BET-IN-12
BET-IN-12 is an orally avtive inhibitor of bromodomain and extra-terminal (BET) with an IC50 of 0.9 nM for BRD4.
For research use only. We do not sell to patients.
- CAS No.: 1800343-11-6
- Formula: C30H29D3FN5O2
- Molecular Weight:516.62
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
0.9 nM (BRD4)[1]
BET-IN-12 (compound 15) (24 hours) displays BRD4 and c-Myc inhibition, MM proliferation with IC50s values of 0.9 nM, 2.0 nM, and 6.0 nM, respectively[1]. BET-IN-12 (compound 15) (24 hours) has high oxidative stability across species and low glucuronidation across species, so that translate into low orally administered minimum efficacious doses (MEDs) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| dose (iv/po, mg/kg) | CLp ((mL/min)/kg) | Vd (L/kg) | half-life (ie, h) | F (%) | AUC (po, nM.h) | |
| mouse | 1.0/3.0 | 4.2 | 1.4 | 3.4 | 100 | 25000 |
| rat | 1.0/5.0 | 18 | 2.9 | 4.1 | 74 | 6600 |
| dog | 0.1/0.3 | 13 | 5.8 | 7.6 | 73 | 550 |
| monkey | 0.1/0.3 | 4.3 | 1.3 | 4.0 | 85 | 1900 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 1800343-11-6
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Molecular Weight 516.62
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Formula C30H29D3FN5O2
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SMILES
CC(C)(O)C(C(F)=C1)=CC(N2[C@@H](C3CCOCC3)C4=CC=CC=C4)=C1C(N=C5)=C2C=C5C(N(N=N6)C)=C6C([2H])([2H])[2H]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BET-IN-12 Related Classifications
HY-150516S Related Classifications
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