1-Naphthyl PP1 (Synonyms: 1NaphthylPP1, PP1 Analog) |
رقم الكتالوجGC12172 |
1-Naphthyl PP1 (1-NA-PP 1) هو مثبط انتقائي لأنازات عائلة src1-Naphthyl PP1 يثبط v-Src و c-Fyn و c-Abl و CDK2 و CAMK II مع IC50s 1.0 و 0.6 و 0.6 و 18 و 22 ميكرومتر على التوالي
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Cas No.: 221243-82-9
Sample solution is provided at 25 µL, 10mM.
1-Naphthyl PP1(1-NA-PP 1) is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively).IC50 Value:1.0 uM (v-Src); 0.6 uM (c-Fyn); 18 uM (c-Abl) [1]Target: Src Family kinase1-NA-PP1 was considerably more potent and showed distinct substituent effects at the pyrazolopyrimidine core. 1-NA-PP1 was cell-active, and potently blocked prostate cancer cell proliferation by inducing G2/M arrest. Overexpression of PKD1 or PKD3 almost completely reversed the growth arrest and the inhibition of tumor cell invasion caused by 1-NA-PP1, indicating that its anti-proliferative and anti-invasive activities were mediated through the inhibition of PKD. Interestingly, a 12-fold increase in sensitivity to 1-NA-PP1 could be achieved by engineering a gatekeeper mutation in the active site of PKD1, suggesting that 1-NA-PP1 could be paired with the analog-sensitive PKD1(M659G) for dissecting PKD-specific functions and signaling pathways in various biological systems [2].
References:
[1]. Bishop AC, et al. A chemical switch for inhibitor-sensitive alleles of any protein kinase. Nature. 2000 Sep 21;407(6802):395-401.
[2]. Tandon M, et al. New pyrazolopyrimidine inhibitors of protein kinase d as potent anticancer agents for prostate cancer cells. PLoS One. 2013 Sep 23;8(9):e75601.
Cas No. | 221243-82-9 | SDF | |
المرادفات | 1NaphthylPP1, PP1 Analog | ||
Chemical Name | 1-tert-butyl-3-naphthalen-1-ylpyrazolo[3,4-d]pyrimidin-4-amine | ||
Canonical SMILES | CC(C)(C)N1C2=C(C(=N1)C3=CC=CC4=CC=CC=C43)C(=NC=N2)N | ||
Formula | C19H19N5 | M.Wt | 317.39 |
الذوبان | DMF: 30 mg/ml,DMF:PBS (pH 7.2) (1:5): 0.15 mg/ml,DMSO: 1 mg/ml,Ethanol: 2 mg/ml | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 3.1507 mL | 15.7535 mL | 31.507 mL |
5 mM | 0.6301 mL | 3.1507 mL | 6.3014 mL |
10 mM | 0.3151 mL | 1.5753 mL | 3.1507 mL |
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5
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