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Chemical Structure : G-749
CAS No.: 1457983-28-6
Catalog No.: PC-42981Not For Human Use, Lab Use Only.
Denfivontinib (G-749) is a potent, broad-spetrum FLT-3 inhibitor with IC50 of 0.4 and 0.6 nM against wt FLT-3 and FLT3-D835Y mutant, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $68 | In stock | |
| 10 mg | $98 | In stock | |
| 25 mg | $158 | In stock | |
| 50 mg | $258 | In stock | |
| 100 mg | Get quote |
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Denfivontinib (G-749) is a potent, broad-spetrum FLT-3 inhibitor with IC50 of 0.4 and 0.6 nM against wt FLT-3 and FLT3-D835Y mutant, respectively.
G-749 also shows potent and sustained inhibition of the FLT3 mutants including FLT3-ITD, FLT3-ITD/N676D, and FLT3-ITD/F691L in cellular assays.
G-749 also inhibits RTKs Ret, FLT1, Axl, Fms, FGFR-1/3 (IC50=9-30 nM), and Aurora A and B (IC50=6-24 nM) inhibits autophosphorylation of FLT3 with IC50 of <8 nM in FLT3-WT bearing RS4-11 and in FLT3-ITD harboring MV4-11 and Molm-14 cells.
G-749 shows potent antileukemic activity in patient blasts harboring FLT3-ITD, FLT3-TKD, and FLT3-ITD/TKD mutations through inhibition of pFLT3 and pERK1/2 both in vitro and in vivo, overcomes drug resistance of AC220 and/or PKC412.
| M.Wt | 521.409 | |
| Formula | C25H25BrN6O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: 25 mg/mL |
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| Chemical Name/SMILES |
Pyrido[4,3-d]pyrimidin-5(6H)-one, 8-bromo-2-[(1-methyl-4-piperidinyl)amino]-4-[(4-phenoxyphenyl)amino]- |
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1. Lee HK, et al. Blood. 2014 Apr 3;123(14):2209-19.
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