PRT062607 acetate
Based on 5 publication(s) in Google Scholar
PRT062607 (P505-15) acetate is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 acetate exerts potent antitumor activity in tumor xenograft mouse models..
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- Pureté : 99.83%
- CAS No.: 1370261-98-5
- Formule: C21H27N9O3
- Masse moléculaire:453.50
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PRT062607 acetate
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Activité biologique
Description
IC50 & Target
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Lck 249 nM (IC50, [2]) |
PAK5 166 nM (IC50, [2]) |
In Vitro
PRT062607 acetate also has significant activity against multiple 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 acetate (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 acetate (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.
In Vivo
PRT062607 acetate (15 mg/kg; po ; bid; 5 d) SYK inhibition in mice prevents Ramos tumor formation in mouse xenograft models[1].
PRT062607 acetate (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.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Research Protocol for Inflammation-related Diseases
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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CAS No. 1370261-98-5
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Appearance Solid
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Masse moléculaire 453.50
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Formule C21H27N9O3
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Color Off-white to light yellow
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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.OC(C)=O
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Synonyms
P505-15 acetate; PRT-2607 acetate; BIIB-057 acetate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (5)
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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 -
Cell Rep
2026 Mar 27;45(4):117183. PMID: 41903135 -
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
Solvant et solubilité
In Vitro:
DMSO : 10 mg/mL (22.05 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (285 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[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 | 1 mM | 2.2051 mL | 11.0254 mL | 22.0507 mL | 55.1268 mL |
| 5 mM | 0.4410 mL | 2.2051 mL | 4.4101 mL | 11.0254 mL | |
| 10 mM | 0.2205 mL | 1.1025 mL | 2.2051 mL | 5.5127 mL | |
| 15 mM | 0.1470 mL | 0.7350 mL | 1.4700 mL | 3.6751 mL | |
| 20 mM | 0.1103 mL | 0.5513 mL | 1.1025 mL | 2.7563 mL |
PRT062607 acetate Related Classifications
HY-15324 Related Classifications
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