BX517(PDK1 inhibitor2)PDK1 inhibitor CAS# 850717-64-5 |
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Quality Control & MSDS
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| Cas No. | 850717-64-5 | SDF | Download SDF |
| PubChem ID | 11161844 | Appearance | Powder |
| Formula | C15H14N4O2 | M.Wt | 282.3 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 27 mg/mL (95.64 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | [(3Z)-2-oxo-3-[1-(1H-pyrrol-2-yl)ethylidene]-1H-indol-5-yl]urea | ||
| SMILES | CC(=C1C2=C(C=CC(=C2)NC(=O)N)NC1=O)C3=CC=CN3 | ||
| Standard InChIKey | DFURSNCTQGJRRX-JYRVWZFOSA-N | ||
| Standard InChI | 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- | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | BX517 is a potent and selective inhibitor of PDK1 with IC50 of 6 nM.In Vitro:BX-517 blocks activation of Akt in tumor cells, is potent with IC50 of 0.1-1.0 μM[1]. BX-517 blocks AKT2 activation in cells with submicromolar potency. BX-517 is 100-fold selective or better against a panel of seven additional Ser/Thr and Tyr kinases[2]. References: | |||||
BX517(PDK1 inhibitor2) Dilution Calculator
BX517(PDK1 inhibitor2) Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.5423 mL | 17.7117 mL | 35.4233 mL | 70.8466 mL | 88.5583 mL |
| 5 mM | 0.7085 mL | 3.5423 mL | 7.0847 mL | 14.1693 mL | 17.7117 mL |
| 10 mM | 0.3542 mL | 1.7712 mL | 3.5423 mL | 7.0847 mL | 8.8558 mL |
| 50 mM | 0.0708 mL | 0.3542 mL | 0.7085 mL | 1.4169 mL | 1.7712 mL |
| 100 mM | 0.0354 mL | 0.1771 mL | 0.3542 mL | 0.7085 mL | 0.8856 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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BX-517 is a potent and selective inhibitor of PDK1 that binds to the ATP binding pocket
of 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-dependent
kinase-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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BX517 is a potent and selective inhibitor of PDK1 with IC50 of 6 nM.
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