产品名称

英文名称：LDK378

同义词

K418KG2GET、5-chloro-2-N-[5-methyl-4-(piperidin-4-yl)-2-(propan-2-yloxy)phenyl]-4-N-[2-(propane-2-sulfonyl)phenyl]pyrimidine-2,4-diamine、5-chloro-N(2)-{5-methyl-4-(piperidin-4-yl)-2-[(propan-2-yl)oxy]phenyl}-N(4)-[2-(propane-2-sulfonyl)phenyl]pyrimidine-2,、色瑞替尼

产品性质

CAS编号：1032900-25-6

分子式：C28H36ClN5O3S

分子量：558.14

PubChem编号：57379345

别名：色瑞替尼

英文别名：K418KG2GET|5-chloro-2-N-[5-methyl-4-(piperidin-4-yl)-2-(propan-2-yloxy)phenyl]-4-N-[2-(propane-2-sulfonyl)phenyl]pyrimidine-2,4-diamine|5-chloro-N(2)-{5-methyl-4-(piperidin-4-yl)-2-[(propan-2-yl)oxy]phenyl}-N(4)-[2-(propane-2-sulfonyl)phenyl]pyrimidine-2,

规格或纯度：≥99%

英文名称：LDK378

生化机理：高度有效的间变性淋巴瘤激酶（ALK）抑制剂（IC50 = 0.2 nM）。还显示出对胰岛素受体（IR），胰岛素样生长因子受体1（IGF1R），丝氨酸/苏氨酸蛋白激酶STK22D和FLT3的有效抑制作用（IC50值分别为7、8、23和60 nM）。在Karpas299和H2228大鼠异种移植模型中抑制肿瘤生长。

储存温度：-20°C储存

运输条件：超低温冰袋运输

备注：5mg卖完停产，不再备货

产品介绍：LDK378是一种有效的ALK抑制剂，IC50为0.2 nM，作用于IGF-1R和InsR，选择性分别为40和35倍。LDK378 is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively.application5-Chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine, is a Anaplastic lymphoma kinase (ALK) inhibitor.

ALogP：6.4

IUPAC Name：5-chloro-2-N-(5-methyl-4-piperidin-4-yl-2-propan-2-yloxyphenyl)-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine

INCHI：InChI=1S/C28H36ClN5O3S/c1-17(2)37-25-15-21(20-10-12-30-13-11-20)19(5)14-24(25)33-28-31-16-22(29)27(34-28)32-23-8-6-7-9-26(23)38(35,36)18(3)4/h6-9,14-18,20,30H,10-13H2,1-5H3,(H2,31,32,33,34)

InChi Key：VERWOWGGCGHDQE-UHFFFAOYSA-N

Canonical SMILES：CC1=CC(=C(C=C1C2CCNCC2)OC(C)C)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)C(C)C)Cl

Isomeric SMILES：CC1=CC(=C(C=C1C2CCNCC2)OC(C)C)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)C(C)C)Cl

PubChem CID：57379345

ChEMBL Ligand：CHEMBL2403108

Wikipedia：Ceritinib

CAS Registry No.：1032900-25-6

RCSB PDB Ligand：4MK

PEP：ceritinib

DrugCentral Ligand：4866

溶解性：溶于DMSO, 最高浓度 (mg/mL) 2.79, 最高浓度(mM) 5 温和加热；溶于ethanol, 最高浓度 (mg/mL) 2.79, 最高浓度(mM) 5 温和加热

象形图：

信号词：Danger

危险声明：H302 Harmful if swallowedH400 Very toxic to aquatic lifeH410 Very toxic to aquatic life with long lasting effectsH372 Causes damage to organs through prolonged or repeated exposureH360 May damage fertility or the unborn child

预防措施声明：P273,P280,P405,P501,P264,P260,P270,P391,P330,P203,P301+P317,P318,P319

产品包装