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HY-11001

CAS:718630-59-2

718630-59-2  Technical Data: Price and Availability of  Cas No:718630-59-2

Cas : 718630-59-2 M.Wt: 361.4818
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 (CDK2), 5 nM(CDK5), 10 nM (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.
 
References on 718630-59-2 :
 

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