Home Cart Sign in  
Chemical Structure| 2081072-29-7 Chemical Structure| 2081072-29-7

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

Chemical Structure| 2081072-29-7

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

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

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Alternative Products

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
HL60 27-125 nM 96 hours NEO2734 significantly reduced the viability of AML cell lines and induced apoptosis. PMC8265862
THP1 100 nM 2 and 5 hours NEO2734 significantly downregulated the expression of c-Myc and Bcl2. PMC8265862
KG1a 27-125 nM 96 hours NEO2734 significantly reduced the viability of AML cell lines and induced apoptosis. PMC8265862
KG1 100 nM 48 hours NEO2734 significantly downregulated the expression of c-Myc and Bcl2. PMC8265862
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 PMC11713734
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 PMC11713734
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 PMC7479962
Primary AML cells 6-175 nM 4 days NEO2734 significantly eliminated primary AML cells and reduced cell survival by inducing apoptosis. PMC8265862
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. PMC8265862
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. PMC6835201
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. PMC6835201
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. PMC9599411
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. PMC9599411
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. PMC9599411
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. PMC9599411
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. PMC9599411
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. PMC9599411
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 PMC11713734
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 PMC11713734

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. PMC8265862
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. PMC6835201
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. PMC9599411
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 PMC11713734
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 PMC10543964
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 PMC7479962

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

 

Historical Records

Categories