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PHA-793887 - 10mM in DMSO, high purity , CAS No.718630-59-2(DMSO), Cyclin-dependent kinase inhibitor

COA

Grade & Purity:

10mM in DMSO

Cas Number: 718630-59-2(DMSO)
Molecular Weight: 361.48

In stock

Item Number

P407796

Grouped product items
SKU	Size	Availability	Price	Qty
P407796-1ml	1ml	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$343.90

CDK9 Selective Inhibitors

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Compound libraries (12325)

Basic Description

Synonyms	N-(6,6-dimethyl-5-(1-methylpiperidine-4-carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-3-methylbutanamide
Specifications & Purity	10mM in DMSO
Biochemical and Physiological Mechanisms	PHA-793887 is a novel and potent inhibitor of CDK2, CDK5 and CDK7 with IC50 of 8 nM, 5 nM and 10 nM. It is greater than 6-fold more selective for CDK2, 5, and 7 than CDK1, 4, and 9. PHA-793887 induces cell-cycle arrest and apoptosis. Phase 1.
Storage Temp	Store at -80°C
Shipped In	Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available.
Action Type	INHIBITOR
Mechanism of action	Cyclin-dependent kinase inhibitor
Product Description	Information PHA-793887 is a novel and potent inhibitor ofCDK2,CDK5andCDK7withIC50of 8 nM, 5 nM and 10 nM. It is greater than 6-fold more selective for CDK2, 5, and 7 than CDK1, 4, and 9. PHA-793887 induces cell-cycle arrest andapoptosis. Phase 1. In vitro PHA-793887 has low activity against CDK1, CDK4, CDK9 and GSK3β with IC50 of 60 nM, 62 nM, 138 nM and 79 nM, respectively. PHA-793887 inhibits cell proliferation of many tumor cell lines, including A2780, HCT-116, COLO-205, C-433, DU-145, A375, PC3, MCF-7, and BX-PC3, with IC50 of 88 nM–3.4 μM. PHA-793887 (1 μM) shows a decrease in the S phase, a subsequent increase of the G1 phase and a slight accumulation of G2/M phase in A2780 cells. PHA-793887 (3 μM) significantly increases G2/M phase and reduces DNA synthsis. PHA-793887 is cytotoxic for leukemic cell lines, including K562, KU812, KCL22, and TOM1, with IC50 of 0.3–7 μM, but it is not cytotoxic for normal unstimulated peripheral blood mononuclear cells or CD34+ hematopoietic stem cells. In colony assays, PHA-793887 shows very high activity against leukemia cell lines with IC50 less than 0.1 μM. PHA-793887 induces cell-cycle arrest, inhibits Rb and nucleophosmin phosphorylation, and modulates cyclin E and cdc6 expression at 0.2−1 μM and induces apoptosis at 5 μM. In vivo PHA-793887 (10–30 mg/kg) shows good efficacy in the human ovarian A2780, colon HCT-116, and pancreatic BX-PC3 carcinoma xenograft models. PHA-793887 (20 mg/kg) is effective in xenograft models of K562 and HL60 cells, primary leukemic disseminated model, and a high-burden disseminated ALL-2 model derived from a relapsed Philadelphia-positive acute lymphoid leukemia patient. Cell Data cell lines： Concentrations：0.1 nM-1 μM, dissolved in DMSO Incubation Time：72 hours Powder Purity:≥95%

Associated Targets(Human)

CDK7 Tchem Cyclin-dependent kinase 7 (1 Activities)

Discover Target: CDK7

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ERCC2 Tchem General transcription and DNA repair factor IIH helicase subunit XPD (1 Activities)

Discover Target: ERCC2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FARSB Tchem Phenylalanine--tRNA ligase beta subunit (1 Activities)

Discover Target: FARSB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK3 Tchem Cyclin-dependent kinase 3 (1 Activities)

Discover Target: CDK3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CLK2 Tchem Dual specificity protein kinase CLK2 (1 Activities)

Discover Target: CLK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta (1 Activities)

Discover Target: GSK3B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GSK3A Tclin Glycogen synthase kinase-3 alpha (1 Activities)

Discover Target: GSK3A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

Smiles	CC(C)CC(=O)NC1=N[NH]C2=C1CN(C(=O)C3CCN(C)CC3)C2(C)C
Molecular Weight	361.48

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

Chemical and Physical Properties

Solubility	Solubility (25°C) In vitro DMSO: 63 mg/mL (199.76 mM); Ethanol: 6 mg/mL (19.02 mM); Water: Insoluble;

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