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DS-9300
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。
DS-9300图片
CAS NO:2259641-46-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
DS-9300 是一种高效的、具有口服活性的选择性EP300/CBP HAT抑制剂,IC50值为 28 nM。DS-9300 具有抗癌活性,可用于前列腺癌疾病研究。
生物活性

DS-9300 is a potent, orally active, selectiveEP300/CBP HATinhibitor with anIC50value of 28 nM. DS-9300 has anticancer activity and can be used in prostatecancerdisease research[1].

体外研究
(In Vitro)

DS-9300 inhibits the growth of prostate cancer cell lines with the IC50values of 0.6, 6.5, 3.4 and 287.2 nM for VCaP, 22Rv1, LNCaP and PC3 cells, respectively, indicating that it could effectively inhibit the growth of prostate cancer cell lines by inhibiting histone acetylation and down-regulating PSA expression[1].

体内研究
(In Vivo)

DS-9300 (p.o., 0.3-3 mg/kg, once daily, 33days) shows dose-dependent antitumor activity with 39%, 74% and 109% tumor growth inhibition at 0.3, 1 and 3 mg/kg, respectively, and no significant toxic effects in Castrated VCaP xenograft mouse model[1].
The pharmacokinetic parameters of DS-9300 in BALB/c mice

PO(10 mg/kg)IV(1 mg/kg)
AUC, AUCu(μM*h)Cmax(μM)T1/2(h)<Vdss(L/kg)CL, CLu(mL/min/kg)F%
130, 5.33342.40.141.6, 3962

分子量

501.50

Formula

C25H26F3N5O3

CAS 号

2259641-46-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.