Alectinib 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.

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库存: 现货

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数量
2mg

￥287.00

230.00

- +
5mg

￥425.00

340.00

- +
50mg

￥1025.00

820.00

- +
100mg

￥1612.00

1290.00

- +
200mg

￥2637.00

2110.00

- +

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货号: ajce54802
CAS: 1256589-74-8
别名: 艾乐替尼盐酸盐; CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride
分子式: C30H35ClN4O2
分子量: 519.08
纯度: >98%
溶解度: DMSO: 6 mg/mL (11.56 mM and warming)
储存: Store at -20°C
库存: 现货

Background

Alectinib (AF802, CH5424802, RO5424802, RG-7853) is a second generation oral drug that selectively inhibits the activity of anaplastic lymphoma kinase (ALK) tyrosine kinase.

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[1].

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[1]. It has antitumor activity against cancers with ALK gene alterations[2].

[1] Song Z, et al. Acta Pharm Sin B. 2015, 5(1):34-7. [2] Kodama T, et al. Cancer Lett. 2014, 351(2):215-21. [3] Ke Yang, et al. Exp Mol Med. 2017, 49(3): e303.