LDK-378

Catalog No. A13238

LDK-378是ALK(间变性淋巴瘤激酶)的高度选择性、生物利用度和AT竞争性小分子抑制剂，ALK是一种受体酪氨酸激酶，被认为是肺癌的重要药物靶点。

Technical details

Catalog Num	A13238
M. Wt	558.14
Formula	C28H36ClN5O3S
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	1032900-25-6
Synonyms	LDK378,LDK 378
SMILES	CC1=CC(=C(C=C1C2CCNCC2)OC(C)C)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)C(C)C)Cl

Biological Activity

LDK-378是ALK(间变性淋巴瘤激酶)的高度选择性、生物利用度和AT竞争性小分子抑制剂，ALK是一种受体酪氨酸激酶，被认为是肺癌的重要药物靶点。

Targets

Target	Value
ALK	IC50: 0.2nM
Insulin Receptor	IC50: 7nM
IGF-1R	IC50: 8nM
STK22D	IC50: 23nM
FLT3	IC50: 60nM
FGFR2	IC50: 0.26μM
RET	IC50: 0.4μM
FGFR3	IC50: 0.43μM
LCK	IC50: 0.56μM
JAK2	IC50: 0.61μM
AuroraA	IC50: 0.66μM
Lyn	IC50: 0.84μM
EGFR	IC50: 0.9μM
FGFR4	IC50: 0.95μM
PDGFRα	IC50: 1.14μM
Abl	IC50: 1.25μM
ROCK2	IC50: 1.27μM
c-Kit	IC50: 1.28μM
MKNK2	IC50: 2.24μM
Syk	IC50: 3.05μM
c-Met	IC50: 3.17μM
BTK	IC50: 3.36μM
JAK1	IC50: 3.73μM
CDK2	IC50: 3.97μM
CDK4	IC50: 4.72μM
ZAP70	IC50: 9.7μM
Akt	IC50: >10μM
GSK-3α	IC50: >10μM
GSK-3β	IC50: >10μM
PAK2	IC50: >10μM

Solubility *

In vitro	DMSO	Warmed: 18 mg/mL (32.25 mM)
	Water	Insoluble
	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.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	17.92 mL	89.58 mL	179.17 mL
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.