|5-氯-N2-(2-异丙基氧基-5-甲基-4-(哌啶-4-基)苯基)-N4-(2-(异丙基磺酰基)苯基)嘧啶-2,4-二胺盐酸盐|CsnPharm

CAS No.: 1380575-43-8

双盐酸盐色瑞替尼 Catalog No. CSN16207

Synonyms: LDK378 dihydrochloride;Ceritinib 2HCl;Ceritinib Dihydrochloride

LDK378 2HCl is a selective ALK inhibitor with an IC50 of 0.2 nM, and also inhibits InsR, IGF-1R, STK22D, FLT3 and FGFR2 with IC50 values of 7 nM, 8 nM, 23 nM, 60 nM and 260 nM.

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技术信息

生物活性

描述Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase of the insulin receptor superfamily. Altered expression and hyperactivation of ALK as a consequence of translocations or point mutations has been demonstrated to be an essential oncogenic lesion in a number of cancers. LDK378 2HCl, which is currently in Phase 1 and 2 clinical trials, is a potent ALK inhibitor with an IC₅₀ of 0.2 nM in a cell-free assay. It also inhibits IGF-1R, InSR, STK22D and FLT3 with IC₅₀ values of 8 nM, 7 nM, 23 nM and 60 nM, respectively. LDK378 exhibited antiproliferative activity especially on BA/F3-NPM-ALK and Karpas290 cells with IC₅₀ values of 26.0 nM and 22.8 nM, and on BA/F3-TEL-INSR and BA/F3-WT cells with IC₅₀ values of 319.5 nM and 2477 nM, respectively. In 2-week Karpas299 rat xenograft models, LDK378 induced a dose-dependent growth inhibition (tumor growth inhibition factor [T/C] = 74% at 6.25 mg/kg; T/C = 30% at 12.5 mg/kg) and tumor regression (T/C = -33% at 25 mg/kg and T/C = -66% at 50 mg/kg). In 2-week H2228 rat xenograft models, LDK378 induced a dose-dependent growth inhibition (T/C = 67% at 5 mg/kg; T/C = 2% at 10 mg/kg) and complete tumor regression at 25mg/kg (T/C = -100% at 25 mg/kg). Moreover, LDK378 was well tolerated and no body weight loss was observed at all doses tested in both models^[2].
作用机制The central pyrimidine ring of LDK378 is sandwiched between Ala₁₁₄₈ and Leu₁₂₅₆ and its chlorine substituent is directed towards the back of the pocket making hydrophobic contact with gatekeeper Leu₁₁₉₆^[2].
参考文献

[1] Marsilje TH, Pei W, et al. Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulf onyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. J Med Chem. 2013 Jul 25;56(14):5675-90.
[2] Marsilje TH, et al. J Med Chem. 2013 Jul 25;56(14):5675-90

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.5846 mL
- 7.9232 mL
- 15.8464 mL
- 5 mM
- 0.3169 mL
- 1.5846 mL
- 3.1693 mL
- 10 mM
- 0.1585 mL
- 0.7923 mL
- 1.5846 mL

技术信息

CAS号

1380575-43-8

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H38Cl3N5O3S

运输

蓝冰

分子量

631.06

别名

LDK378 dihydrochloride;Ceritinib 2HCl;Ceritinib Dihydrochloride;双盐酸盐色瑞替尼

溶解度

DMSO	105.0 mg/mL (166.4 mM)
Water	150.0 mg/mL (237.7 mM)

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