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1mg |
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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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Purity: ≥98%
1-Naphthyl PP1 HCl (also known as 1-NA-PP1 hydrochloride) is a novel, potent and selective ATP-competitive inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl with IC50 values of 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively. Compared with IKK-16, 1-NA-PP1 demonstrated a high degree of selectivity for PKD, according to analysis of several related kinases. The pyrazolopyrimidine core exhibited distinct substituent effects, and 1-NA-PP1 was found to be significantly more potent based on SAR analysis. 1. Because it induced G2/M arrest, cell-active NA-PP1 effectively inhibited the proliferation of prostate cancer cells. Furthermore, it showed promising multimodal anticancer activities by potently inhibiting the migration and invasion of prostate cancer cells. The growth arrest and inhibition of tumor cell invasion induced by 1-NA-PP1 were nearly entirely reversed by overexpressing PKD1 or PKD3, suggesting that the anti-proliferative and anti-invasive properties of the compound were mediated through the inhibition of PKD. Interestingly, engineering a gatekeeper mutation in PKD1's active site could increase sensitivity to 1-NA-PP1 by a factor of 12, indicating that 1-NA-PP1 and the analog-sensitive PKD1(M659G) could be used together to analyze PKD-specific roles and signaling pathways in diverse biological systems.
Targets |
c-Fyn (IC50 = 0.035 nM); c-Abl (IC50 = 0.6 μM); v-Src (IC50 = 1.0 μM); CDK2 (IC50 = 18 μM); CAMKII (IC50 = 22 μM)
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References |
Molecular Formula |
C19H20CLN5
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Molecular Weight |
353.8486
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Exact Mass |
353.14
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Elemental Analysis |
C, 64.49; H, 5.70; Cl, 10.02; N, 19.79
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CAS # |
956025-47-1
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Related CAS # |
1-Naphthyl PP1;221243-82-9
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Appearance |
Solid
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SMILES |
CC(C)(C)N1C2=NC=NC(=C2C(=N1)C3=CC=CC4=CC=CC=C43)N.Cl
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InChi Key |
UKLRSYUALPIALU-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C19H19N5.ClH/c1-19(2,3)24-18-15(17(20)21-11-22-18)16(23-24)14-10-6-8-12-7-4-5-9-13(12)14;/h4-11H,1-3H3,(H2,20,21,22);1H
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Chemical Name |
1-tert-butyl-3-naphthalen-1-ylpyrazolo[3,4-d]pyrimidin-4-amine;hydrochloride
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Synonyms |
1-NA-PP 1 hydrochloride; 1-Naphthyl PP1 hydrochloride; 1-Naphthyl PP1 (hydrochloride)
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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) |
DMSO: ~71 mg/mL (~200.7 mM)
Ethanol: ~71 mg/mL (~200.7 mM) |
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.8261 mL | 14.1303 mL | 28.2606 mL | |
5 mM | 0.5652 mL | 2.8261 mL | 5.6521 mL | |
10 mM | 0.2826 mL | 1.4130 mL | 2.8261 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.
Synthesis and SAR analysis of 1-NA-PP1 analogs.PLoS One.2013 Sep 23;8(9):e75601. th> |
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1-NA-PP1 did not inhibit PKC and CAMK.PLoS One.2013 Sep 23;8(9):e75601. td> |
Inhibition of PKD isoforms by 1-NA-PP1 and IKK-16. IKK-16 and 1-NA-PP1 were ATP-competitive inhibitors of PKD.PLoS One.2013 Sep 23;8(9):e75601. td> |