Sitravatinib

SKU: orb1226961

Description

A novel, broad spectrum small molecule inhibitor that blocks a wide array of RTKs known to be amplified/overexpressed in sarcomas, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl (IC50=1.5-30 nM); significantly blocks the phosphorylation of potential driver RTKs and induces potent anti-proliferative effects in vitro; suppresses tumor growth in tumor xenografts in vivo.Lung Cancer Phase 2 Clinical(In Vitro):Sitravatinib (0.01 nM-10 μM; 14 days) reduces colony formation in a dose-dependent manner in KLN205 and E0771 cell lines.Sitravatinib (0.001-10 μM; 5 days) inhibits tumor cell viability with IC50s of approximately 1 μM in KLN205, E0771 and CT1B-A5 cell lines.(In Vivo):Sitravatinib (20 mg/kg; p.o.; once per day for 6 days) significantly inhibits tumor progression and induces tumor regression in C57BL/6 mice bearing CT1B-A5 cells model.

Key Properties

• CAS Number: 1123837-84-2
• MW: 629.6763
• Purity: >98% (HPLC)
• Formula: C₃₃H₂₉F₂N₅O₄S
• SMILES: O=C(C1(C(NC2=CC=C(F)C=C2)=O)CC1)NC3=CC=C(OC4=C5C(C=C(C6=NC=C(CNCCOC)C=C6)S5)=NC=C4)C(F)=C3
• Target: c-Kit
• Solubility: DMSO: ≥ 32 mg/mL

Bioactivity

• In Vivo:
  Animal model: 6-week-old C57BL/6 mice (bearing CT1B-A5 cells). Dosage: 20 mg/kg. Administration: Oral administration; once per day for 6 days. Result: Significantly inhibited tumor progression and induced tumor regression.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MGCD-516 | MG-516

Quick Database Links

Gene Symbol

c-Kit