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Borussertib is a first-in-class covalent-allosteric inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Aktwt.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | 128 € | In Stock | |
5 mg | 274 € | In Stock | |
10 mg | 432 € | In Stock | |
25 mg | 715 € | In Stock | |
50 mg | 1.007 € | In Stock | |
100 mg | 1.358 € | In Stock | |
1 mL x 10 mM (in DMSO) | 360 € | In Stock |
Description | Borussertib is a first-in-class covalent-allosteric inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Aktwt. |
Targets&IC50 | Akt (WT):0.8 nM, Akt (WT):2.2 nM (ki) |
In vitro | Borussertib exhibits excellent cellular activity in the nanomolar range with superior profile against clinical candidate Akt inhibitors as well as the cytostatic drug doxorubicin. With the EC50 values are 191±90 nM, 48±15 nM, 5±1 nM, 277±90 nM, 373±54 nM, 7770±641 nM in AN3CA (endometrium), T47D (breast), ZR-75-1 (breast), MCF-7 (breast), BT-474 (breast) and KU-19-19 (bladder) cell lines, respectively[1]. |
Molecular Weight | 596.68 |
Formula | C36H32N6O3 |
Cas No. | 1800070-77-2 |
Smiles | C=CC(=O)Nc1ccc2[nH]c(=O)n(C3CCN(Cc4ccc(cc4)-c4nc5cc[nH]c(=O)c5cc4-c4ccccc4)CC3)c2c1 |
Relative Density. | 1.318 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 25 mg/mL (41.90 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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