BX912
BX912 is a selective potent PDK1 inhibitor with IC50 of 12 nM. BX912 blocks PDK1/Akt signaling in tumor cells and suppresses the anchorage-dependent growth of a variety of tumor cell lines (such as PC-3 cells) in culture or induces apoptosis.
1: Mashukova A, Forteza R, Wald FA, Salas PJ. PDK1 in apical signaling endosomes participates in the rescue of the polarity complex atypical PKC by intermediate filaments in intestinal epithelia. Mol Biol Cell. 2012 May;23(9):1664-74. Epub 2012 Mar 7. PubMed PMID: 22398726; PubMed Central PMCID: PMC3338434.
| Chemical | |
|---|---|
| CAS Num | 702674-56-4 |
| Chemical Formula | C20H23BrN8O |
| Molecular Weight | 471.35 |
| IUPAC Chemical Name | N-(3-((4-((2-(1H-imidazol-4-yl)ethyl)amino)-5-bromopyrimidin-2-yl)amino)phenyl)pyrrolidine-1-carboxamide |
| Exact Mass | 470.11782 |
| Elemental Analysis | C, 50.96; H, 4.92; Br, 16.95; N, 23.77; O, 3.39 |
| Synonym | BX912; BX 912; BX912. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | O=C(N1CCCC1)NC2=CC=CC(NC3=NC=C(Br)C(NCCC4=CNC=N4)=N3)=C2 |
| Biological | |
| Targets and Effects | PDK1 inhibitor. |
| Pathways | Apoptosis |
| Physical | |
| Appearance | White solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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