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  3. XY153

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。

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XY153 Chemical Structure

XY153 Chemical Structure

CAS No. : 2933176-32-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

XY153 (compound 8l) is a BD2-selective BET inhibitor and selectively binds to BRD4 BD2. XY153 binds to BRD4 BD2, BRD3 BD2 and BRD2 BD2 with IC50s 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) and cancer[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 IC50 value of 4.6 μM.
分子量

555.64

Formula

C33H34FN3O4

CAS 号
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.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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XY153
目录号:
HY-143317
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