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PHA-793887

PHA-793887

Item no.	HY-11001-10mM
Manufacturer	MedChem Express
CASRN	718630-59-2
Amount	10 mM/1 mL
Quantity options	100 mg 10 mM/1 mL 10 mg 25 mg 50 mg 5 mg
Category	Oncology Neuroscience Neuroinflammation Neural Signaling Inhibitors & Compound Libraries Small Molecules By Organ Colorectal Cancer Heart & Blood Cancer Uterine, Ovarian & Cervical Cancer
Type	Inhibitors
Specific against	other
Purity	99.25
Citations	[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.
Smiles	CC(C)CC(NC1=NNC2=C1CN(C(C3CCN(C)CC3)=O)C2(C)C)=O
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	718630-59-2
Shipping Condition	Room temperature
Available
Manufacturer - Type	Reference compound
Manufacturer - Applications	Cancer-Kinase/protease
Manufacturer - Targets	Apoptosis; CDK
Shipping Temperature	Room Temperature
Storage Conditions	-20°C, 3 years; 4°C, 2 years (Powder)
Molecular Weight	361.48
Product Description	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.
Manufacturer - Research Area	Cancer
Solubility	DMSO: ≥ 50 mg/mL
Manufacturer - Pathway	Apoptosis; Cell Cycle/DNA Damage
Isoform	CDK1; CDK2; CDK4; CDK5; CDK7; CDK9
Clinical information	Phase 1

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

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HY-11001-10mM-safety-datasheet.pdf