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NVS-PAK1-1
🥰Excellent
Catalog No. T16367Cas No. 1783816-74-9
NVS-PAK1-1 is an effective and selective allosteric PAK1 inhibitor (IC50: 5 nM).
NVS-PAK1-1
🥰Excellent
Purity: 99.35%
Catalog No. T16367Cas No. 1783816-74-9
NVS-PAK1-1 is an effective and selective allosteric PAK1 inhibitor (IC50: 5 nM).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $44 | In Stock | |
| 5 mg | $97 | In Stock | |
| 10 mg | $177 | In Stock | |
| 25 mg | $387 | In Stock | |
| 50 mg | $579 | In Stock | |
| 100 mg | $828 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $97 | In Stock |
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Purity:99.35%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | NVS-PAK1-1 is an effective and selective allosteric PAK1 inhibitor (IC50: 5 nM). |
| Targets&IC50 | PAK1:5 nM |
| In vitro | NVS-PAK1-1 inhibits the proliferation of the Su86.86 cell line only above a concentration of 2 μM, consistent with the observation. NVS-PAK1-1 (6-20 μM) inhibits the phosphorylation of the downstream substrate MEK1 Ser289. Inhibition of downstream signaling, by applying a mixture of NVS-PAK1-1 and PAK2 shRNA, and cell proliferation at a significantly lower 0.21 μM concentration is achieved. NVS-PAK1-1 shows high selectivity for inhibition of PAK1 over other PAK isoforms and the kinome in general. NVS-PAK1-1 has a biochemical PAK1 Kd of 7 nM and a PAK2 Kd of 400 nM. NVS-PAK1-1 displays excellent activity in biochemical assays and an exceptional selectivity profile against other known kinases . |
| In vivo | NVS-PAK1-1 displays relatively poor stability in rat liver microsomes (RLM). This would limit its application for in vivo studies (t1/2 in RLM 3.5 min). |
| Molecular Weight | 479.93 |
| Formula | C23H25ClF3N5O |
| Cas No. | 1783816-74-9 |
| Smiles | CC(C)NC(=O)N1CC[C@@H](C1)NC1=Nc2cc(F)ccc2N(CC(F)F)c2ccc(Cl)cc12 |
| Relative Density. | 1.42 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 125 mg/mL (260.45 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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