| Identification | Back Directory | [Name]
PDK1 Inhibitor | [CAS]
850717-64-5 | [Synonyms]
BX-517
CS-1693
BX-517;BX 517
PDK1 Inhibitor 2
PDK1 Inhibitor II
BX517(PDK1 inhibitor2)
5-Ureido-3-[1-(pyrrol-2-yl)ethylidene]indolin-2-one
Urea, [2,3-dihydro-2-oxo-3-[1-(1H-pyrrol-2-yl)ethylidene]-1H-indol-5-yl]-
Urea, N-[2,3-dihydro-2-oxo-3-[1-(1H-pyrrol-2-yl)ethylidene]-1H-indol-5-yl]- | [Molecular Formula]
C15H14N4O2 | [MDL Number]
MFCD28044315 | [MOL File]
850717-64-5.mol | [Molecular Weight]
282.3 |
| Chemical Properties | Back Directory | [Boiling point ]
572.431±50.00 °C(Press: 760.00 Torr)(predicted) | [density ]
1.431±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; insoluble in EtOH; ≥8.55 mg/mL in DMSO | [form ]
solid | [pka]
12.818±0.20(predicted) | [color ]
Light yellow to khaki | [InChI]
1S/C15H14N4O2/c1-8(11-3-2-6-17-11)13-10-7-9(18-15(16)21)4-5-12(10)19-14(13)20/h2-7,17H,1H3,(H,19,20)(H3,16,18,21)/b13-8- | [InChIKey]
DFURSNCTQGJRRX-JYRVWZFOSA-N |
| Hazard Information | Back Directory | [Uses]
BX-517 is a potent and selective inhibitor of PDK1 that binds to the ATP binding pocket of the protein (IC50 = 6 nM). | [Biological Activity]
bx-517 is a potent and selective inhibitor of pdk1 that binds to the atp binding pocketof the protein (ic50 = 6 nm). bx-517 also blocks activation of akt in tumor cells with 10-fold more potent (ic50 = 0.1–1.0 μm) than its analogs tested at the highest dose tested (10 μm). [1] the phosphoinositide-dependent kinase-1 (pdk1) is a ser/thr kinase that is a crucial activator of a range of protein kinases in the agc kinase super-family that play key roles in the progression of cancer and for the activation of akt, s6 kinase, and protein kinase c. [2] | [References]
1. islam i, brown g, bryant j et al. indolinone based phosphoinositide-dependentkinase-1 (pdk1) inhibitors. part 2: optimization of bx-517. bioorg med chem lett.2007 jul 15;17(14):3819-25. 2. islam i, bryant j, chou yl etc. indolinone based phosphoinositide-dependent kinase-1 (pdk1)inhibitors. part 1: design, synthesis and biological activity. bioorg med chem lett. 2007 jul 15;17(14):3814-8. |
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| Company Name: |
Struchem Co., Ltd.
|
| Telephone: |
0512-63009836 18994340901 |
| Website: |
http://www.beidapharma.com |
| Company Name: |
Tcichem, Inc.
|
| Telephone: |
13918644899 |
| Website: |
https://www.chemicalbook.com/ShowSupplierProductsList19113/0_EN.htm |
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