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MedKoo Cat#: 462200 | Name: Sitravatinib malate

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

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

Theoretical Analysis

MedKoo Cat#: 462200

Name: Sitravatinib malate

CAS#: 2244864-88-6 (malate)

Chemical Formula: C37H35F2N5O9S

Exact Mass: 763.2124

Molecular Weight: 763.77

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 currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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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

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
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