貨號	規格	價格	上海	北京	武漢	南京
S80959-1mg	99.1%	￥500.00 S80959-1mg ￥500.00 現貨	9 9	-	-	-
S80959-5mg	99.1%	￥1580.00 S80959-5mg ￥1580.00 現貨	9 9	-	-	-
S80959-10mg	99.1%	￥2300.00 S80959-10mg ￥2300.00 現貨	9 9	-	-	-
S80959-50mg	99.1%	￥6400.00 S80959-50mg ￥6400.00 現貨	6 6	-	-	-

產品介紹

Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.

產品描述：

靶點：

cyclin A/CDK2:45 nM (IC50);cyclin E/CDK2:363 nM (IC50);cyclin H/CDK7:150 nM (IC50);cyclin D1/CDK4:160 nM (IC50);cyclin B/CDK1:398 nM (IC50);TRKA:53 nM (IC50);Trkreceptor;CDK;Autophagy

體內研究：

Milciclib (PHA-848125; 5, 10, and 15 mg/kg, p.o.) inhibits the growth of tumor in 7,12-dimethylbenz(a) anthracene (DMBA)-induced rat mammary carcinoma model. Milciclib has significant antitumor activity in various human xenografts and carcinogen-induced tumors as well as in disseminated primary leukemia models, with plasma concentrations in rodents in the same range as those found active in inhibiting cancer cell proliferation. Milciclib (PHA-848125; 40 mg/kg) induces a significant tumor growth inhibition in K-RasG12DLA2 mice, and this is accompanied by a reduction in the cell membrane turnover

參考文獻：

1. Caporali S, Alvino E, Levati L, Esposito AI, Ciomei M, Brasca MG, Del Bufalo D, Desideri M, Bonmassar E, Pfeffer U, D'Atri S. Down-regulation of the PTTG1 proto-oncogene contributes to the melanoma suppressive effects of the cyclin-dependent kinase inhib 2. Albanese C, Alzani R, Amboldi N, Avanzi N, Ballinari D, Brasca MG, Festuccia C, Fiorentini F, Locatelli G, Pastori W, Patton V, Roletto F, Colotta F, Galvani A, Isacchi A, Moll J, Pesenti E, Mercurio C, Ciomei M. Dual targeting of CDK and tropomyosin rec 3. Degrassi A, et al. Efficacy of PHA-848125, a cyclin-dependent kinase inhibitor, on the K-Ras(G12D)LA2 lung adenocarcinoma transgenic mouse model: evaluation by multimodality imaging. Mol Cancer Ther. 2010 Mar;9(3):673-81. 4. Brasca, M.G., et al. Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor. J. Med. Chem. 52(16)

溶解性：

DMSO : 20 mg/mL (43.42 mM; Need ultrasonic)

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.171 ml	10.856 ml	21.712 ml
5 mM	0.434 ml	2.171 ml	4.342 ml
10 mM	0.217 ml	1.086 ml	2.171 ml
50 mM	0.043 ml	0.217 ml	0.434 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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