产品
编 号：F097577
分子式：C30H35ClN4O2
分子量：519.08
分子式：C30H35ClN4O2
分子量：519.08
产品类型
规格
价格
是否有货
2mg
233
In-stock
5mg
368
In-stock
10mg
517
In-stock
25mg
928
In-stock
50mg
1200
In-stock
100mg
1536
In-stock
200mg
1996
In-stock
结构图
CAS No: 1256589-74-8
产品详情
生物活性：
Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively. Alectinib demonstrates effective central nervous system (CNS) penetration.
体内研究：
Alectinib Hydrochloride (0.2 -20 mg/kg；口服给药；每日一次；持续 11 天；SCID 或携带 NCI-H2228 细胞的裸鼠) 处理可导致剂量依赖性肿瘤生长抑制 (EC50 0.46 mg/kg) 和肿瘤消退。在任何剂量水平下，均未观察到体重差异或总体毒性迹象。Animal Model:SCID or nude mice bearing NCI-H2228 cells
Dosage:0.2 mg/kg, 0.6 mg/kg, 2 mg/kg, 6 mg/kg, 20 mg/kg
Administration:Oral administration; once daily; for 11 days
Result:Resulted in dose-dependent tumor growth inhibition (EC50 of 0.46 mg/kg) and tumor regression.
体外研究：
Alectinib (0-1000 nM；2 小时；NCI-H2228 细胞) 处理可以防止表达 EML4-ALK 的 NCI-H2228 细胞中 ALK 的自磷酸化，并且还可以显著抑制 STAT3 和 AKT 的磷酸化。Alectinib (0-1000 nM；5 天；HCC827、A549 或 NCIH522 细胞) 处理以剂量依赖性方式降低细胞活性。
Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively. Alectinib demonstrates effective central nervous system (CNS) penetration.
体内研究：
Alectinib Hydrochloride (0.2 -20 mg/kg；口服给药；每日一次；持续 11 天；SCID 或携带 NCI-H2228 细胞的裸鼠) 处理可导致剂量依赖性肿瘤生长抑制 (EC50 0.46 mg/kg) 和肿瘤消退。在任何剂量水平下，均未观察到体重差异或总体毒性迹象。Animal Model:SCID or nude mice bearing NCI-H2228 cells
Dosage:0.2 mg/kg, 0.6 mg/kg, 2 mg/kg, 6 mg/kg, 20 mg/kg
Administration:Oral administration; once daily; for 11 days
Result:Resulted in dose-dependent tumor growth inhibition (EC50 of 0.46 mg/kg) and tumor regression.
体外研究：
Alectinib (0-1000 nM；2 小时；NCI-H2228 细胞) 处理可以防止表达 EML4-ALK 的 NCI-H2228 细胞中 ALK 的自磷酸化，并且还可以显著抑制 STAT3 和 AKT 的磷酸化。Alectinib (0-1000 nM；5 天；HCC827、A549 或 NCIH522 细胞) 处理以剂量依赖性方式降低细胞活性。
产品资料
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