Antibodies
PD168393
- 貨號 Cat. No.
- S7039
- 規格 Size
- 1mgã€10mM/1mL
- 品牌 Brand
- Selleckchem
Description
PD168393
Catalog No.S7039
PD168393 is an irreveasible EGFR inhibitor with IC50 of 0.70 nM, irreversibly alkylate Cys-773; inactive against insulin, PDGFR, FGFR and PKC.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | PD168393 is an irreveasible EGFR inhibitor with IC50 of 0.70 nM, irreversibly alkylate Cys-773; inactive against insulin, PDGFR, FGFR and PKC. | |||||
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| Targets | EGFR | |||||
| IC50 | 0.70 nM [1] | |||||
| In vitro | PD 168393 is docked into the ATP binding pocket of EGFR TK. PD168393 completely suppresses EGF-dependent receptor autophosphorylation in A431 cells during continuous exposure, with continous suppression even after 8 hr in compound-free medium. PD168393 inhibits heregulin-induced tyrosine phosphorylation in MDA-MB-453 cells with IC50 of 5.7 nM. PD168393 is inactive against insulin, PDGF and basic FGFR TKs as well as PKC. PD168393 inhibits EGF-mediated tyrosine phosphorylation in HS-27 human fibroblasts with IC50 of 1-6 nM but has little effect on FGF- or PDGF-mediated tyrosine phosphorylation. [1]PD168393 shows rapid and potent inhibition of Her2-induced tyrosine phosphorylation with IC50 of ~100 nM in 3T3-Her2 cells. D168393 also inhibits phosphorylation of PLCγ1/Stat1/Dok1/δ-catenin in 3T3-Her2 cells, except for Fyb. [2] | |||||
| In vivo | PD 168393 produces tumor growth inhibition of 115% in A431 human epidermoid carcinoma xenograft in nude mice, with 50% reduced phosphotyrosine content of EGFR. PD 168393 also shows a low plasma concentration. [1] | |||||
| Features | Preclinical compound used in the design of CI-1033. | |||||
Protocol(Only for Reference)
Kinase Assay: [1]
| Enzyme Assays | The enzyme assay is performed in 96-well filte plates. The total volume is 0.1 mL containing 20 mM HEPES, pH 7.4, 50 μM sodium vanadate, 40 mM magnesium chloride, 10 μM ATP containing 0.5 μCi of [32P]ATP, 20 μg of polyglutamic acid/tyrosine, 1 ng of EGF receptor tyrosine kinase, and appropriate dilutions of inhibitor and/or ATP. All components except the ATP are added to the well, and the plate is incubated with shaking for 10 min at 25 °C. The reaction is started by adding [32P]ATP, and the plate is incubated with shaking at 25 °C for 10 min. The reaction is terminated by the addition of 0.1 mL of 20% TCA, and the plate is kept at 4 °C for at least 15 min to allow the substrate to precipitate. The wells are then washed five times with 0.125 mL of 10% TCA, and [32P] incorporation is determined with a Wallac beta plate counter. To assess the type of inhibition, kinetic data are fitted by nonlinear regression computer programs. |
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Animal Study: [1]
| Animal Models | Athymic nude mice with A431 human epidermoid carcinoma |
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| Dosages | 58 mg/kg |
| Administration | i.p. |
| Solubility | 30% PEG400/0.5% Tween80/5% propylene glycol, 10 mg/mL |
References
Chemical Information
| Molecular Weight (MW) | 369.22 |
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| Formula | C17H13BrN4O |
| CAS No. | 194423-15-9 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 74 mg/mL (200 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| In vivo | 30% PEG400/0.5% Tween80/5% propylene glycol, | 10 mg/mL | |
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck 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. | |||
| Chemical Name | 2-Propenamide, N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]- |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
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| Mass(mg) | 0.36922 | 3.6922 | 7.3844 | 11.0766 |
