PHA-793887

PHA-793887 is a potent, ATP-competitive CDK inhibitor, can inhibit Cdk2, Cdk1, Cdk4, and Cdk9 with IC50s of 8 nM, 60 nM, 62 nM and 138 nM, respectively, and also inhibits glycogen synthase kinase 3β with an IC50 of 79 nM.


Cat. No.: EX-A2134	Purity: >98%

For research only, Do not use for Human!

Size	Unit Price (US$)	Stock
100mg	450	In-stock
200mg	750	In-stock
500mg	1050	In-stock
1g	1500	In-stock
5g	4500	In-stock
10g	6750	Inqurie

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CAS No.	718630-59-2
Purity	>98%
Formula	C19H31N5O2
Mol Weight	361.4817
Appearance	solid powder
Solubility	Soluble in DMSO?>=50 mg/mL
Shelf Life	>2 years if stored properly
Storage	Powder -20℃ 2 years; In solvent -20℃ 1 month;
Shipping	Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Reference:	[1]. Locatelli G, et al. Transcriptional analysis of an E2F gene signature as a biomarker of activity of the cyclin-dependent kinase inhibitor PHA-793887 in tumor and skin biopsies from a phase I clinical study. Mol Cancer Ther. 2010 May;9(5):1265-73. [2]. Massard C, et al. A first in man, phase I dose-escalation study of PHA-793887, an inhibitor of multiple cyclin-dependent kinases (CDK2, 1 and 4) reveals unexpected hepatotoxicity in patients with solid tumors. Cell Cycle. 2011 Mar 15;10(6):963-70. Epub 2011 Mar 15. [3]. Alzani R, et al. Therapeutic efficacy of the pan-cdk inhibitor PHA-793887 in vitro and in vivo in engraftment and high-burden leukemia models. Exp Hematol. 2010 Apr;38(4):259-269.e2. [4]. Brasca MG, et al. Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing. Bioorg Med Chem. 2010 Mar 1;18(5):1844-53.
CoA	CoA of PHA-793887

Smiles:	CC(C)CC(=O)NC1=NNC2=C1CN(C(=O)C1CCN(C)CC1)C2(C)C


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