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Chemical Structure : MZH29
Catalog No.: PC-35238Not For Human Use, Lab Use Only.
MZH29 is a novel potent, selective, orally active type II FLT3 inhibitor with IC50 of 9 nM and 7 nM against FLT3-WT and FLT3-ITD, respectively.
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MZH29 is a novel potent, selective, orally active type II FLT3 inhibitor with IC50 of 9 nM and 7 nM against FLT3-WT and FLT3-ITD, respectively.
MZH29 shows little to no inhibition for c-Kit in a panel of 50kinases。
MZH29 efficiently induces apoptosis and inhibits FLT3 phosphorylation in vitro, inhibited the phosphorylation of FLT3, Stat5, ERK, and c-MYC in MV4-11, MOLM-11, and NOMO-1 cells。
MZH29 inhibits FLT3-ITD/F691L and FLT3-D835V autophosphorylation and downstream signaling more potently than AC220, overcomes drug resistance in FLT3 mutant cells。
MZH29 caused complete tumor regression and extended survival in a mouse model of AML with less toxicity (10 mg/kg).
| M.Wt | 560.626 | |
| Formula | C31H33FN4O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Xu B, et al. Leukemia. 2017 Apr;31(4):913-921.
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