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| 25mg |
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Purity: =99.58%
1-Naphthyl PP1 (also known as 1-NA-PP1) 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 |
PKD3 (IC50 = 109.4 nM); PKD2 (IC50 = 133.4 nM); PKD1 (IC50 = 154.6 nM); v-Fyn (IC50 = 0.6 μM); c-Abl (IC50 = 0.6 μM)
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| References |
| Molecular Formula |
C19H19N5
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|---|---|
| Molecular Weight |
317.3877
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| Exact Mass |
317.16404563
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| CAS # |
221243-82-9
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| Related CAS # |
1-Naphthyl PP1 hydrochloride;956025-47-1
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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
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| InChi Key |
XSHQBIXMLULFEV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H19N5/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)
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| Chemical Name |
1-tert-butyl-3-naphthalen-1-ylpyrazolo[3,4-d]pyrimidin-4-amine
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| Synonyms |
1-Naphthyl PP1; 1-NA-PP 1
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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: 9~12.5 mg/mL (28.4~39.4 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.94 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 12.5 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: ≥ 1.25 mg/mL (3.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1507 mL | 15.7535 mL | 31.5070 mL | |
| 5 mM | 0.6301 mL | 3.1507 mL | 6.3014 mL | |
| 10 mM | 0.3151 mL | 1.5753 mL | 3.1507 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.
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