OSI-930 - CAS 728033-96-3
Catalog number:
Not Intended for Therapeutic Use. For research use only.
OSI-930 is a selective thiophene-derived tyrosine kinase inhibitor with potential antineoplastic activity. Tyrosine kinase inhibitor OSI-930 inhibits stem cell factor receptor (c-Kit) and the vascular endothelial growth factor receptor 2 (VEGFR2), which may result in the inhibition of both tumor cell proliferation and tumor angiogenesis. Both c-Kit and VEGFR2 are overexpressed in a variety of cancers.
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B0084-286626 10 mg $198 In stock
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Light yellow to yellow Solid
OSI 930; OSI930
Current Developer:
OSI Pharmaceuticals, Inc
1.OSI-930 analogues as novel reversal agents for ABCG2-mediated multidrug resistance.
Kuang YH1, Patel JP, Sodani K, Wu CP, Liao LQ, Patel A, Tiwari AK, Dai CL, Chen X, Fu LW, Ambudkar SV, Korlipara VL, Chen ZS. Biochem Pharmacol. 2012 Sep 15;84(6):766-74. doi: 10.1016/j.bcp.2012.06.019. Epub 2012 Jun 28.
OSI-930, a dual c-Kit and KDR tyrosine kinase inhibitor, is reported to have undergone a Phase I dose escalation study in patients with advanced solid tumors. A series of fifteen pyridyl and phenyl analogues of OSI-930 were designed and synthesized. Extensive screening of these compounds led to the discovery that nitropyridyl and ortho-nitrophenyl analogues, VKJP1 and VKJP3, were effective in reversing ABC subfamily G member 2 (ABCG2) transporter-mediated multidrug resistance (MDR). VKJP1 and VKJP3 significantly sensitized ABCG2-expressing cells to established substrates of ABCG2 including mitoxantrone, SN-38, and doxorubicin in a concentration-dependent manner, but not to the non-ABCG2 substrate cisplatin. However, they were unable to reverse ABCB1- or ABCC1-mediated MDR indicating their selectivity for ABCG2. Western blotting analysis was performed to evaluate ABCG2 expression and it was found that neither VKJP1 nor VKJP3 significantly altered ABCG2 protein expression for up to 72 h.
2.Inhibition of c-Kit, VEGFR-2 (KDR), and ABCG2 by analogues of OSI-930.
Patel JP1, Kuang YH, Chen ZS, Korlipara VL. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6495-9. doi: 10.1016/j.bmcl.2011.08.070. Epub 2011 Aug 22.
The quinoline domain of OSI-930, a dual inhibitor of receptor tyrosine kinases (RTKs) c-Kit and KDR, was modified in an effort to further understand the SAR of OSI-930, and the binding site characteristics of c-Kit and KDR. A series of 16 compounds with heteroatom substituted pyridyl and phenyl ring systems was synthesized and evaluated against a panel of kinases including c-Kit and KDR. Aminopyridyl derivative 6 was found to be the most active member of the series with 91% and 57% inhibition of c-Kit at 10μM and 1μM, respectively and 88% and 50% inhibition of KDR at 10μM and 1μM, respectively. The target compounds were also tested for their ability to inhibit efflux of mitoxantrone through inhibition of ATP dependent ABCG2 pump. Nitropyridyl derivative 5 and o-nitrophenyl derivative 7 exhibited complete inhibition of the ABCG2 pump with IC(50) values of 13.67μM and 16.67μM, respectively.
3.A phase 1 study of OSI-930 in combination with erlotinib in patients with advanced solid tumours.
Macpherson IR1, Poondru S, Simon GR, Gedrich R, Brock K, Hopkins CA, Stewart K, Stephens A, Evans TR. Eur J Cancer. 2013 Mar;49(4):782-9. doi: 10.1016/j.ejca.2012.09.036. Epub 2012 Oct 22.
AIM: To determine the maximum tolerated dose (MTD) of OSI-930 that can be combined with erlotinib, and establish recommended phase 2 doses when both agents are administered daily in patients with advanced solid tumours.
4.First-in-human phase I trial of two schedules of OSI-930, a novel multikinase inhibitor, incorporating translational proof-of-mechanism studies.
Yap TA1, Arkenau HT, Camidge DR, George S, Serkova NJ, Gwyther SJ, Spratlin JL, Lal R, Spicer J, Desouza NM, Leach MO, Chick J, Poondru S, Boinpally R, Gedrich R, Brock K, Stephens A, Eckhardt SG, Kaye SB, Demetri G, Scurr M. Clin Cancer Res. 2013 Feb 15;19(4):909-19. doi: 10.1158/1078-0432.CCR-12-2258. Epub 2013 Feb 12.
PURPOSE: OSI-930 is a novel, potent, oral small-molecule receptor tyrosine kinase inhibitor, predominantly against VEGF receptors (VEGFR), c-Kit, and platelet-derived growth factor receptors. A phase I trial was undertaken to determine safety, maximum-tolerated dose (MTD), pharmacokinetics, pharmacodynamics, and antitumor activity of OSI-930 in patients with advanced solid tumors.
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