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           APIs&Intermediates Chemicals of Shanghai APIs Chemical Co., Ltd 


Product Indentification


Name:   CHIR-258
Synonyms:   4-Amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one
CAS Registry Number:   405169-16-6
Molecular Formula:   C21H21FN6O
Molecular Weight:    392.44
Molecular Structure:    



                   In stock!!


                   Appearance:  Yellow solid





                   Storage: 4 deg C



                  Inquiry (H1NMR,HPLC,LC-MS)



Related pages:

     Search CHIR-258 in google
     Search CAS 405169-16-6  in google
     Search C21H21FN6O  in google


Related information:


       CHIR-258,a Novel Multi-targeted Tyrosine Kinase Inhibitor, for the Treatment of t(4;14) Multiple Myeloma. It is a highly potent, novel multitargeted growth factor receptor kinase inhibitor with IC50 of 1, 2, 10, 8, 27, 36 nM for FLT3, c-KIT, VEGFR1/2/3, PDGFRß and CSF-1R, respectively. It shows both antitumor and antiangiogenic activities in vivo. It potently inhibits FGFR3 with an inhibitory concentration of 50% (IC50) of 5 nM in in vitro kinase assays and selectively inhibited the growth of B9 cells and human myeloma cell lines expressing wild-type (WT) or activated mutant FGFR3. Antiproliferative activity of CHIR-258 against MV4;11 was ~24-fold greater compared with RS4;11, indicating more potent inhibition against cells with constitutively activated FLT3 ITD.



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