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INCB054329

Cat. No. M13822
INCB054329 Structure
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Biological Activity

INCB054329 is a potent BET inhibitor.

Chemical Information
Molecular Weight 348.36
CAS Number 1628607-64-6
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] Haley E Ramsey, et al. Clin Cancer Res. BET Inhibition Enhances the Antileukemic Activity of Low-dose Venetoclax in Acute Myeloid Leukemia

[2] Pei Wan, et al. Oncol Rep. BRDT is a novel regulator of eIF4EBP1 in renal cell carcinoma

[3] Ramiro Vzquez, et al. Eur Urol Oncol. Efficacy of Novel Bromodomain and Extraterminal Inhibitors in Combination with Chemotherapy for Castration-Resistant Prostate Cancer

[4] Matthew C Stubbs, et al. Clin Cancer Res. The Novel Bromodomain and Extraterminal Domain Inhibitor INCB054329 Induces Vulnerabilities in Myeloma Cells That Inform Rational Combination Strategies

[5] Andrew J Wilson, et al. Gynecol Oncol. The BET inhibitor INCB054329 reduces homologous recombination efficiency and augments PARP inhibitor activity in ovarian cancer

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Keywords: INCB054329 supplier, Epigenetic Reader Domain, inhibitors, activators


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