Chemical Structure : AKT1 (E17K) inhibitor compound 4
CAS No.:
2982896-18-2
AKT1 (E17K) inhibitor compound 4
货号: PC-23916Not For Human Use, Lab Use Only.
AKT1 (E17K) inhibitor compound 4 is a potent, mutant-selective inhibitor of AKT1 (E17K) mutant, potently reduces cell viability of LAPC4-CR cells with EC50 of 9 nM.
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纯度 & COA & 质检文件 纯度:
>98% (HPLC)
生物&药学活性
AKT1 (E17K) inhibitor compound 4 is a potent, mutant-selective inhibitor of AKT1 (E17K) mutant, potently reduces cell viability of LAPC4-CR cells with EC50 of 9 nM.
Compound 4 binds to AKT1 (E17K) more potently than Compound 3 and shows greater selectivity over WT AKT1 (2.5-fold) and AKT2 (24-fold).
Compound 4 dissociates from purified WT AKT1 18-fold faster than AKT1 (E17K) and shows greater potency towards E17K-mutant LAPC4-CR and HBCx-2 cells relative to SkBr3 and MCF7 cells.
Compound 4 (30 mg /kg, twice-daily) significantly blocked LAPC4-CR tumour growth showed significant, exhibited dose-dependent tumour growth inhibition (75% at 20 mg/kg; 96% at 30 mg/kg) in homozygous E17K-mutant breast cancer model (HBCx-2 patient-derived xenograft), while WT AKT1 breast cancer xenograft model (BT-474) was less sensitive.
物理化学性质&存储条件
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分子量
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572.60
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分子式
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C33H25FN6O3
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外观性状
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Solid
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CAS No.
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储存条件
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- 固体粉末
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-20°C 12 个月; 4°C 6 个月
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- 配置液
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-80°C 6 个月; -20°C 6 个月
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(4-(2-(2-aminopyridin-3-yl)-5-phenyl-3H-imidazo[4,5-b]pyridin-3-yl)benzyl)-2-(2-fluoro-4-formyl-3-hydroxyphenyl)acetamide
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参考文献
1. Craven GB, et al. Nature. 2025 Jan;637(8044):205-214.
