Antibodies
PRT062607 (P505-15, BIIB057) HCl
- 貨號 Cat. No.
- S8032
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
PRT062607 (P505-15, BIIB057) HCl
Catalog No.S8032
PRT062607 (P505-15) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM, >80-fold selective for Syk than Fgr, Lyn, FAK, Pyk2 and Zap70.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | PRT062607 (P505-15) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM, >80-fold selective for Syk than Fgr, Lyn, FAK, Pyk2 and Zap70. | |||||
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| Targets | Syk | Fgr | MLK1 | |||
| IC50 | 1 nM | 81 nM | 88 nM [1] | |||
| In vitro | PRT062607(P505-15) anti-SYK activity is at least 80-fold greater than its affinity for other kinases. at least 80-fold greater than its affinity for other kinases. PRT062607 potently inhibits B cell antigen receptor-mediated B cell signaling and activation (IC50 0.27 and 0.28 μM, respectively) and Fcε receptor 1-mediated basophil degranulation (IC50 0.15 μM). [1] PRT062607 inhibits BCR-dependent secretion of the chemokines CCL3 and CCL4 by CLL cells, and leukemia cell migration toward the tissue homing chemokines CXCL12, CXCL13, and beneath stromal cells. PRT062607 furthermore inhibits Syk and extracellular signal-regulated kinase phosphorylation after BCR triggering. [2] | |||||
| In vivo | The pharmacokinetic/pharmacodynamic relationship predicted that 70% Syk suppression is maintained in mice over a 24h period after 30 mg/kg dosing. At 15 mg/kg, Syk inhibition ranges from 7.5% (Cmin) to 78.4% (Cmax) with an average inhibition of 67% over 24 h. Oral administration of PRT062607 produced dose-dependent anti-inflammatory activity in two rodent models of rheumatoid arthritis. Statistically significant efficacy is observed at concentrations that specifically suppressed Syk activity by 67%.[1] | |||||
| Features | ||||||
Protocol(Only for Reference)
Kinase Assay: [1]
| fluorescence resonance energy transfer (FRET) assay | The extent of substrate phosphorylation by Syk is measured in the presence of various PRT062607 concentrations. Syk activity is determined by a fluorescent antibody specific for phosphorylated tyrosine by using the increase of FRET. Twelve concentrations are tested for dose response. Specificity and potency of kinase inhibition is determined by evaluation of PRT062607 in the Millipore KinaseProfiler panel of 270 independent purified kinase assays. For profiling, PRT062607 is tested in duplicate at two concentrations at a fixed concentration of ATP. Subsequently, IC50 determinations using the radioactive assays are carried out at an ATP concentration optimized for each individual kinase. All radioactive ATP incorporation enzyme assays are performed at Millipore. |
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Cell Assay: [1]
| Cell lines | Syk-dependent BaF3 cell |
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| Concentrations | ~6 μM |
| Incubation Time | 3 days |
| Method | CellTiter Glo |
Animal Study: [1]
| Animal Models | Mouse Collagen Antibody-Induced Arthritis Model |
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| Dosages | 5, 15, 30 mg/kg, b.i.d. |
| Administration | Oral |
| Solubility | Saline, 30 mg/mL |
References
Chemical Information
Download PRT062607 (P505-15, BIIB057) HCl SDF
| Molecular Weight (MW) | 429.91 |
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| Formula | C19H23N9O.HCl |
| CAS No. | 1370261-97-4 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 86 mg/mL (200 mM) |
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| Water | 86 mg/mL (200 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| In vivo | Saline, | 30 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 | 5-Pyrimidinecarboxamide, 2-[[(1R,2S)-2-aminocyclohexyl]amino]-4-[[3-(2H-1,2,3-triazol-2-yl)phenyl]amino]-, hydrochloride (1:1) |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
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| Mass(mg) | 0.42991 | 4.2991 | 8.5982 | 12.8973 |
