貨號(hào)	規(guī)格	價(jià)格	上海	北京	武漢	南京
S80570-2mg	99.5%	￥400.00 S80570-2mg ￥400.00 現(xiàn)貨	5 5	-	-	-
S80570-5mg	99.5%	￥530.00 S80570-5mg ￥530.00 現(xiàn)貨	2 2	-	-	-
S80570-10mg	99.5%	￥800.00 S80570-10mg ￥800.00 現(xiàn)貨	4 4	-	-	-
S80570-25mg	99.5%	￥1290.00 S80570-25mg ￥1290.00 現(xiàn)貨	5 5	-	-	-

產(chǎn)品介紹

Tasquinimod is an oral antiangiogenic agent, which has the potential for castration-resistant prostate cancer treatment. Tasquinimod binds to the regulatory Zn2+ binding domain of HDAC4 with Kd of 10-30 nM. Tasquinimod also is a S100A9 inhibitor

產(chǎn)品描述：

靶點(diǎn)：

HDAC4:10-30 nM (Kd);HDAC

體內(nèi)研究：

The bioavailability and oral absorption of Tasquinimod is excellent when adult male mice (i.e., C57Bl/6J, or athymic nude mice) are given 0.1-30 mg/kg (i.e., 0.2-74 μmoles/kg) via gavage or the drinking water. The potency of Tasquinimod expressed as the daily oral dose of Tasquinimod which inhibits cancer growth by 50% ranges from 0.1-1.0 mg/kg/d (i.e., 0.24-2.40 μmoles/kg/day) against a series (n>5) of human prostate cancer xenografts in immune-deficient mice. Tasquinimod at a chronic dose of 5 mg/kg/day via the drinking water produces > 80% inhibition (p<0.05) of TRAMP-C2 mouse prostate cancer growth in immune-competent syngeneic mice. Nude mice carrying subcutaneous LNCaP tumors are treated with Tasquinimod for 3 weeks. Exposure to Tasquinimod at 1 mg/kg/day and 10 mg/kg/day started on day 7 after inoculation. There is a statistically significant dose dependent reduction in tumor weight both at 1 mg/kg/day and 10 mg/kg/day compare to the untreated control group 28 days after inoculation (p<0.001), illustrating the anti-tumor effect of Tasquinimod

參考文獻(xiàn)：

1. Isaacs JT, et al. Tasquinimod Is an Allosteric Modulator of HDAC4 survival signaling within the compromised cancer microenvironment. Cancer Res. 2013 Feb 15;73(4):1386-99. 2. Isaacs JT, et al. Anti-cancer potency of tasquinimod is enhanced via albumin-binding facilitating increased uptake in the tumor microenvironment. Oncotarget. 2014 Sep 30;5(18):8093-106. 3. Olsson A, et al. Tasquinimod (ABR-215050), a quinoline-3-carboxamide anti-angiogenic agent, modulates the expression of thrombospondin-1 in human prostate tumors. Mol Cancer. 2010 May 17;9:107.

溶解性：

DMSO : ≥ 42 mg/mL (103.36 mM) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.461 ml	12.304 ml	24.609 ml
5 mM	0.492 ml	2.461 ml	4.922 ml
10 mM	0.246 ml	1.23 ml	2.461 ml
50 mM	0.049 ml	0.246 ml	0.492 ml

注意：

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

參考文獻(xiàn)

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