Sitravatinib - CAS 1123837-84-2
Catalog number: 1123837-84-2
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C33H29F2N5O4S
Molecular Weight:
629.68
COA:
Inquire
Targets:
c-Kit
Description:
Sitravatinib, a new inhibitor of tyrosine kinase, has been studied to have effective in inhibiting tyrosine kinases receptors involved in driving sarcoma cell growth. It is still under a phase II trial for Non small cell lung cancer. IC50: 3980 nmol/L.
Purity:
98%
Appearance:
Powder
Synonyms:
MGCD516; MGCD-516; MGCD 516; MG516; MG 516; MG-516; Sitravatinib
Solubility:
Soluble in DMSO, not in water
Storage:
-20ºC Freeze
MSDS:
Inquire
Application:
Sitravatinib has been studied to have effective in inhibiting tyrosine kinases receptors involved in driving sarcoma cell growth. It is still under a phase II trial for Non small cell lung cancer.
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
InChIKey:
WLAVZAAODLTUSW-UHFFFAOYSA-N
InChI:
InChI=1S/C33H29F2N5O4S/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/h2-10,13,16-17,19,36H,11-12,14-15,18H2,1H3,(H,39,41)(H,40,42)
Canonical SMILES:
COCCNCC1=CN=C(C=C1)C2=CC3=NC=CC(=C3S2)OC4=C(C=C(C=C4)NC(=O)C5(CC5)C(=O)NC6=CC=C(C=C6)F)F
Current Developer:
Mirati Therapeutics
1.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.
Patwardhan PP;Ivy KS;Musi E;de Stanchina E;Schwartz GK Oncotarget. 2016 Jan 26;7(4):4093-109. doi: 10.18632/oncotarget.6547.
Sarcomas are rare but highly aggressive mesenchymal tumors with a median survival of 10-18 months for metastatic disease. Mutation and/or overexpression of many receptor tyrosine kinases (RTKs) including c-Met, PDGFR, c-Kit and IGF1-R drive defective signaling pathways in sarcomas. MGCD516 (Sitravatinib) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth. In the present study, we evaluated the efficacy of MGCD516 both in vitro and in mouse xenograft models in vivo. MGCD516 treatment resulted in significant blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects in vitro. Furthermore, MGCD516 treatment of tumor xenografts in vivo resulted in significant suppression of tumor growth. Efficacy of MGCD516 was superior to imatinib and crizotinib, two other well-studied multi-kinase inhibitors with overlapping target specificities, both in vitro and in vivo. This is the first report describing MGCD516 as a potent multi-kinase inhibitor in different models of sarcoma, superior to imatinib and crizotinib. Results from this study showing blockade of multiple driver signaling pathways provides a rationale for further clinical development of MGCD516 for the treatment of patients with soft-tissue sarcoma.
2.Targeting TRK family proteins in cancer.
Khotskaya YB;Holla VR;Farago AF;Mills Shaw KR;Meric-Bernstam F;Hong DS Pharmacol Ther. 2017 May;173:58-66. doi: 10.1016/j.pharmthera.2017.02.006. Epub 2017 Feb 4.
The tropomyosin receptor kinase (TRK) family includes TRKA, TRKB, and TRKC proteins, which are encoded by NTRK1, NTRK2 and NTRK3 genes, respectively. Binding of neurotrophins to TRK proteins induces receptor dimerization, phosphorylation, and activation of the downstream signaling cascades via PI3K, RAS/MAPK/ERK, and PLC-gamma. TRK pathway aberrations, including gene fusions, protein overexpression, and single nucleotide alterations, have been implicated in the pathogenesis of many cancer types, with NTRK gene fusions being the most well validated oncogenic events to date. Although the NTRK gene fusions are infrequent in most cancer types, certain rare tumor types are predominately driven by these events. Conversely, in more common histologies, such as lung and colorectal cancers, prevalence of the NTRK fusions is well below 5%. Selective inhibition of TRK signaling may therefore be beneficial among patients whose tumors vary in histologies, but share underlying oncogenic NTRK gene alterations. Currently, several TRK-targeting compounds are in clinical development. The ongoing Phase 2 trials with entrectinib and LOXO-101, two of the leading TRK inhibitors, are designed as 'basket trials', inclusive of patients whose tumors harbor NTRK gene fusions, independent of histology.
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