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Bromodomain IN-2

Cat. No. M41642
Bromodomain IN-2 Structure
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Biological Activity

BD-IN-1 is a pan bromodomain (BD) inhibitor with KD values of 250, 420, 130, 430, 67, 240, 970 nM for BRD4(1), CBP, BRPF1B, BRD7, BRD9, BRDT(1), CECR2 respectively.

Chemical Information
Molecular Weight 288.77
Formula C16H17ClN2O
CAS Number 2445335-77-1
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] Peter P Toth et al. Am J Prev Cardiol. Reduction in the risk of major adverse cardiovascular events with the BET protein inhibitor apabetalone in patients with recent acute coronary syndrome, type 2 diabetes, and moderate to high likelihood of non-alcoholic fatty liver disease

[2] Gautam Borthakur et al. Cancer. A phase 1 study of the pan-bromodomain and extraterminal inhibitor mivebresib (ABBV-075) alone or in combination with venetoclax in patients with relapsed/refractory acute myeloid leukemia

[3] Tiziana Servidei et al. Int J Mol Sci. The BET Inhibitor OTX015 Exhibits In Vitro and In Vivo Antitumor Activity in Pediatric Ependymoma Stem Cell Models

[4] Todd M Stevens et al. Mod Pathol. NUTM1-rearranged neoplasia: a multi-institution experience yields novel fusion partners and expands the histologic spectrum

[5] Minsun Jung et al. Oncologist. Clinicopathological and Preclinical Findings of NUT Carcinoma: A Multicenter Study

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Keywords: Bromodomain IN-2 supplier, Epigenetic Reader Domain, inhibitors, activators


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