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LDK-378

促销

ALK 抑制剂

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产品目录号: A13238

库存状态:中国现货中国现货

产品名 目录号 价格 数量
LDK-378 5mg A13238-5
¥ 400.00
LDK-378 10mg A13238-10
¥ 700.00
LDK-378 50mg A13238-50
¥ 1,000.00
LDK-378 10mM * 1mL in DMSO A13238-10mM-D
¥ 600.00

产品仅用于研究,不针对患者销售,望谅解.

产品简介

LDK378 is a highly selective, orally bioavailable and ATP-competitive small molecule inhibitor of ALK (Anaplastic Lymphoma Kinase), a receptor tyrosine kinase considered to be an important lung cancer drug target.

LDK-378

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Chemical Information

目录号 A13238
Mechanism of action Inhibitor
分子量 558.14
化学分子式 C28H36ClN5O3S
Solubility DMSO
纯度 >98%
储存方式 at -20°C 2 years
CAS No. 1032900-25-6
Synonyms LDK378,LDK 378
SMILES code CC1=CC(=C(C=C1C2CCNCC2)OC(C)C)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)C(C)C)Cl
化学名称 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine

生物活性

Description
LDK378 is a highly selective, orally bioavailable and ATP-competitive small molecule inhibitor of ALK (Anaplastic Lymphoma Kinase), a receptor tyrosine kinase considered to be an important lung cancer drug target.
Targets
Target Value
ALKIC50: 0.2nM
Insulin ReceptorIC50: 7nM
IGF-1RIC50: 8nM
STK22DIC50: 23nM
FLT3IC50: 60nM
FGFR2IC50: 0.26μM
RETIC50: 0.4μM
FGFR3IC50: 0.43μM
LCKIC50: 0.56μM
JAK2IC50: 0.61μM
AuroraAIC50: 0.66μM
LynIC50: 0.84μM
EGFRIC50: 0.9μM
FGFR4IC50: 0.95μM
PDGFRαIC50: 1.14μM
AblIC50: 1.25μM
ROCK2IC50: 1.27μM
c-KitIC50: 1.28μM
MKNK2IC50: 2.24μM
SykIC50: 3.05μM
c-MetIC50: 3.17μM
BTKIC50: 3.36μM
JAK1IC50: 3.73μM
CDK2IC50: 3.97μM
CDK4IC50: 4.72μM
ZAP70IC50: 9.7μM
AktIC50: >10μM
GSK-3αIC50: >10μM
GSK-3βIC50: >10μM
PAK2IC50: >10μM

溶解性

Solubility (25°C)* In vitro DMSO 20 mg/mL heating (35.83 mM)
Water <1 mg/mL (<1 mM)
Ethanol 3 mg/mL (5.37 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

制备储备液

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 17.92 mL 89.58 mL 179.17mL
0.5 mM 3.58 mL 17.92 mL 35.83 mL
1 mM 1.79 mL 8.96 mL 17.92 mL
5 mM 0.36 mL 1.79 mL 3.58 mL

*The above data is based on the productmolecular weight 558.14. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

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