貨號(hào)	規(guī)格	價(jià)格	上海	北京	武漢	南京
S82527-1mg	99.5%	￥560.00 S82527-1mg ￥560.00 現(xiàn)貨	11 >10	-	-	-
S82527-5mg	99.5%	￥1820.00 S82527-5mg ￥1820.00 現(xiàn)貨	11 >10	-	-	-
S82527-10mg	99.5%	￥3570.00 S82527-10mg ￥3570.00 現(xiàn)貨	13 >10	-	-	-

產(chǎn)品介紹

Tinostamustine (EDO-S101) is a pan HDAC inhibitor; inhibits HDAC6, HDAC1, HDAC2 and HDAC3 with IC50 values of 6 nM, 9 nM, 9 nM and 25 nM, respectively

產(chǎn)品描述：

Tinostamustine (EDO-S101) is a pan HDAC inhibitor; inhibits HDAC6, HDAC1, HDAC2 and HDAC3 with IC50 values of 6 nM, 9 nM, 9 nM and 25 nM, respectively

靶點(diǎn)：

HDAC6:6 nM (IC50);HDAC1:9 nM (IC50);HDAC2:9 nM (IC50);HDAC3:25 nM (IC50);HDAC10:72 nM (IC50);HDAC8:107 nM (IC50);HDAC

體外研究：

Tinostamustine inhibits HDAC activity in rat peripheral blood mononuclear cells (PBMCs) in a cellular assay by approximately 90% one hour after dosing with 10mg/kg i.v. HDAC inhibition in PBMCs could not be increased with higher doses up to 50mg/kg. Tinostamustine triggers apoptosis and shows strong antitumor activity in HL60 and Daudi cells. Initial in vitro experiments in HL60 cells shows an activation of the intrinsic pathway of apoptosis with cleavage of caspases 3, 9 and PARP and a marked reduction of anti-apoptotic proteins XIAP and Mcl-1

體內(nèi)研究：

Intracellular HDAC inhibition of Tinostamustine, which occurs rapidly after dosing is at maximum activity already at the lowest dose of 10mg/kg and lasts for about 12-16 hours. Exposure to Tinostamustine causes a strong DNA repair response evidenced by activation of pH2AX and p53 in tumors taken from mice bearing subcutaneous human Burkitt’s lymphoma. Tumors of BL rapidly shrink or are completely eradicated after i.v. administration of Tinostamustine

參考文獻(xiàn)：

1. Mehrling T, et al. The Alkylating-HDAC Inhibition Fusion Principle: Taking Chemotherapy to the Next Level with the First in Class Molecule EDO-S101. Anticancer Agents Med Chem. 2016;16(1):20-8.

溶解性：

Soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.408 ml	12.038 ml	24.076 ml
5 mM	0.482 ml	2.408 ml	4.815 ml
10 mM	0.241 ml	1.204 ml	2.408 ml
50 mM	0.048 ml	0.241 ml	0.482 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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