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Birabresib
🥰Excellent
Catalog No. T6032Cas No. 202590-98-5
Alias OTX015 （MK 8628/Birabresib）, OTX-015, MK-8628
Birabresib (MK-8628) is a synthetic, small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins 2, 3 and 4 with potential antineoplastic activity.
Birabresib
🥰Excellent
Purity: 99.93%
Catalog No. T6032Alias OTX015 （MK 8628/Birabresib）, OTX-015, MK-8628Cas No. 202590-98-5
Birabresib (MK-8628) is a synthetic, small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins 2, 3 and 4 with potential antineoplastic activity.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $41 | In Stock | |
| 5 mg | $67 | In Stock | |
| 10 mg | $87 | In Stock | |
| 25 mg | $153 | In Stock | |
| 50 mg | $247 | In Stock | |
| 100 mg | $417 | In Stock | |
| 200 mg | $622 | In Stock | |
| 500 mg | $992 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $72 | In Stock |
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Purity:99.93%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | Birabresib (MK-8628) is a synthetic, small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins 2, 3 and 4 with potential antineoplastic activity. |
| Targets&IC50 | BRDs:10-19 nM(EC50) |
| In vitro | Birabresib inhibits the binding of BRD2, BRD3, and BRD4 to AcH4 with IC50 ranging from 92 to 112 nM, and inhibits the growth of a variety of human cancer cell lines with GI50 ranging from 60 to 200 nM. [1] Birabresib results in rapid down-regulation of c-MYC expression, and show the synergistic anti-proliferative effects in combination with ALK inhibitors in ALKpos ALCL cell lines. [2] |
| In vivo | OTX015 (p.o.) significantly inhibits the growth of Ty82 BRD-NUT midline carcinoma tumors in nude mice by 79% at 100 mg/kg qd and 61% at 10 mg/kg bid, respectively. [1] |
| Kinase Assay | |
| Cell Research | Effects of OTX015 on cancer cell proliferation are evaluated by incubating human tumor cells for 72 h with increasing concentrations of OTX015 and assessing proliferation using a tetrazolium salt (WST-8)-based colorimetric assay.(Only for Reference) |
| Alias | OTX015 （MK 8628/Birabresib）, OTX-015, MK-8628 |
| Molecular Weight | 491.99 |
| Formula | C25H22ClN5O2S |
| Cas No. | 202590-98-5 |
| Smiles | CC=1C2=C(N3C([C@H](CC(NC4=CC=C(O)C=C4)=O)N=C2C5=CC=C(Cl)C=C5)=NN=C3C)SC1C |
| Relative Density. | 1.45 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: 9.8 mg/mL (20 mM) DMSO: 45 mg/mL (91.47 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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