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Chemical Structure| 2081072-29-7 Chemical Structure| 2081072-29-7

Structure of NEO2734
CAS No.: 2081072-29-7

Chemical Structure| 2081072-29-7

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NEO2734 is an orally dual p300/CBP and BET bromodomain inhibitor with IC50 values of <30 nM for both p300/CBP and BET bromodomains.

Synonyms: EP31670

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Product Details of NEO2734

CAS No. :2081072-29-7
Formula : C22H24F3N3O3
M.W : 435.44
SMILES Code : O=C1C(C)=CC(C2=CC=C3N=C(C4CCOCC4)N(CCOC(F)(F)F)C3=C2)=CN1C
Synonyms :
EP31670
MDL No. :MFCD32857168
InChI Key :KPWWFNXRLAAREN-UHFFFAOYSA-N
Pubchem ID :126582741

Safety of NEO2734

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H312-H332
Precautionary Statements:P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P330-P362-P403+P233-P501

Related Pathways of NEO2734

epigenetics

Isoform Comparison

Biological Activity

Description
NEO2734 (EP31670) is an orally active inhibitor selectively targeting both p300/CBP and BET bromodomains, displaying IC50 values of less than 30 nM for each[1].
Target
  • p300/CBP

    p300/CBP, IC50:<30 nM

  • BET

    BET, IC50:<30 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
KG1 100 nM 48 hours NEO2734 significantly downregulated the expression of c-Myc and Bcl2. Hemasphere. 2021 Jul 8;5(8):e610.
KN473 60 µM 72 hours Evaluate the antitumor activity of NEO2734 on UPS cells, results showed over 40% of viable cells remained at higher doses Transl Oncol. 2025 Feb;52:102236.
IB119 25 µM 72 hours Evaluate the antitumor activity of NEO2734 on UPS cells, results showed over 40% of viable cells remained at higher doses Transl Oncol. 2025 Feb;52:102236.
DLBCL cell lines 157 nM (median IC50) 72 hours Evaluate the antiproliferative activity of NEO2734 in DLBCL cell lines, showing higher sensitivity in ABC-DLBCL than GCB-DLBCL Blood Adv. 2020 Sep 8;4(17):4124-4135.
Primary AML cells 6-175 nM 4 days NEO2734 significantly eliminated primary AML cells and reduced cell survival by inducing apoptosis. Hemasphere. 2021 Jul 8;5(8):e610.
KG1a 27-125 nM 96 hours NEO2734 significantly reduced the viability of AML cell lines and induced apoptosis. Hemasphere. 2021 Jul 8;5(8):e610.
MV4;11 100 nM 2 and 5 hours NEO2734 significantly downregulated the expression of c-Myc but had minimal effect on Bcl2, though it reduced MCL1 expression. Hemasphere. 2021 Jul 8;5(8):e610.
THP1 100 nM 2 and 5 hours NEO2734 significantly downregulated the expression of c-Myc and Bcl2. Hemasphere. 2021 Jul 8;5(8):e610.
HL60 27-125 nM 96 hours NEO2734 significantly reduced the viability of AML cell lines and induced apoptosis. Hemasphere. 2021 Jul 8;5(8):e610.
C4-2 cells 2 μM 72 hours To evaluate the inhibitory effect of NEO2734 on the growth of SPOP mutant C4-2 cells. Results showed that F133V mutant cells were resistant to JQ1 but sensitive to NEO2734. EMBO Mol Med. 2019 Nov 7;11(11):e10659.
DU145 cells 2 μM 72 hours To evaluate the inhibitory effect of NEO2734 on the growth of SPOP Q165P mutant DU145 cells. Results showed that NEO2734 significantly inhibited cell growth, with superior effect compared to the combination of JQ1 and CPI-637. EMBO Mol Med. 2019 Nov 7;11(11):e10659.
SNU-407 0.036 µM 72 hours To evaluate the inhibitory effect of NEO2734 on the growth of SNU-407 cells, results showed that NEO2734 significantly inhibited cell growth with an IC50 of 0.036 µM. Front Oncol. 2022 Oct 12;12:1018775.
NCI-H508 0.059 µM 72 hours To evaluate the inhibitory effect of NEO2734 on the growth of NCI-H508 cells, results showed that NEO2734 significantly inhibited cell growth with an IC50 of 0.059 µM. Front Oncol. 2022 Oct 12;12:1018775.
DLD-1 10 µM 48 hours To evaluate the effect of NEO2734 on apoptosis in DLD-1 cells, results showed that NEO2734 induced cleavage of caspase-3, indicating activation of apoptosis. Front Oncol. 2022 Oct 12;12:1018775.
RKO 10 µM 48 hours To evaluate the effect of NEO2734 on apoptosis in RKO cells, results showed that NEO2734 induced cleavage of caspase-3, indicating activation of apoptosis. Front Oncol. 2022 Oct 12;12:1018775.
LOVO 1 µM 48 hours To evaluate the effect of NEO2734 on apoptosis in LOVO cells, results showed that NEO2734 induced cleavage of caspase-3, indicating activation of apoptosis. Front Oncol. 2022 Oct 12;12:1018775.
HCT116 10 µM 24 hours To evaluate the effect of NEO2734 on apoptosis in HCT116 cells, results showed that NEO2734 significantly increased the proportion of Annexin V-positive cells, indicating induction of apoptosis. Front Oncol. 2022 Oct 12;12:1018775.
JR588 0.2863 µM 72 hours Evaluate the antitumor activity of NEO2734 on UPS cells, results showed NEO2734 decreased cell viability through regulation of E2F targets and cell cycle Transl Oncol. 2025 Feb;52:102236.
IB106 1.088 µM 72 hours Evaluate the antitumor activity of NEO2734 on UPS cells, results showed NEO2734 decreased cell viability through regulation of E2F targets and cell cycle Transl Oncol. 2025 Feb;52:102236.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
SCID (CB17) mice MV4;11 tumor xenograft model Oral 10 mg/kg Once daily for 11 consecutive days NEO2734 significantly inhibited tumor growth of MV4;11 cells. Hemasphere. 2021 Jul 8;5(8):e610.
SCID mice SPOP Q165P mutant PDX model Intraperitoneal injection 30 mg/kg 5 days per week for 3 consecutive weeks To evaluate the inhibitory effect of NEO2734 on the growth of SPOP Q165P mutant PDX tumors. Results showed that NEO2734 significantly suppressed tumor growth, with superior effect compared to the combination of JQ1 and CPI-637. EMBO Mol Med. 2019 Nov 7;11(11):e10659.
Nude mice HCT116 xenograft model Oral gavage 30 mg/kg Administered on days 1, 5, and 9, for a total of 9 days To evaluate the antitumor effect of NEO2734 in the HCT116 xenograft model, results showed that NEO2734 significantly inhibited tumor growth and induced tumor cell apoptosis. Front Oncol. 2022 Oct 12;12:1018775.
Rag2-/- γc-/- mice JR588 and KN473 PDX models Oral 10 mg/kg Once daily (5 days-on/2 days-off) Evaluate the antitumor activity of NEO2734 in vivo, results showed NEO2734 significantly inhibited tumor growth in JR588 PDX model Transl Oncol. 2025 Feb;52:102236.
Mice 22Rv1 xenograft model Intraperitoneal injection 10 mg/kg 5 days per week for 21 days Evaluate the effect of NEO2734 alone or in combination with ENZ on 22Rv1 xenograft tumor growth, results showed combination therapy significantly inhibited tumor growth Cancer Res. 2023 Oct 2;83(19):3192-3204
NOD-SCID mice TMD8 xenograft model Oral 10 mg/kg Once daily, 6 days per week Evaluate the antitumor activity of NEO2734 in a DLBCL xenograft model, showing significant tumor growth inhibition Blood Adv. 2020 Sep 8;4(17):4124-4135.

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT05488548 Castrate Resistant Prostate Ca... More >>ncer|NUT Carcinoma|Chronic Myelomonocytic Leukemia|Myelofibrosis Less << PHASE1 RECRUITING 2025-05-25 Mayo Clinic Arizona, Phoenix, ... More >>Arizona, 85054, United States|Mayo Clinic Florida, Jacksonville, Florida, 32224, United States|Dana Farber Cancer Institute, Boston, Massachusetts, 02215, United States|Mayo Clinic Rochester, Rochester, Minnesota, 55905, United States|The University of Texas MD Anderson Cancer Center, Houston, Texas, 77030, United States|University of Washington/Fred Hutchinson Cancer Center, Seattle, Washington, 98109, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.30mL

0.46mL

0.23mL

11.48mL

2.30mL

1.15mL

22.97mL

4.59mL

2.30mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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