PRT062607 Hydrochloride
Based on 4 publication(s) in Google Scholar
PRT062607 (P505-15) Hydrochloride is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 Hydrochloride exerts potent antitumor activity in tumor xenograft mouse models.
For research use only. We do not sell to patients.
- Purity: 98.07%
- CAS No.: 1370261-97-4
- Formula: C19H24ClN9O
- Molecular Weight:429.91
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PRT062607 Hydrochloride
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Biological Activity
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Lck 249 nM (IC50, [2]) |
PAK5 166 nM (IC50, [2]) |
PRT062607 Hydrochloride also has significant activity against a variety of kinases, with IC50s of 81 nM (Fgr), 88 nM (MLK1), 123 nM (Yes), 139 nM (Flt3), 166 nM (PAK5), 192 nM (Lyn), 244 nM (cSRC), 249 nM (Lck), 108 nM (Pyk), 415 nM (FAK), 1.05 nM (ZAP-70)[1].
PRT062607 Hydrochloride (0.01-2 μM; 3 d) Inhibits Phosphorylation of ERK(Y204), AKT(S473) and SYK(Y352) in Ramos cells, and inhibition of BLNK Tyr84 phosphorylation[1][2].
PRT062607 Hydrochloride (2 μM; 24 h) in SU-DHL6 cells Induces apoptosis in human whole blood[1].
In human whole blood, P505-15 can effectively inhibit B cell antigen receptor-mediated B cell signaling and activation (IC50: 0.27 and 0.28 μM) and Fc receptor 1-mediated induced basophil degranulation (IC50: 0.15 μM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ramos cells[1], SUDHL4 cells[2]
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Concentration:0.01, 0.025, 0.064, 0.16, 0.4, 2.5 μM
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Incubation Time:3 days
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Result:Resulted not entirely concentration-dependent and complete inhibition on ERK (Y204) and AKT (S473) phosphorylation, Lyn phosphorylation of SYK at Y352.
Inhibited BLNK Tyr84 phosphorylation in a concentration dependent manner, while whitout inhibitory effect on Lyn activity.
Potently inhibited BCR-mediated pERK Tyr204 in the Ramos B cell line, without suppressing PMA-mediated pERK Tyr204.
PRT062607 Hydrochloride (15 mg/kg; po ; bid; 5 d) SYK inhibition in mice prevents Ramos tumor formation in mouse xenograft models[1].
PRT062607 Hydrochloride (10-20 mg/kg; po; bid, ) prevents BCR mediated splenomegaly and significantly inhibited NHL tumor growth in xenograft models[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:anti-IgD Stimulated Mouse Inflammation Model[1]
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Dosage:10 mg/kg, 15 mg/kg, 20 mg/kg
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Administration:po; bid for 5 days
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Result:Suppressed mouse B-cell activation following stimulation with this anti-IgD.
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Animal Model:Ramos Tumor Xenograft Model in NOD/SCID mice[1]
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Dosage:15 mg/kg, 30 mg/kg
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Administration:po; bid; terminated when tumor weights began reaching approximately 1.5 mg, at which time tumors were excised and weighed.
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Result:Protected mouse from Ramos tumor growth in vivo.
Chemical Information
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CAS No. 1370261-97-4
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Appearance Solid
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Molecular Weight 429.91
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Formula C19H24ClN9O
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Color Light yellow to khaki
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SMILES
NC(C1=CN=C(N[C@H]2[C@@H](N)CCCC2)N=C1NC3=CC=CC(N4N=CC=N4)=C3)=O.[H]Cl
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Synonyms
P505-15 Hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (4)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Cell Death Dis
Activation of AKT via a dual mechanism enhances the susceptibility of melanoma cells to glucose deprivation. [Abstract]2025 Aug 7;16(1):595. PMID: 40774947 -
Proc Natl Acad Sci U S A
Endocytosis triggers V-ATPase-SYK-mediated priming of cGAS activation and innate immune response. [Abstract]2022 Oct 25;119(43):e2207280119. PMID: 36252040 -
Int J Ophthalmol
NADPH oxidase 2 plays a protective role in experimental Aspergillus fumigatus keratitis in mice through killing fungi and limiting the degree of inflammation. [Abstract]2022 Jul 18;15(7):1044-1052. PMID: 35919314
Solvent & Solubility
H2O : ≥ 50 mg/mL (116.30 mM)
DMSO : ≥ 33 mg/mL (76.76 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (116.30 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Spurgeon SE, et al. The selective SYK inhibitor P505-15 (PRT062607) inhibits B cell signaling and function in vitro and in vivo and augments the activity of fludarabine in chronic lymphocytic leukemia. J Pharmacol Exp Ther. 2013 Feb;344(2):378-87. [Content Brief]
[2]. Coffey G, et al. Specific inhibition of spleen tyrosine kinase suppresses leukocyte immune function and inflammation in animal models of rheumatoid arthritis. J Pharmacol Exp Ther. 2012 Feb;340(2):350-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.3261 mL | 11.6303 mL | 23.2607 mL | 58.1517 mL |
| 5 mM | 0.4652 mL | 2.3261 mL | 4.6521 mL | 11.6303 mL | |
| 10 mM | 0.2326 mL | 1.1630 mL | 2.3261 mL | 5.8152 mL | |
| 15 mM | 0.1551 mL | 0.7754 mL | 1.5507 mL | 3.8768 mL | |
| 20 mM | 0.1163 mL | 0.5815 mL | 1.1630 mL | 2.9076 mL | |
| 25 mM | 0.0930 mL | 0.4652 mL | 0.9304 mL | 2.3261 mL | |
| 30 mM | 0.0775 mL | 0.3877 mL | 0.7754 mL | 1.9384 mL | |
| 40 mM | 0.0582 mL | 0.2908 mL | 0.5815 mL | 1.4538 mL | |
| 50 mM | 0.0465 mL | 0.2326 mL | 0.4652 mL | 1.1630 mL | |
| 60 mM | 0.0388 mL | 0.1938 mL | 0.3877 mL | 0.9692 mL | |
| H2O | 80 mM | 0.0291 mL | 0.1454 mL | 0.2908 mL | 0.7269 mL |
| 100 mM | 0.0233 mL | 0.1163 mL | 0.2326 mL | 0.5815 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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