Molecular Weight(MW): 443.44
OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl. Phase 1.
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RE-luc2P-HEK293 cells were pretreated with 1uM OSI-930 (green), 20uM TBB (blue), 10uM CKI-7 (purple), or 10uM H-89 (orange) for 16 h and infected with Y. enterocolitica WA or Y. pestis Ind195 at MOI 1 and 20, respectively, for 1 h. Following stimulation with 10 ng/ml TNF-α at 5 h post-infection, luciferase activity was measured 24 h post-infection. Results were determined from two independent experiments performed in triplicate. A"*" denotes that the % NF-κβ inhibition using the inhibitors was significantly different (p<0.05) compared to the no drug control (black). The relative NF-κB inhibition by Yersinia infection was determined as a percentage of luciferase activity in bacteria-infected cells relative to luciferase activity in bacteria-free control cells.
BMC Microbiol 2013 13, 249. OSI-930 purchased from Selleck.
Table 2. shows the reversal effect of OSI-930 and Fumitremorgin C (FTC) on the cytotoxicity of mitoxantrone to HEK293/pcDNA3.1 and HEK293-ABCG2-482-R2.aIC50: concentration that inhibited cell survival by 50% (means ± SD). bFR: fold-resistance was the value of that IC50 value for mitoxantrone of HEK293/pcDNA3.1 cells was divided by IC50 value for mitoxantrone of HEK293/pcDNA3.1 and HEK293-ABCG2-482-R2 cells in the absence or presence of OSI-930 and Fumitremorgin C (FTC). Values in table are representative of at least three independent experiments performed in triplicate.
OSI-930 purchased from Selleck.
For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of OSI-930 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan
Dr. Yong-Weon Yi from Georgetown University Medical Center. OSI-930 purchased from Selleck.
Purity & Quality Control
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|Description||OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl. Phase 1.|
OSI-930 inhibits the cell proliferation in the HMC-1 cell line with IC50 of 14 nM without significant effect on growth of the COLO-205 cell line that does not express a constitutively active mutant receptor tyrosine kinase. Moreover, OSI-930 also induces apoptosis in HMC-1 cell line with EC50 of 34 nM.  A recent study shows that OSI-930 inactivates purified, recombinant cytochrome P450 (P450) 3A4 with a Ki of 24 μM in a time- and concentration-dependent mode. 
|In vivo||OSI-930, administrated at the maximally efficacious dose of 200 mg/kg by oral gavage, exhibits potent antitumor activity in a broad range of preclinical xenograft models including HMC-1, NCI-SNU-5, COLO-205 and U251 xenograft models. |
Protein kinase assays :Protein kinase assays are either done in-house by ELISA-based assay methods (Kit, KDR, PDGFRα, and PDGFRβ) or by a radiometric method. In-house ELISA assays used poly(Glu:Tyr) as the substrate bound to the surface of 96-well assay plates; phosphorylation is then detected using an antiphosphotyrosine antibody conjugated to HRP. The bound antibody is then quantitated using ABTS as the peroxidase substrate by measuring the absorbance at 405/490 nm. All assays uses purified recombinant kinase catalytic domains that are either expressed in insect cells or in bacteria. The Kit and EGFR protein used for in-house assays are prepared internally; other enzymes are obtained. Recombinant Kit protein is expressed as an NH2-terminal glutathione S-transferase fusion protein in insect cells and is initially purified as a nonphosphorylated (nonactivated) enzyme with a relatively high Km for ATP (400 μM). In some assays, an activated (tyrosine phosphorylated) form of the enzyme is prepared by incubation with 1 mM ATP for 1 hour at 30 °C. The phosphorylated protein is then passed through a desalting column to remove the majority of the ATP and stored at −80 °C in buffer containing 50% glycerol. The resultant preparation has a considerably higher specific activity and a lower Km for ATP (25 μM) than the initial nonphosphorylated preparation. The inhibition of Kit autophosphorylation by OSI-930 is assayed by incubation of the nonphosphorylated enzyme at 30 °C in the presence of 200 μM ATP and various concentrations of OSI-930. The reaction is stopped by removal of aliquots into SDS-PAGE sample buffer followed by heating to 100 °C for 5 minutes. The degree of phosphorylation of Kit is then determined by immunoblotting for both total Kit and phosphorylated Kit.
|In vitro||DMSO||89 mg/mL (200.7 mM)|
|Ethanol||3 mg/mL (6.76 mM)|
|In vivo||30% PEG400+0.5% Tween80+5% propylene glycol||5 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00603356||Completed||Advanced Solid Tumors||Astellas Pharma Inc|OSI Pharmaceuticals||November 2007||Phase 1|
|NCT00513851||Completed||Advanced Solid Tumors||Astellas Pharma Inc|OSI Pharmaceuticals||April 2006||Phase 1|
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