貨號	規格	價格	上海	北京	武漢	南京
S81559-5mg	98.1%	￥300.00 S81559-5mg ￥300.00 現貨	5 5	-	-	-
S81559-10mg	98.1%	￥460.00 S81559-10mg ￥460.00 現貨	5 5	-	-	-
S81559-25mg	98.1%	￥600.00 S81559-25mg ￥600.00 現貨	5 5	-	-	-
S81559-100mg	98.1%	￥1400.00 S81559-100mg ￥1400.00 現貨	2 2	-	-	-

產品介紹

SNX-5422 is a synthetic, novel, small molecule Hsp90 Inhibitor. As an oral formulation that demonstrates strong efficacy and tolerability, SNX-5422 is positioned as a breakthrough therapy with broad applicability across a wide range of cancers.

產品描述：

靶點：

HSP;HER;HSP;?HER

體內研究：

PF-04929113對Her-2穩定性表現出有效的作用并導致預期的Hsp70上調。PF-04929113顯示針對廣泛癌癥細胞類型的有效抗增殖活性,例如,MCF-7（IC50 = 16 nM）,SW620（IC50 = 19 nM）,K562（IC50 = 23 nM）,SK-MEL-5（IC50 = 25 nM）和A375（IC50 = 51 nM）

細胞實驗：

Cell lines: MCF-7,SW620,K562,SK-MEL-5 and A375 cancer cell lines. Concentrations: 0-300 nM. Method: Proliferation rates are measured by seeding cells into 96-well plates,followed by compound addition 24 h later.After addition of PF-04929113,cells are allowed to grow for either an additional 72 or 144 h depending on the rate of growth.At harvest,media is removed and DNA content for individual wells is determined using CyQuant DNA dye.Levels of Hsp90 client proteins and phosphor-regulated proteins in A375 are measured by high content analysis (HCA) using an ArrayScan 4.5 instrument after 24 hours of treatment with PF-04929113,followed by methanol fixation.After fixation in 4% PBS-buffered formalin and permeablization with 0.1% TX-100,cells are probed with anti-Her2,antiphospho-S6 (pS6),antipERK,and anti-Hsp70 primary antibodies,followed by TRITC or FITC conjugated secondary antibodies.Nuclei are also stained with Hoechst DNA binding dye.For each well,250-500 individual nuclei are identified along with the avera

動物實驗：

Animal Models: 5 ×106 MM.1S cells are inoculated subcutaneously in the Fox Chase SCID mice (6-7 weeks old). Formulation: PF-04929113 is dissolved in 1% carboxy methylcellulose/0.5% Tween 80 at 10 mg/mL and stored at 4 °C. Dosages: 20 or 40 mg/kg. Administration: orally 3 times per week,3 weeks in total.

參考文獻：

1.Lamoureux F, et al, Clin Cancer Res, 2011, 17(8), 2301-2313. 2.Huang KH, et al, J Med Chem, 2009, 52(14), 4288-4305 3.Yutaka Okawa, et al, Blood, 2009, 113(4), 846-855.

溶解性：

H2O:<1 mg/mL Ethanol:3 mg/mL(5.8 mM) DMSO:96 mg/mL (184.1 mM)

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.917 ml	9.587 ml	19.174 ml
5 mM	0.383 ml	1.917 ml	3.835 ml
10 mM	0.192 ml	0.959 ml	1.917 ml
50 mM	0.038 ml	0.192 ml	0.383 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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PF-04929113 (SNX-5422)