PHA-793887

ArtNr	HY-11001-50mg
Hersteller	MedChem Express
CAS-Nr.	718630-59-2
Menge	50 mg
Quantity options	100 mg 10 mM/1 mL 10 mg 25 mg 50 mg 5 mg
Kategorie	Oncology Neuroscience Neuroinflammation Neural Signaling Inhibitors & Compound Libraries Small Molecules By Organ Colorectal Cancer Heart & Blood Cancer Uterine, Ovarian & Cervical Cancer
Typ	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
Versandbedingung	Raumtemperatur
Lieferbar
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

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HY-11001-50mg-safety-datasheet.pdf