[CAS NO. 1370261-97-4] PRT062607Hydrochloride
PRODUCTS SPECIFICATIONS [1370261-97-4]
DESCRIPTION [1370261-97-4]
Overview
| MDL | MFCD25976708 |
|---|---|
| Molecular Weight | 429.91 |
| Molecular Formula | C19H24ClN9O |
| SMILES | NC(C1=CN=C(N[C@H]2[C@@H](N)CCCC2)N=C1NC3=CC=CC(N4N=CC=N4)=C3)=O.[H]Cl |
3 Publications Citing Use of MCE
Summary
PRT062607 Hydrochloride (P505-15 Hydrochloride) is a highly specific and potent inhibitor of purified Syk ( IC 50 1-2 nM).
IC50 & Target
IC50: 1 nM (Syk), 81 nM (Fgr), 88 nM (MLK1), 123 nM (Yes) [1]
In Vitro
PRT062607 (P505-15) is a novel, highly specific, and potent orally available small-molecule inhibitor of Syk. The potency of PRT062607 against its target kinase Syk is initially tested in two different purified kinase assays. Using a FRET assay, half-maximal Syk inhibition required 6±0.2 nM (mean±S.E.M.). Similar potency is observed when tested in a radioactive enzyme assay, with a resulting Syk IC 50 of 2.1±0.4 nM (mean±S.E.M.). In human whole blood, PRT062607 potently inhibits B cell antigen receptor-mediated B cell signaling and activation (IC 50 0.27 and 0.28 μM, respectively) and Fcε receptor 1-mediated basophil degranulation (IC 50 0.15 μM) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
In the mouse CAIA model, oral administration of PRT062607 (P505-15) results in an average inhibition of paw inflammation, as measured by daily scoring of inflammation compared with vehicle controls, of 12, 44, and 87% with average plasma concentration (C average over 24 h) assessed at the end of the study of 0.38, 0.95, and 1.47 μM, respectively. In mice treated with 30 mg/kg PRT062607, the damage to the joints is significantly reduced and seemed indistinguishable from normal mice. In the rat CIA model, the high dose of PRT062607 (15 mg/kg b.i.d.) completely suppresses inflammation in a majority of the animals (seven of eight), by the end of the study (mean inflammation score±S.E.M.=0.63±1.1; p<0.0001 versus vehicle) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01652937 | Biogen |
Rheumatoid Arthritis
|
August 2012 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : ≥ 50 mg/mL ( 116.30 mM )
DMSO : ≥ 33 mg/mL ( 76.76 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3261 mL | 11.6303 mL | 23.2607 mL |
| 5 mM | 0.4652 mL | 2.3261 mL | 4.6521 mL |
| 10 mM | 0.2326 mL | 1.1630 mL | 2.3261 mL |
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1.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (116.30 mM); Clear solution; Need ultrasonic
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2.
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3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution
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4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution
Synonyms