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Alectinib Hydrochloride
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Alectinib Hydrochloride图片
CAS NO:1256589-74-8
包装与价格：
包装价格(元)
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议
1 g电议

产品名称
艾乐替尼盐酸盐
CH5424802 Hydrochloride
RO5424802 Hydrochloride
AF-802 Hydrochloride
产品介绍
Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) 是一种有效，选择性和口服的ALK抑制剂，其IC50为 1.9 nM，Kd值为 2.4 nM (以 ATP 竞争方式)，并且还抑制ALK F1174L和ALK R1275Q，其IC50分别为 1 nM 和 3.5 nM。Alectinib Hydrochloride 还具有有效的中枢神经系统 (CNS) 渗透能力。
生物活性

Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally availableALKinhibitor with anIC50of 1.9 nM and aKdvalue of 2.4 nM (in an ATP-competitive manner), and also inhibitsALK F1174LandALK R1275QwithIC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].

IC50& Target

IC50: 1.9 nM (ALK), 1 nM (ALKF1174L), 3.5 nM (ALKR1275Q)[1]
Kd: 2.4 nM (ALK)[1]

体外研究
(In Vitro)

Alectinib (0-1000 nM; 2 hours; NCI-H2228 cells) treatment could prevent autophosphorylation of ALK in NCI-H2228 cells expressing EML4-ALK, and it also resulted in substantial suppression of phosphorylation of STAT3 and AKT[1].
Alectinib (0-1000 nM; 5 days; HCC827, A549, or NCIH522 cells) treatment reduces cell activity in a dose-dependent manner[1].

Western Blot Analysis[1]

Cell Line:NCI-H2228 cells
Concentration:0 nM,10 nM,100 nM, 1000 nM
Incubation Time:2 hours
Result:Inhibition of ALK phosphorylation and signal transduction.

Cell Viability Assay[1]

Cell Line:HCC827, A549, or NCIH522 cells
Concentration:0-1000 nM
Incubation Time:5 days
Result:Reduced cell activity in a dose-dependent manner.
体内研究
(In Vivo)

Alectinib (0.2-20 mg/kg; oral administration; once daily; for 11 days; SCID or nude mice bearing NCI-H2228 cells) treatment can result in dose-dependent tumor growth inhibition (EC50of 0.46 mg/kg) and tumor regression. At any dose level, no differences in body weight or gross signs of toxicity are observed[1].

Animal Model:SCID or nude mice bearing NCI-H2228 cells[1]
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 (EC50of 0.46 mg/kg) and tumor regression.
Clinical Trial
分子量

519.08

性状

Solid

Formula

C30H35ClN4O2

CAS 号

1256589-74-8

中文名称

艾乐替尼盐酸盐；盐酸阿雷替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 5 mg/mL(9.63 mM;Need ultrasonic)

H2O :< 0.1 mg/mL(insoluble)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.9265 mL9.6324 mL19.2649 mL
5 mM0.3853 mL1.9265 mL3.8530 mL
10 mM---------
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。