PD 0332991 Isethionate

Catalog No. A13811

PD 0332991 Isethionate是CDK4/6的高选择性抑制剂，IC50分别为11 nM/16 nM。

Product Citations

K Keegan ,etc. Preclinical evaluation of AMG 925, a FLT3/CDK4 dual kinase inhibitor for treating acute myeloid leukemia. Molecular cancer therapeutics, 2014, 13(4), 880-889.

Technical details

Catalog Num	A13811
M. Wt	483.99
Formula	C24H30ClN7O2
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	827022-33-3
Synonyms	PD0332991, PD-0332991
SMILES	CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.C(CS(=O)(=O)O)O

Biological Activity

PD 0332991 Isethionate是CDK4/6的高选择性抑制剂，IC50分别为11 nM/16 nM。

Targets

Target	Value
CDK4/CyclinD3	IC50: 9nM
CDK4/CyclinD1	IC50: 11nM
CDK6/CyclinD2	IC50: 15nM
CDK2/CyclinE2	IC50: >10μM
CDK2/CyclinA	IC50: >10μM
CDK1/CyclinB	IC50: >10μM
CDK5/p25	IC50: >10μM
EGFR	IC50: >10μM
FGFR	IC50: >10μM
PDGFR	IC50: >10μM
Insulin Receptor	IC50: >10μM
VEGFR	IC50: >10μM
AMPK	IC50: >10μM
Chk1	IC50: >10μM
c-Src	IC50: >10μM
GSK-3β	IC50: >10μM
MAPK2/ERK2	IC50: >10μM
MAPKK	IC50: >10μM
p70S6K	IC50: >10μM
PKB	IC50: >10μM
PKC	IC50: >10μM

Solubility *

In vitro (25°C)	DMSO	Insoluble
	Water	Warmed: 9 mg/mL (15.69 mM)
	Ethanol	Insoluble
In vivo	saline (with warming)	9 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	20.66 mL	103.31 mL	206.62 mL
0.5 mM	4.13 mL	20.66 mL	41.32 mL
1 mM	2.07 mL	10.33 mL	20.66 mL
5 mM	0.41 mL	2.07 mL	4.13 mL

*The above data is based on the productmolecular weight 483.99. 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.