Sitravatinib, Multikinase inhibitor / Immuno-oncology agent (TBI4826)

Description

Product Details

Formal Name: 1-N’-[3-Fluoro-4-[2-[5-[(2-methoxyethylamino)methyl]pyridin-2-yl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

Alternate Names: MGCD516

Molecular Formula: C₃₃H₂₉F₂N₅O₄S

Formula Weight: 629.68

CAS Number: 1123837-84-2

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml) or in Ethanol (up to at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

Multikinase inhibitor / Immuno-oncology agent

Functions

Sitravatinib is a broad spectrum receptor tyrosine kinase inhibitor. Its targets include Axl, c-Met, PDGFR, VEGFR, Ephrin receptor family, and FLT3 among others at nanomolar levels. Sitravatinib has been tested in mouse models of sarcoma and showed better efficacy than both imatinib and crizotinib. Because of its unique kinase inhibition profile (especially that of TAM receptors), it has been used to restore response to anti-PD-1 therapy (nivolumab) in NSCLC patients. Sitravatinib was able to significantly alter the immunosuppressive tumor microenvironment in three preclinical tumor models to enhance the effects of PD-1 blockade therapy.

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml) or in Ethanol (up to at least 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.