NEO2734

Catalog No.S9648 Batch:S964801

Technical Data

Formula	C₂₂H₂₄F₃N₃O₃
Molecular Weight	435.44	CAS No.	2081072-29-7
Solubility (25°C)*	In vitro	DMSO	87 mg/mL (199.79 mM)
		Ethanol	87 mg/mL (199.79 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

NEO2734 (EP31670) is a novel, orally active and selective dual inhibitor of p300/CBP and BET bromodomain with IC50 of both <30 nM.

Targets

p300/CBP ^[1] (Cell-free assay)	BET ^[1] (Cell-free assay)
<30 nM	<30 nM

In vitro

Treatment of NMC cells with the novel dual p300/CBP and BET bromodomain–selective inhibitor, NEO2734, potently inhibits growth and induces differentiation of NMC cells in vitro; findings that correspond with potentiated transcriptional effects from combined BET and p300 bromodomain inhibition.^[1]

In vivo

In three disseminated NMC xenograft models, NEO2734 provides greater growth inhibition, with tumor regression and significant survival benefit seen in two of three models, compared with a lead clinical BET inhibitor or “standard” chemotherapy.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines NUT carcinoma patient cell lines (TC-797, 14169, 10-15, PER-403) Concentrations 1 μM Incubation Time 24 h Method NUT carcinoma patient cell lines (TC-797, 14169, 10-15, and PER-403) are plated in T-25 flasks and grown in DMEM (797) containing 10 % fetal bovine serum and 1 % penicillin/streptomycin. Cells are treated with either 500 nM OTX-015, 1 μM GNE-781, combination of 62.5 nM GNE-781 and 62.5 nM OTX-015, 1 μM NEO2734, or the equivalent volume of DMSO (0.025 %). At 24H, 2 × 10⁶ cells are spun at 500 × g for 5 minutes at 4 ℃ and washed twice with PBS. Pellets are resuspended in 1 ml of cold PBS and added dropwise while gently vortexing to 9 ml 70 % ethanol in a 15 ml polypropylene centrifuge tube. Fixed cells are then frozen at –20 ℃ overnight. The next day, cells are centrifuged at 500 × g for 10 minutes at 4 ℃ and washed twice with 3 ml of cold PBS. Cells are resuspended in 400 μl of propidium iodide staining solution (0.2 mg/ml RNAse A, 0.02 mg/ml propidium iodide, 0.1 % Triton-X in PBS) and incubated for 15 minutes at 37 ℃.
Animal Study:^{^[1]}	Animal Models tumor bearing NSG mice Dosages 8 mg/kg Administration Oral gavage

Cell Assay:^{^[1]}

Cell lines
NUT carcinoma patient cell lines (TC-797, 14169, 10-15, PER-403)
Concentrations
1 μM
Incubation Time
24 h
Method
NUT carcinoma patient cell lines (TC-797, 14169, 10-15, and PER-403) are plated in T-25 flasks and grown in DMEM (797) containing 10 % fetal bovine serum and 1 % penicillin/streptomycin. Cells are treated with either 500 nM OTX-015, 1 μM GNE-781, combination of 62.5 nM GNE-781 and 62.5 nM OTX-015, 1 μM NEO2734, or the equivalent volume of DMSO (0.025 %). At 24H, 2 × 10⁶ cells are spun at 500 × g for 5 minutes at 4 ℃ and washed twice with PBS. Pellets are resuspended in 1 ml of cold PBS and added dropwise while gently vortexing to 9 ml 70 % ethanol in a 15 ml polypropylene centrifuge tube. Fixed cells are then frozen at –20 ℃ overnight. The next day, cells are centrifuged at 500 × g for 10 minutes at 4 ℃ and washed twice with 3 ml of cold PBS. Cells are resuspended in 400 μl of propidium iodide staining solution (0.2 mg/ml RNAse A, 0.02 mg/ml propidium iodide, 0.1 % Triton-X in PBS) and incubated for 15 minutes at 37 ℃.

Animal Study:^{^[1]}

Animal Models
tumor bearing NSG mice
Dosages
8 mg/kg
Administration
Oral gavage

References

[1] Chevaun D Morrison-Smith, et al. Mol Cancer Ther. 2020 Jul;19(7):1406-1414.

Selleck's NEO2734 has been cited by 5 publications

Targeting of vulnerabilities of drug-tolerant persisters identified through functional genetics delays tumor relapse [ Cell Rep Med, 2024, 5(3):101471]	PubMed: 38508142
PD-1 instructs a tumor-suppressive metabolic program that restricts glycolysis and restrains AP-1 activity in T cell lymphoma [ Nat Cancer, 2023, 4(10):1508-1525]	PubMed: 37723306
Characterization of molecular mechanisms driving Merkel cell polyomavirus oncogene transcription and tumorigenic potential [ PLoS Pathog, 2023, 19(8):e1011598]	PubMed: 37647312
PD-1 instructs a tumor-suppressive metabolic program that restricts glycolysis and restrains AP-1 activity in T cell lymphoma [ Nat Cancer, 2023, 10.1038/s43018-023-00635-7]	PubMed: 37723306
Therapeutic impact of BET inhibitor BI 894999 treatment: backtranslation from the clinic [ Br J Cancer, 2022, 10.1038/s41416-022-01815-5]	PubMed: 35444289

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SHIPPING AND STORAGE
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