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Sitravatinib

Cat. No. M9626
Sitravatinib Structure
Synonym:

MGCD516; MG516

Size Price Availability Quantity
10mg USD 119  USD119 In stock
25mg USD 218  USD218 In stock
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Quality Control
Biological Activity

Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib treatment resulted in significant blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects in vitro. Sitravatinib reduces colony formation in a dose-dependent manner in KLN205 and E0771 cell lines.

In vivo, Sitravatinib (20 mg/kg/day; p.o.; 6 days) significantly inhibits tumor progression and induces tumor regression in C57BL/6 mice bearing CT1B-A5 cells model.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 629.68
Formula C33H29F2N5O4S
CAS Number 1123837-84-2
Purity 100.0%
Solubility DMSO ≥ 26 mg/mL
Storage at -20°C
References

[1] Wenting Du, et al. JCI Insight. Sitravatinib potentiates immune checkpoint blockade in refractory cancer models

[2] Parag P Patwardhan, et al. Oncotarget. 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

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Sitravatinib, MGCD516; MG516 supplier, VEGFR/PDGFR, inhibitors

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