CZC24832Selective PI3K-γ inhibitor CAS# 1159824-67-5 |
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Quality Control & MSDS
3D structure
Package In Stock
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| Cas No. | 1159824-67-5 | SDF | Download SDF |
| PubChem ID | 42623951 | Appearance | Powder |
| Formula | C15H17FN6O2S | M.Wt | 364.4 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 53 mg/mL (145.44 mM) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 5-(2-amino-8-fluoro-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-N-tert-butylpyridine-3-sulfonamide | ||
| SMILES | CC(C)(C)NS(=O)(=O)C1=CN=CC(=C1)C2=CN3C(=NC(=N3)N)C(=C2)F | ||
| Standard InChIKey | RXRZPHQBTHQXSV-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C15H17FN6O2S/c1-15(2,3)21-25(23,24)11-4-9(6-18-7-11)10-5-12(16)13-19-14(17)20-22(13)8-10/h4-8,21H,1-3H3,(H2,17,20) | ||
| 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 | Selective inhibitor of PI 3-kinase γ (IC50 = 1.0 μM in a PI 3-Kγ-dependent fMLP-induced neutrophil migration assay). Exhibits limited off-target effects in kinome profiling of 154 identified lipid and protein kinases and 922 other proteins. Orally effective in a rodent model of inflammatory disease. |
CZC24832 Dilution Calculator
CZC24832 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.7442 mL | 13.7212 mL | 27.4424 mL | 54.8847 mL | 68.6059 mL |
| 5 mM | 0.5488 mL | 2.7442 mL | 5.4885 mL | 10.9769 mL | 13.7212 mL |
| 10 mM | 0.2744 mL | 1.3721 mL | 2.7442 mL | 5.4885 mL | 6.8606 mL |
| 50 mM | 0.0549 mL | 0.2744 mL | 0.5488 mL | 1.0977 mL | 1.3721 mL |
| 100 mM | 0.0274 mL | 0.1372 mL | 0.2744 mL | 0.5488 mL | 0.6861 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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PI3Kγ is one of four class I PI3Ks, a family of dual lipid and protein kinases involved in the regulation of numerous biological processes, such as cell growth, differentiation, survival, proliferation and migration1. A high-throughput chemoproteomics method has benen optimized to enable multiplexed screening resulting in the finding of CZC24832.
In vitro: Plenty of target- and cell-based studies of CZC24832 revealed regulation of interleukin-17–producing T helper cell (TH17) differentiation by PI3Kg, therefore giving selective inhibition of PI3Kg as a potential treatment for inflammatory and autoimmune diseases [1].
In vivo: CZC24832, the first selective inhibitor of phosphoinositide 3-kinase g (PI3Kg), was found to have efficacy in in vivo models of inflammation [1].
Clinical trial: Currenlty no clinical data are available.
Reference:
[1] Bergamini G, Bell K, Shimamura S, Werner T, Cansfield A, Müller K, Perrin J, Rau C, Ellard K, Hopf C, Doce C, Leggate D, Mangano R, Mathieson T, O'Mahony A, Plavec I, Rharbaoui F, Reinhard F, Savitski MM, Ramsden N, Hirsch E, Drewes G, Rausch O, Bantscheff M, Neubauer G. A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation. Nat Chem Biol. 2012;8(6):576-82.
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A selective inhibitor reveals PI3Kgamma dependence of T(H)17 cell differentiation.[Pubmed:22544264]
Nat Chem Biol. 2012 Apr 29;8(6):576-82.
We devised a high-throughput chemoproteomics method that enabled multiplexed screening of 16,000 compounds against native protein and lipid kinases in cell extracts. Optimization of one chemical series resulted in CZC24832, which is to our knowledge the first selective inhibitor of phosphoinositide 3-kinase gamma (PI3Kgamma) with efficacy in in vitro and in vivo models of inflammation. Extensive target- and cell-based profiling of CZC24832 revealed regulation of interleukin-17-producing T helper cell (T(H)17) differentiation by PI3Kgamma, thus reinforcing selective inhibition of PI3Kgamma as a potential treatment for inflammatory and autoimmune diseases.
SAR studies around a series of triazolopyridines as potent and selective PI3Kgamma inhibitors.[Pubmed:22819766]
Bioorg Med Chem Lett. 2012 Aug 15;22(16):5257-63.
Herein we describe the SAR of a novel series of 6-aryl-2-amino-triazolopyridines as potent and selective PI3Kgamma inhibitors. The 6-aryl-triazolopyridine core was identified by chemoproteomic screening of a kinase focused library. Rapid chemical expansion around a bi-functional core identified the key features required for PI3Kgamma activity and selectivity. The series was optimized to afford 43 (CZC19945), a potent PI3Kgamma inhibitor with high oral bioavailability and selectivity over PI3Kalpha and PI3Kdelta. Modification to the core afforded 53 (CZC24832) which showed increased selectivity over the entire kinome in particular over PI3Kbeta.
