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OSI-930

Chemical Structure : OSI-930

CAS No.: 728033-96-3

OSI-930 (OSI 930;OSI930)

Catalog No.: PC-42449Not For Human Use, Lab Use Only.

A potent, orally active, dual inhibitor of c-Kit and VEGFR-2 (KDR) with IC50 of 15 nM and 9 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

OSI-930 is a potent, orally active, dual inhibitor of c-Kit and VEGFR-2 (KDR) with IC50 of 15 nM and 9 nM, respectively.
OSI-930 also inhibits Lck, c-Raf, Flt1, and CSF-1R (IC50<100 nM).
OSI-930 exhibits antitumor activity in mutant Kit-expressing HMC-1 xenograft model.

Physicochemical Properties

M.Wt 443.4416
Formula C22H16F3N3O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-Thiophenecarboxamide, 3-[(4-quinolinylmethyl)amino]-N-[4-(trifluoromethoxy)phenyl]-

References

1. Garton AJ, et al. Cancer Res. 2006 Jan 15;66(2):1015-24.

2. Yap TA, et al. Clin Cancer Res. 2013 Feb 15;19(4):909-19.

3. Patel JP, et al. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6495-9.

4. Macpherson IR, et al. Eur J Cancer. 2013 Mar;49(4):782-9.

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