Sitravatinib malate

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MedKoo CAT#: 462200

CAS#: 2244864-88-6 (malate)

Description: Sitravatinib, also known as MGCD516 or MG516, is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth. MGCD516 treatment resulted in significant blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects in vitro. MGCD516 treatment of tumor xenografts in vivo resulted in significant suppression of tumor growth.t.

Chemical Structure

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Sitravatinib malate
CAS# 2244864-88-6 (malate)
Instruction

Theoretical Analysis

MedKoo Cat#: 462200
Name: Sitravatinib malate
CAS#: 2244864-88-6 (malate)
Chemical Formula: C37H35F2N5O9S
Exact Mass: 763.21
Molecular Weight: 763.770
Elemental Analysis: C, 58.19; H, 4.62; F, 4.97; N, 9.17; O, 18.85; S, 4.20

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Related CAS #: 2244864-88-6 (malate)   1123837-84-2 (free base)    

Synonym: Sitravatinib malate; MGCD516 malate; MG-516 malate

IUPAC/Chemical Name: 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 (S)-2-hydroxysuccinate

InChi Key: GDLGZWLGDROYHH-WNQIDUERSA-N

InChi Code: InChI=1S/C33H29F2N5O4S.C4H6O5/c1-43-15-14-36-18-20-2-8-25(38-19-20)29-17-26-30(45-29)28(10-13-37-26)44-27-9-7-23(16-24(27)35)40-32(42)33(11-12-33)31(41)39-22-5-3-21(34)4-6-22;5-2(4(8)9)1-3(6)7/h2-10,13,16-17,19,36H,11-12,14-15,18H2,1H3,(H,39,41)(H,40,42);2,5H,1H2,(H,6,7)(H,8,9)/t;2-/m.0/s1

SMILES Code: FC1=CC(NC(C2(CC2)C(NC3=CC=C(F)C=C3)=O)=O)=CC=C1OC4=C5C(C=C(C6=NC=C(CNCCOC)C=C6)S5)=NC=C4.OC(C[C@H](O)C(O)=O)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 763.77 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Patwardhan PP, Ivy KS, Musi E, de Stanchina E, Schwartz GK. 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;7

2: Du W, Huang H, Sorrelle N, Brekken RA. Sitravatinib potentiates immune checkpoint blockade in refractory cancer models. JCI Insight. 2018;3(21):e124184. Published 2018 Nov 2. doi:10.1172/jci.insight.1241844):4093-4109. doi:10.18632/oncotarget.6547