DDO-2093 dihydrochloride

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

DDO-2093 dihydrochloride 是一种有效的MLL1和WDR5蛋白-蛋白相互作用抑制剂 (IC₅₀=8.6 nM;K_d=11.6 nM)，具有抗肿瘤活性。DDO-2093 dihydrochloride 选择性抑制 MLL 复合物的催化活性。

生物活性

DDO-2093 dihydrochloride is a potentMLL1-WDR5 protein-protein interactioninhibitor (IC₅₀=8.6 nM;K_d=11.6 nM) with antitumor activity. DDO-2093 dihydrochloride selectively inhibits the catalytic activity of MLL complex^[1].

体外研究
(In Vitro)

DDO-2093 (5 μM; pretreated 7 days) dihydrochloride inhibits MLL-fusion protein dependent genes expression (HOXA9andMeis1)^[1].

Western Blot Analysis^[1]

Cell Line:	MV4-11 cells
Concentration:	1, 2.5, 5, and 10 μM
Incubation Time:	7 days
Result:	Dose-dependently reduced the mono-, di-, and trimethylation of H3K4.

体内研究
(In Vivo)

DDO-2093 (20-80 mg/kg; i.p.; every other day for 21 days) dihydrochloride significantly suppresses the tumor size and weight in a dose-dependent manner^[1].

Animal Model:	Female nude mice (MV4-11 human leukemia cancer xenografts)^[1]
Dosage:	20, 40, and 80 mg/kg
Administration:	Intraperitoneal injection; every other day for 21 days
Result:	Had the tumor volume growth inhibition (GI) values were calculated to be 13.7%, 37.6% and 63.9% with doses of 20 mg/kg, 40 mg/kg and 80 mg/kg, respectively.

分子量

687.04

性状

Solid

Formula

C₂₉H₃₉Cl₃FN₉O₃

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month