| Identification | Back Directory | [Name]
OSI-930 | [CAS]
728033-96-3 | [Synonyms]
OSI-930
CS-1804
OSI-930; OSI930
OSI-930 USP/EP/BP
3-(Quinolin-4-ylmethylamino)-N-(4-(trifluoromethoxy)phenyl)thiophene-2-carboxamide
3-[(4-Quinolinylmethyl)amino]-N-[4-(trifluoromethoxy)phenyl]-2-thiophenecarboxamide
2-Thiophenecarboxamide, 3-[(4-quinolinylmethyl)amino]-N-[4-(trifluoromethoxy)phenyl]-
3-[(4-Quinolinylmethyl)amino]-N-[4-(trifluoromethoxy)phenyl]-2-thiophenecarboxamide OSI930 | [Molecular Formula]
C22H16F3N3O2S | [MDL Number]
MFCD11100358 | [MOL File]
728033-96-3.mol | [Molecular Weight]
443.44 |
| Chemical Properties | Back Directory | [Boiling point ]
517.4±50.0 °C(Predicted) | [density ]
1.450 | [storage temp. ]
Store at -20°C | [solubility ]
≥22.15 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH | [form ]
solid | [pka]
11.36±0.70(Predicted) | [color ]
Light yellow to yellow | [InChI]
InChI=1S/C22H16F3N3O2S/c23-22(24,25)30-16-7-5-15(6-8-16)28-21(29)20-19(10-12-31-20)27-13-14-9-11-26-18-4-2-1-3-17(14)18/h1-12,27H,13H2,(H,28,29) | [InChIKey]
FGTCROZDHDSNIO-UHFFFAOYSA-N | [SMILES]
C1(C(NC2=CC=C(OC(F)(F)F)C=C2)=O)SC=CC=1NCC1C2C(N=CC=1)=CC=CC=2 |
| Hazard Information | Back Directory | [Uses]
OSI-930 is an inhibitor of the receptor tyrosine kinases c-Kit (IC50:9.5nM) and VEGFR-2 (IC50:10.1nM). | [Definition]
ChEBI: 3-(4-quinolinylmethylamino)-N-[4-(trifluoromethoxy)phenyl]-2-thiophenecarboxamide is an aromatic amide. | [Biological Activity]
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]. | [in vivo]
OSI-930 (oral gavage; once a day; 38 days; 200 mg/kg) exhibits potent antitumor activity in a broad range of preclinical xenograft models[1]. | Animal Model: | Female nu/nu CD-1 mice bearing HMC-1, NCI-SNU-5, COLO-205 and U251 xenograft models[1] | | Dosage: | 200 mg/kg | | Administration: | Oral gavage; once a day; 38 days | | Result: | Showed a significant level of inhibition of Kit, KDR and CSF-1R. |
| [target]
c-Kit | [IC 50]
KDR: 9 nM (IC50); Flt-1: 8 nM (IC50); Kit: 80 nM (IC50); PDGFRβ: 6900 nM (IC50); PDGFRα: 3408 nM (IC50); CSF-1R: 15 nM (IC50); c-Raf: 41 nM (IC50); Flt-3: 1303 nM (IC50); Lck: 22 nM (IC50); Abl: 4738 nM (IC50) | [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. |
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| Company Name: |
NCE Biomedical Co.,Ltd.
|
| Telephone: |
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15748/0_EN.htm |
| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
|