XY153

Cat. No.: HY-143317: FAQs
Data Sheet Handling Instructions

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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

CAS No. : 2933176-32-8

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Description

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].

MedChemExpress (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

CAS No.

2933176-32-8

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

Handling Instructions (2659 KB)

References

[1]. Li J, et al. Structure-Based Discovery and Optimization of Furo[3,2-c]pyridin-4(5H)-one Derivatives as Potent and Second Bromodomain (BD2)-Selective Bromo and Extra Terminal Domain (BET) Inhibitors. J Med Chem. 2022 Apr 14;65(7):5760-5799. [Content Brief]

XY153 Related Classifications

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Keywords:

XY1532933176-32-8XY 153XY-153Epigenetic Reader Domainanti-proliferationanticancerAMLBD222Rv1HT-29MV4-11MOLM-13Kasumi-1THP-1Inhibitorinhibitorinhibit

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