GSK1838705A

Catalog No. A11175

GSK1838705A是一种小分子激酶抑制剂，其抑制IGF-IR和胰岛素受体的IC50分别为2.0和1.6 nmol/L。

Product Citations

Watanabe S, .et al. Insulin augments serotonin-induced contraction via activation of the IR/PI3K/PDK1 pathway in the rat carotid artery, Pflugers Arch, 2016, Apr;468(4):667-77 PMID: 26577585

Technical details

Catalog Num	A11175
M. Wt	532.57
Formula	C27H29FN8O3
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	1116235-97-2
Synonyms	GSK-1838705A
SMILES	CNC(=O)C1=C(C=CC=C1F)NC2=NC(=NC3=C2C=CN3)NC4=C(C=C5CCN(C5=C4)C(=O)CN(C)C)OC

Biological Activity

GSK1838705A是一种小分子激酶抑制剂，其抑制IGF-IR和胰岛素受体的IC50分别为2.0和1.6 nmol/L。

Targets

Target	Value
ALK	IC50: 0.5nM
Insulin Receptor	IC50: 1.6nM
IGF-1R	IC50: 2nM
RSK1	IC50: 1.6μM
JNK3	IC50: 2μM
B-Raf(V600E)	IC50: >2μM
JNK1	IC50: 5μM
JAK3	IC50: 5μM
JNK2	IC50: 8μM
Akt1	IC50: >10μM
Akt2	IC50: >10μM
ALK5	IC50: >10μM
AuroraA	IC50: >10μM
AuroraB	IC50: >10μM
CaMKK2	IC50: >10μM
CDK2/CyclinA	IC50: >10μM
EGFR	IC50: >10μM
ErbB2	IC50: >10μM
HGK	IC50: >10μM
IKK3	IC50: >10μM
PAK1	IC50: >10μM
PCTAIRE1	IC50: >10μM
PDK-1	IC50: >10μM
PI3Kα	IC50: >10μM
PI3Kβ	IC50: >10μM
PI3Kδ	IC50: >10μM
PI3Kγ	IC50: >10μM
PKCε	IC50: >10μM
ROCK1	IC50: >10μM
Src1	IC50: >10μM
VEGFR2	IC50: >10μM
YAK3	IC50: >10μM
p70S6K	IC50: >10μM
JAK2	IC50: 13μM
JAK1	IC50: >25μM
ASK1	IC50: >25μM
ErbB4	IC50: >25μM
GSK-3β	IC50: >25μM
IKK1	IC50: >25μM
IKK2	IC50: >25μM
ITK	IC50: >25μM
LCK	IC50: >25μM
MAPKAPK2	IC50: >25μM
p38α	IC50: >25μM
Syk	IC50: >25μM
ZAP70	IC50: >25μM

Solubility *

In vitro (25°C)	DMSO	103 mg/mL (193.4 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	15% Captisol+citrate vehicle	28 mg/mL
* <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	18.78 mL	93.88 mL	187.77 mL
0.5 mM	3.76 mL	18.78 mL	37.55 mL
1 mM	1.88 mL	9.39 mL	18.78 mL
5 mM	0.38 mL	1.88 mL	3.76 mL

*The above data is based on the productmolecular weight 532.57. 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.