Alectinib (CH5424802) hydrochloride

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CAS number：1256589-74-8 molecular formula：C30H35ClN4O2

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compound introduction

Alectinib (AF802, CH5424802, RO5424802, RG-7853)是一种选择性抑制ALK酪氨酸激酶的口服药物，IC50为1.9 nM。应用： 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。 Information Alectinib (CH5424802) hydrochloride Alectinib (AF802, CH5424802, RO5424802, RG-7853) is a second generation oral drug that selectively inhibits the activity of anaplastic lymphoma kinase (ALK) tyrosine kinase. Targets ALK (Cell-free) 1.9 nM In vitro Alectinib inhibits ALK with an IC50 value of 1.9 nmol/L and shows higher selectivity for ALK than for a number of other serine/tyrosine kinases. It also inhibits the ALK gatekeeper mutation L1196M with an IC50 of 1.56 nmol/L. Alectinib is effective with crizotinib-resistant ALK mutations L1196M, F1174L, R1275Q and C1156Y. In the KARPAS-299 (lymphoma), NB-1 (neuroblastoma) and NCI-H2228 (lung cancer) ALK-positive cell lines, alectinib inhibits cell proliferation with IC50 values of 3, 4.5 and 53 nmol/L, respectively. In vivo Alectinib dose-dependently inhibits EML4-ALK positive NCI-H2228 xenograft model at doses ranging from 2 to 20 mg/kg p.o., q.d. Significant efficacy is also achieved in the EML4-ALK L1196M-driven tumors. It has antitumor activity against cancers with ALK gene alterations. Cell Research(from reference) Cell lines：KB cells Concentrations：0.01-100 μM Incubation Time：72 h

Specs

Chinese alias	-
English alias	9-Ethyl-6,6-dimethyl-8-(4-morpholin-4-ylpiperidin-1-yl)-11-oxo-5H-benzo[B]carbazole-3-carbonitrile,hydrochloride \| ALECTINIB HYDROCHLORIDE [WHO-DD] \| 5H-BENZO(B)CARBAZOLE-3-CARBONITRILE, 9-ETHYL-6,11-DIHYDRO-6,6-DIMETHYL-8-(4-(4-MORPHOLINYL)-1-PIPERIDINYL
CAS number	1256589-74-8	molecular formula	C30H35ClN4O2
molecular weight	519.09 g/mol	Exact mass	2mM in DMSO
PSA	72.400 Å²	logp	-

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GHS08

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Hazard Statement：

H341: 怀疑引起遗传缺陷 H373: 通过长时间或反复暴露对器官造成损害 H361: 怀疑破坏生育力或未出生的孩子

Statement of Preventive Measures：

P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P281: 根据需要使用个人防护设备。 P203: 使用前，获取、阅读并遵守所有安全说明。 P318: 如果暴露或担心，请就医。 P319: 如果你感到不适，请寻求医疗帮助。