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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
PP1 (known also as EI275; EI-275; PP-1; PP 1; AG1872; AG-1872) is a novel, potent and selective Src kinase inhibitor with potential antitumor activity. It inhibits Lck/Fyn kinases with IC50 of 5 nM/6 nM. It exhibits excellent anti-proliferative activity in vitro and high in vivo antitumor efficacy.
ln Vitro |
In vitro, PP1 exhibits much lower doses of inhibition against Lck (IC50=5 nM) and FynT (IC50=6 nM) than against ZAP-70 (IC50>100 μM), JAK2 (IC50>50 μM), EGFR, and protein A. In human T cells, PP1 inhibits the production of the IL-2R gene and GM-CSF-induced IL-2 gene [1].
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ln Vivo |
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Animal Protocol |
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References |
[1]. Hanke JH, et al. Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation. J Biol Chem. 1996 Jan 12;271(2):695-701
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Molecular Formula |
C16H19N5
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Molecular Weight |
281.36
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CAS # |
172889-26-8
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Related CAS # |
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SMILES |
NC1=C2C(N(C(C)(C)C)N=C2C3=CC=C(C)C=C3)=NC=N1
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (5.94 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (5.94 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.67 mg/mL (5.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.5542 mL | 17.7708 mL | 35.5417 mL | |
5 mM | 0.7108 mL | 3.5542 mL | 7.1083 mL | |
10 mM | 0.3554 mL | 1.7771 mL | 3.5542 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT03666715 | Completed | Drug: Oral Antipsychotics (OAPs) Drug: Paliperidone Palmitate 1-Month Formulation (PP1M) |
Schizophrenia | Janssen-Cilag Farmaceutica Ltda. | August 7, 2018 | |
NCT00791843 | Completed Has Results | Drug: Growth hormone releasing hormone/ placebo |
Congestive Heart Failure | University of Pennsylvania | March 2004 | Phase 2 |
NCT03713658 | Completed | Drug: Risperidone 3 mg Drug: Paliperidone Palmitate 50 mg eq. |
Schizophrenia | Janssen Research & Development, LLC | October 18, 2018 | Phase 4 |
NCT03345342 | Completed Has Results | Drug: PP6M Drug: PP3M 350 mg eq. |
Schizophrenia | Janssen Research & Development, LLC | November 20, 2017 | Phase 3 |