PHA-793887

Catalog No. A10716

PHA-793887是一种新型有效的CDK2，CDK5和CDK7抑制剂，IC50分别为8 nM，5 nM 和10 nM，作用于CDK2，5，和7比作用于CDK1，4，和9选择性高6倍以上。可在低浓度下靶向多种细胞周期蛋白依赖性激酶，并具有针对多种癌细胞的高活性。

Product Citations

Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168

Technical details

Catalog Num	A10716
M. Wt	361.5
Formula	C19H31N5O2
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	718630-59-2
Synonyms	PHA793887
SMILES	CC(C)CC(=O)NC1=NNC2=C1CN(C2(C)C)C(=O)C3CCN(CC3)C

Biological Activity

Targets

Target	Value
CDK5/p25	IC50: 5nM
CDK2/CyclinA	IC50: 8nM
CDK2/CyclinE	IC50: 8nM
CDK7/CyclinH	IC50: 10nM
CDK1/CyclinB	IC50: 60nM
CDK4/CyclinD1	IC50: 62nM
GSK-3β	IC50: 79nM
CDK9/CyclinT1	IC50: 138nM

Solubility *

In vitro (25°C)	DMSO	61 mg/mL (168.75 mM)
	Water	Insoluble
	Ethanol	61 mg/mL (168.75 mM)
In vivo	30% propylene glycol, 5% Tween 80, 65% D5W	14 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	27.66 mL	138.31 mL	276.63 mL
0.5 mM	5.53 mL	27.66 mL	55.33 mL
1 mM	2.77 mL	13.83 mL	27.66 mL
5 mM	0.55 mL	2.77 mL	5.53 mL

*The above data is based on the productmolecular weight 361.5. 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.