CS-2638
Sitravatinib
CAS: 1123837-84-2
Molecular Formula: C33H29F2N5O4S
CS-2638 - Names and Identifiers
| Name | Sitravatinib |
| Synonyms | MG516 CS-2638 Sitravatinib 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)- |
| CAS | 1123837-84-2 |
CS-2638 - Physico-chemical Properties
| Molecular Formula | C33H29F2N5O4S |
| Molar Mass | 629.6763 |
| Density | 1.417±0.06 g/cm3(Predicted) |
| Boling Point | 833.5±65.0 °C(Predicted) |
| Solubility | DMSO: ≥ 32 mg/mL |
| Appearance | Form solid, color Off-white |
| pKa | 13.17±0.70(Predicted) |
| Storage Condition | -20°C |
| 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. |
| Physical and Chemical Properties | Bioactive Sitravatinib (MGCD516, MG-516) is a new type of small molecule inhibitor targeting various RTKs involved in regulating the growth of S180 sarcoma cells, including c-Kit, PDGFRβ, PDGFRα, c-Met and Axl. |
CS-2638 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.588 ml | 7.941 ml | 15.881 ml |
| 5 mM | 0.318 ml | 1.588 ml | 3.176 ml |
| 10 mM | 0.159 ml | 0.794 ml | 1.588 ml |
| 5 mM | 0.032 ml | 0.159 ml | 0.318 ml |
Last Update：2024-01-02 23:10:35
CS-2638 - Uses and synthesis methods
Target
Target Value
DDR2
(Cell-free assay) 0.5 nM
EPHA3
(Cell-free assay) 1 nM
Axl
(Cell-free assay) 1.5 nM
Mer
(Cell-free assay) 2 nM
VEGFR3 (FLT4)
(Cell-free assay) 2 nM
in vitro studies
MGCD516 (Sitravatinib) is an oral small molecule inhibitor that inhibits a group of closely related RTKs, including RET, split RTKs(VEGFR, PDGFR and KIT), TRK family, DDR2 and Axl. MGCD516 result in the phosphorylation of potential drivers RTKs being significantly inhibited and effective antiproliferative effects induced in vitro.
In vivo studies
In non-clinical cancer models containing sitravatinib targets with genetic variants (including RET, NTRK or CHR4q12 amplification), Sitravatinib have anti-tumor activity. In vivo MGCD516 administration of xenograft tumor models can significantly inhibit tumor growth, and its effect is better than that of imatinib and crizotinib (two fully studied multi-kinase inhibitors have overlapping target specificity).
Last Update：2024-04-10 22:41:03
CS-2638 - Nature
| Solubility | Soluble in DMSO (up to at least 25 mg/ml), or in Ethanol (up to at least 25 mg/ml) |
Last Update：2024-04-09 01:59:50
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CAS: 1123837-84-2
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Product Name: Sitravatinib Visit Supplier Webpage Request for quotation
CAS: 1123837-84-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1123837-84-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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