XY153

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XY153

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。

XY153 (compound 8l) 是 BD2 选择性的BET抑制剂，选择性地与 BRD4 BD2 结合。XY153 与 BRD4 BD2，BRD3 BD2 和 BRD2 BD2 结合IC₅₀值分别为 0.79，5.31 和 5.09 nM。XY153 对多种肿瘤细胞系显示出有效的抗增殖活性。XY153 可用于急性髓性白血病和癌症的研究。

生物活性

XY153 (compound 8l) is a BD2-selectiveBETinhibitor and selectively binds toBRD4BD2. XY153 binds toBRD4BD2,BRD3BD2 andBRD2BD2 withIC₅₀s of 0.79, 5.31 and 5.09 nM, respectively. XY153 shows potent antiproliferative activity against multiple tumor cell lines. XY153 can be used for the research of acute myeloid leukemia (AML) andcancer^[1].

IC₅₀& Target

IC50: 0.79 nM (BRD4 BD2), 5.31 nM (BRD3 BD2), 5.09 nM (BRD2 BD2)^[1]

体外研究
(In Vitro)

XY153 shows strong antiproliferative activities for specific cancer cell lines but with a better safety profile against a normal lung fibroblast cell line^[1].

Cell Viability Assay^[1]

Cell Line:	MV4-11, MOLM-13, Kasumi-1, THP-1, HT-29, 22Rv1, Du145, MCF-7, MDA-MB-231, A549, U2OS, U937, HepG2, BxPC-3 and HFL-1 cell lines
Concentration:	0.001 nM-10 μM
Incubation Time:	96 hours
Result:	Inhibited acute myeloid leukemia (AML) cell lines with IC₅₀s of 0.55 nM, 260 nM, 471 nM and 1.3 μM for MV4-11, MOLM-13, Kasumi-1 and THP-1 cell lines, respectively. Showed potent cytotoxicity to AR-positive prostate cancer cell line 22Rv1 and colorectal cancer cell line HT-29 with IC₅₀s of 232 and 300 nM, respectively. Exhibited weak cytotoxicity to normal lung fibroblast cell line HFL-1 with an IC₅₀value of 4.6 μM.

分子量

555.64

Formula

C₃₃H₃₄FN₃O₄

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.