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NEO2734 (EP31670)

Cat. No. M10489
NEO2734 (EP31670) Structure
Synonym:

EP31670; NEO-2734

Size Price Availability Quantity
5mg USD 350  USD350 In stock
10mg USD 550  USD550 In stock
25mg USD 800  USD800 In stock
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Quality Control & Documentation
Biological Activity

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

Chemical Information
Molecular Weight 435.44
Formula C22H24F3N3O3
CAS Number 2081072-29-7
Solubility (25°C) DMSO 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Katie R Ryan, et al. Eur J Haematol. Targeting both BET and CBP/EP300 proteins with the novel dual inhibitors NEO2734 and NEO1132 leads to anti-tumor activity in multiple myeloma

[2] Chevaun D Morrison-Smith, et al. Mol Cancer Ther. Combined Targeting of the BRD4-NUT-p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734

[3] Yuqian Yan, et al. EMBO Mol Med. The novel BET-CBP/p300 dual inhibitor NEO2734 is active in SPOP mutant and wild-type prostate cancer

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  Catalog
Abmole Inhibitor Catalog




Keywords: NEO2734 (EP31670), EP31670; NEO-2734 supplier, Epigenetic Reader Domain, inhibitors, activators


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