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OSI-930

Catalog No.
A2838
Inhibitor of Kit, KDR, Flt, CSF-1R, c-Raf and Lck
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$150.00
In stock
5mg
$105.00
In stock
25mg
$320.00
In stock
100mg
$700.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

OSI-930 is a novel, potent inhibitor of Flt1, kinase insert domain receptor (KDR), CSF-1R, Lck, c-Raf and activated receptor tyrosine kinases Kit with IC50 values of 8, 9, 15, 22, 41 and 80 nM, respectively [1].

OSI-930 has been demonstrated to inhibit proliferation and induce apoptosis in the HMC-1 cell line which is highly dependent on Kit signaling for survival. On the contrary, OSI-930 revealed no growth inhibition of COLO-205 cell line under normal culture conditions [1].

OSI-930 has shown to time- and concentration-dependently inactivate P450 3A4. Additionally, OSI-930 could reduce CO difference spectra of P450 3A4 [2].

References:
[1] Garton AJ1, Crew AP, Franklin M, Cooke AR, Wynne GM, Castaldo L, Kahler J, Winski SL, Franks A, Brown EN, Bittner MA, Keily JF, Briner P, Hidden C, Srebernak MC, Pirrit C, O'Connor M, Chan A, Vulevic B,Henninger D, Hart K, Sennello R, Li AH, Zhang T, Richardson F, Emerson DL, Castelhano AL, Arnold LD,Gibson NW. OSI-930: a novel selective inhibitor of Kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models. Cancer Res. 2006 Jan 15;66(2):1015-24.
[2] Lin HL1, Zhang H, Medower C, Hollenberg PF, Johnson WW. Inactivation of cytochrome P450 (P450) 3A4 but not P450 3A5 by OSI-930, a thiophene-containing anticancer drug. Drug Metab Dispos. 2011 Feb;39(2):345-50.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt443.44
Cas No.728033-96-3
FormulaC22H16F3N3O2S
Solubility≥22.15 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
Chemical Name3-(quinolin-4-ylmethylamino)-N-[4-(trifluoromethoxy)phenyl]thiophene-2-carboxamide
SDFDownload SDF
Canonical SMILESC1=CC=C2C(=C1)C(=CC=N2)CNC3=C(SC=C3)C(=O)NC4=CC=C(C=C4)OC(F)(F)F
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description OSI-930 is a potent inhibitor of receptor tyrosine kinases with IC50 values of 80 nM, 9 nM, 8 nM, 15 nM, 41 nM and 22 nM for c-Kit, KDR, Flt, CSF-1R, c-Raf and Lck , respectively.
Targets c-Kit KDR Flt CSF-1R c-Raf Lck
IC50 80 nM 9 nM 8 nM 15 nM 41 nM 22 nM

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