718630-59-2
Chemical Structure
PHA-793887
- CAS No.: 718630-59-2
- Formula:C19H31N5O2
- Molecular Weight:361.48
IUPAC Name: N-(6,6-dimethyl-5-(1-methylpiperidine-4-carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-3-methylbutanamide
InChIKey: HUXYBQXJVXOMKX-UHFFFAOYSA-N
SMILES: CC(C)CC(NC1=NNC2=C1CN(C(C3CCN(C)CC3)=O)C2(C)C)=O
Biological Activity: PHA-793887 is a CDK inhibitor (with IC50 values of 8 nM for Cdk2, 60 nM for Cdk1, 62 nM for Cdk4, 138 nM for Cdk9). PHA-793887 inhibits purified GSK3β (IC50 79 nM). PHA-793887 reduces the phosphorylation level of nucleophosmin/cdc6, induces G1/G2/M phase arrest, and triggers Apoptosis by activating Caspase-3. PHA-793887 exhibits anticancer activity against leukemia. PHA-793887 can be used in research related to acute leukemia, chronic myeloid leukemia, and advanced/metastatic solid tumors[1][2][3][4].
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PHA-793887 | 99.25% | PHA-793887 is a CDK inhibitor (with IC50 values of 8 nM for Cdk2, 60 nM for Cdk1, 62 nM for Cdk4, 138 nM for Cdk9). PHA-793887 inhibits purified GSK3β (IC50 79 nM). PHA-793887 reduces the phosphorylation level of nucleophosmin/cdc6, induces G1/G2/M phase arrest, and triggers Apoptosis by activating Caspase-3. PHA-793887 exhibits anticancer activity against leukemia. PHA-793887 can be used in research related to acute leukemia, chronic myeloid leukemia, and advanced/metastatic solid tumors. | ||||||||||||||||||||
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PHA-793887 (Standard) | ≥98% | PHA-793887 (Standard) is the analytical standard of PHA-793887 (HY-11001). This product is intended for research and analytical applications. 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. | ||||||||||||||||||||
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References
- [1]. 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. Experimental hematology. 2010 Apr;38(4):259-269.e2. [Content Brief]
- [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 (Georgetown, Tex.). 2011 Mar 15;10(6):963-70. [Content Brief]
- [3]. 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. Bioorganic & medicinal chemistry. 2010 Mar 01;18(5):1844-53. [Content Brief]
- [4]. 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. Molecular cancer therapeutics. 2010 May;9(5):1265-73. [Content Brief]
