Chemical 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
Multikinase inhibitor / Immuno-oncology agent
Molecular Weight:
629.68
Purity:
98% by HPLC NMR (Conforms)
Form:
Off-white solid
CAS Number:
[1123837-84-2]
Formula:
C33H29F2N5O4S
Application Notes:
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.1 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.2 Sitravatinib was able to significantly alter the immunosuppressive tumor microenvironment in three preclinical tumor models to enhance the effects of PD-1 blockade therapy.3
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