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Quizartinib

Quizartinib

品 牌 MCE
C A S 号 950769-58-1
货 号 HY-13001
规 格 5mg
价 格(元) 1548.00
咨询优惠价
货号 规格 价格
HY-13001 5mg 1548.00
HY-13001 10mg 2650.00
HY-13001 50mg 6200.00
HY-13001 100mg 10114.00

产品说明


Quizartinib (AC220)是第二代FLT3抑制剂,对Flt3(ITD和WT)的IC50分别为1.1 nM和4.2 nM,比对KIT,PDGFRα,PDGFRβ,RET和CSF-1R的抑制性强10倍。



Quizartinib的生物活性


Quizartinib (AC220) is a second-generation FLT3 inhibitor for Flt3(ITD/WT) with IC50 of 1.1 nM/4.2 nM, 10-fold more selective for Flt3 than KIT, PDGFRα, PDGFRβ, RET, and CSF-1R.
IC50 value: 1.1 nM/4.2 nM( Flt3 ITD/WT) [1]
Target: FLT3
in vitro: AC220, a unique, potent and selective inhibitor of FLT3, has high affinity for FLT3 with a Kd value of 1.6 nM. AC220 inhibits the autophosphorylation of FLT3 in the human leukemia cell lines MV4-11 which harbor a homozygous FLT3-ITD mutation and is FLT3 dependent, and RS4;11 which expresses wild-type FLT3 with IC50 values of 1.1 nM and 4.2 nM, respectively. AC220 is the most potent cellular FLT3-ITD inhibitor, leading to the most significant inhibition of MV4-11 cell proliferation with IC50 of 0.56 nM compared to all other FLT3 inhibitors whose IC50 values range from 0.87 nM to 64 nM. AC220 has no inhibitory activity against the proliferation of A375 cells which harbor an activating mutation in BRAF and are not FLT3 dependent, indicating a large window between FLT3 inhibition and general cytotoxic effects.
in vivo: Oral administration of AC220 (10 mg/kg) induces time-dependent inhibition of FLT3 autophosphorylation in the FLT3-ITD–dependent MV4-11 tumor xenograft mouse model; the inhibition being 90% at 2 hours and 40% at 24 hours. AC220 significantly extends survival in a mouse model of FLT3-ITD AML with doses as low as 1 mg/kg given orally once a day. Treatment with AC220 at 10 mg/kg for 28 days results in rapid and complete regression of tumors in all mice with no tumor regrowth during the 60-day posttreatment period. AC220 displays more significant efficacy compared to sunitinib treatment which causes tumors to shrink slowly and resume growth immediately upon discontinuation of treatment in all but one of the mice.

化学信息


分子量 560.67 储存条件 参考CoA中推荐的条件进行储存。
分子式 C₂₉H₃₂N₆O₄S
CAS号 950769-58-1
溶剂/溶解度 DMSO: ≥ 33 mg/mL

相关文献


[1]. Zarrinkar PP, et al. AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood, 2009, 114(14), 2984-2992.