货号	规格	价格	上海	北京	珠海	重庆	武汉
S86314-5mg买3赠1	98.10%	￥142.00 S86314-5mg ￥142.00 现货（买3赠1）	7 7	-	-	-	-
S86314-10mg买3赠1	98.10%	￥255.00 S86314-10mg ￥255.00 现货（买3赠1）	9 9	-	-	-	-
S86314-50mg	98.10%	￥810.00 S86314-50mg ￥810.00 现货	6 6	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S86314-5mg买3赠1

98.10%

￥142.00

S86314-10mg买3赠1

98.10%

￥255.00

S86314-50mg

98.10%

￥810.00

产品描述：

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

靶点：

Cdk5/p25:5 nM (IC50);cdk2/cyclin A:8 nM (IC50);CDK2/cyclinE:8 nM (IC50);CDK7/cyclin H:10 nM (IC50);Cdk1/cyclin B:60 nM (IC50);Cdk4/cyclin D1:62 nM (IC50);CDK9/cyclinT1:138 nM (IC50);GSK-3β:79 nM (IC50);Apoptosis;CDK

体外研究：

PHA-793887 partially inhibits Rb phosphorylation at 1 μM and almost completely at 3 μM, in A2780 tumor cell line. PHA-793887 (1 μM) partially inhibits phosphorylation of the Cdk2 substrates Rb and NPM in A2780 tumor cell line. PHA-793887 (6 μM) significantly inhibits Rb and NPM phosphorylation in MCF7 cell line. PHA-793887 shows cytotoxic activities against leukemic cell lines in vitro, with IC50 ranging from 0.3 to 7 μM. In colony assays, PHA-793887 is highly cytotoxic for leukemia cell lines, with an IC50 <0.1 μM. PHA-793887 induces cell-cycle arrest, inhibits Rb and nucleophosmin phosphorylation, and modulates cyclin E and cdc6 expression at low doses of 0.2 to 1 μM and induces apoptosis at the highest dose of 5 μM. PHA-793887 is a novel inhibitor of several cdk, including cdk1, cdk2, cdk4, cdk5, cdk7, and cdk9 with IC50 in the 5 to 140 nM range

体内研究：

PHA-793887 induces tumor growth inhibition in the range of 50% at dose of 15 mg/kg to 75% at dose of 30 mg/kg in CD-1 nude mice. PHA-793887 (30 mg/kg, i.v.) also induces significant downregulation of the 58-gene panel in the skin of CD-1 mice. PHA-793887 (20 mg/kg, i.v.) induces tumor regression in the HL60 model. In the K562 model, PHA-793887 significantly reduces tumor growth. Moreover, PHA-793887 (20 mg/kg, i.v.) inhibits human primary leukemia growth in engraftment setting in vivo

参考文献：

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.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.766 ml	13.832 ml	27.664 ml
5 mM	0.553 ml	2.766 ml	5.533 ml
10 mM	0.277 ml	1.383 ml	2.766 ml
50 mM	0.055 ml	0.277 ml	0.553 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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