | [References]
1) Parag?et al.?(2016)?Significant blockade of multiple receptor kinases by MGCD516 (Sitravatinib), a novel small molecule inhibitor, shows potent anti-tumor activity in preclinical models of sarcoma; Oncotarget?7?4093
2) Leal?et al.?(2017)?Evidence of clinical activity of sitravatinib in combination with nivolumab in NSCLC patients progressing on prior checkpoint inhibitors; J. Thorac. Oncol.?12?S1803
3) Du?et al.?(2018);?Sitravatinib potentiates immune checkpoint blockade in refractory cancer models; JCI Insight?3?124184 |
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