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- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
Biological Activity
BX-795 is a potent PDK1 inhibitor that blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induced apoptosis.
Targets
| Target | Value | |
|---|---|---|
| TBK1/IKKε | ||
| PDK-1 | IC50: 6nM | |
| c-Kit | IC50: 320nM | |
| CDK2/CyclinE | IC50: 430nM | |
| Chk1 | IC50: 510nM | |
| GSK-3β | IC50: 620nM | |
| PKA | IC50: 840nM | |
| KDR | IC50: 1.1μM | |
| T-Fyn | IC50: 6.4μM | |
| PKC | IC50: 9.3μM | |
| EGFR | IC50: >10μM | |
| Insulin Receptor | IC50: >10μM |
| In vitro (25°C) | DMSO | 88 mg/mL (148.78 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 2% DMSO+30% PEG +2% Tween 80+ddH2O | 3 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 16.91 mL | 84.53 mL | 169.06 mL |
| 0.5 mM | 3.38 mL | 16.91 mL | 33.81 mL |
| 1 mM | 1.69 mL | 8.45 mL | 16.91 mL |
| 5 mM | 0.34 mL | 1.69 mL | 3.38 mL |
*The above data is based on the productmolecular weight 591.5 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A11148 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 702675-74-9 |
| Formula | C23H26IN7O2S |
| M. Wt | 591.5 |
| Purity | >98% |
| Synonyms | BX795 |
| SMILES | C1CCN(C1)C(=O)NC2=CC=CC(=C2)NC3=NC=C(C(=N3)NCCCNC(=O)C4=CC=CS4)I |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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