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  3. XY153

XY153 

Cat. No.: HY-143317
Handling Instructions

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.

For research use only. We do not sell to patients.

XY153 Chemical Structure

XY153 Chemical Structure

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Description

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]

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.
Molecular Weight

555.64

Formula

C33H34FN3O4

SMILES

CC1=CC(F)=CC(C)=C1OC2=C(C=C(C=C2)C(C)(O)C)C3=CN(C(C4=C3OC(C5=CN=C(N5)C6CCCC6)=C4)=O)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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XY153
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HY-143317
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