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Cat. No.: HY-143317

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XY153

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.

CAS No.: 2933176-32-8
Formula: C₃₃H₃₄FN₃O₄
Molecular Weight:555.64

Storage:

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

Data Sheet (275 KB)

XY153 Chemical Structure

CAS No.: 2933176-32-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

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

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Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	1 μM Compound: 8l; XY153	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 35333526]
BXPC-3	IC₅₀	1 μM Compound: 8l; XY153	Antiproliferative activity against human BxPC-3 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay Antiproliferative activity against human BxPC-3 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 35333526]
CWR22R	IC₅₀	232 nM Compound: 8l; XY153	Antiproliferative activity against human 22Rv1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay Antiproliferative activity against human 22Rv1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 35333526]
DU-145	IC₅₀	1 μM Compound: 8l; XY153	Antiproliferative activity against AR-negative human DU-145 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay Antiproliferative activity against AR-negative human DU-145 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 35333526]
HepG2	IC₅₀	1 μM Compound: 8l; XY153	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 35333526]
HFL1	IC₅₀	4.6 μM Compound: 8l; XY153	Cytotoxicity against human HFL1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay Cytotoxicity against human HFL1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 35333526]
HT-29	IC₅₀	300 nM Compound: 8l; XY153	Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 120 hrs by Cell titre Glo-luminiscence cell viability assay Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 120 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 35333526]
Kasumi 1	IC₅₀	471 nM Compound: 8l; XY153	Antiproliferative activity against human Kasumi 1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay Antiproliferative activity against human Kasumi 1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 35333526]
MCF7	IC₅₀	1 μM Compound: 8l; XY153	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 96 hrs by Cell titre Glo-luminiscence cell viability assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 96 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 35333526]
MDA-MB-231	IC₅₀	1 μM Compound: 8l; XY153	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 96 hrs by Cell titre Glo-luminiscence cell viability assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 96 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 35333526]
MOLM-13	IC₅₀	260 nM Compound: 8l; XY153	Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 35333526]
MV4-11	IC₅₀	0.00054 μM Compound: 8l; XY153	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 120 hrs by Cell titre Glo-luminiscence cell viability assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 120 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 35333526]
THP-1	IC₅₀	1.3 μM Compound: 8l; XY153	Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 35333526]
U2OS	IC₅₀	1 μM Compound: 8l; XY153	Antiproliferative activity against human U2OS cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay Antiproliferative activity against human U2OS cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 35333526]
U-937	IC₅₀	1 μM Compound: 8l; XY153	Antiproliferative activity against human U-937 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay Antiproliferative activity against human U-937 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay	[PMID: 35333526]

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.

Chemical Information

CAS No. 2933176-32-8
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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XY153

All Epigenetic Reader Domain Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

XY153 Related Classifications

HY-143317 Related Classifications