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HY-11001

CAS:718630-59-2

 (Synonyms  PHA 793887;PHA793887)
718630-59-2  Technical Data: Price and Availability of  Cas No:718630-59-2

Cas : 718630-59-2 M.Wt: 361.48
Cas : 718630-59-2 Formula: C19H31N5O2
Cas : 718630-59-2 Purity: >98 %
Cas : 718630-59-2 Storage: at 20℃ 2 years
Cas : 718630-59-2 Solubility: 10 mM in DMSO
Cas : 718630-59-2 Name: PHA-793887
USD
5mg/$100 In-stock
10mg/$150 In-stock
50mg/$550 In-stock
100mg/$850 In-stock
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718630-59-2  Data Sheet:
 
Introduction of 718630-59-2 :
PHA-793887 is a novel pan-cdk inhibitor, including cdk1, cdk2, cdk4, cdk5, cdk7, and cdk9 with IC50 in the 5 to 140 nM range. IC50 Value: 8 nM(for CDK2); 5 nM(for CDK5); 10 nM(for CDK7) Target: CDKs in vitro: 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. 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. in vivo: 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. PHA-793887 (10–30 mg/kg) shows good efficacy in the human ovarian A2780, colon HCT-116, and pancreatic BX-PC3 carcinoma xenograft models. in vivo:
 
References on 718630-59-2 :
 

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