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> NVS-PAK1-1 [1783816-74-9]

NVS-PAK1-1 [1783816-74-9]

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Référence HY-100519-10mg

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NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM.

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NVS-PAK1-1 Chemical Structure

NVS-PAK1-1 Chemical Structure

CAS No. : 1783816-74-9

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Based on 1 publication(s) in Google Scholar

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Description

NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM.

IC50 & Target

IC50: 5 nM (PAK1)[1]
In Vitro

NVS-PAK1-1 demonstrates 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 shows excellent activity in biochemical assays and an exceptional selectivity profile against other known kinases. NVS-PAK1-1 at 6-20 μM inhibits the phosphorylation of the downstream substrate MEK1 Ser289. Consistent with the observation, NVS-PAK1-1 inhibits proliferation of Su86.86 cell line only above a concentration of 2 μM. In contrast, by applying a mixture of NVS-PAK1-1 and PAK2 shRNA, inhibition of downstream signaling and cell proliferation at a significantly lower 0.21 μM concentration are achieved[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NVS-PAK1-1 Related Antibodies
In Vivo

NVS-PAK1-1 shows a relatively poor stability in rat liver microsomes (RLM) and this would limit its application for in vivo studies (t1/2 in RLM 3.5 min)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Masse moléculaire

479.93

Formule

C23H25ClF3N5O
CAS No.

1783816-74-9
Appearance

Solid

Color

White to off-white

SMILES

FC1=CC2=C(C=C1)N(CC(F)F)C3=C(C=C(Cl)C=C3)C(N[C@H]4CCN(C(NC(C)C)=O)C4)=N2
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvant et solubilité
In Vitro: 

DMSO : 100 mg/mL (208.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0836 mL 10.4182 mL 20.8364 mL
5 mM 0.4167 mL 2.0836 mL 4.1673 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Calculateur de molarité

  • Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
Références

  • [1]. Karpov AS, et al. Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor. ACS Med Chem Lett. 2015 May 22;6(7):776-81.  [Content Brief]

Essai de kinase
[1]

Inhibition of PAK1 kinase activity is measured using the Caliper assay. The assay is performed using 384-well microtiter plates. Compounds (NVS-PAK1-1) are tested as 8-point dose responses. The assays are prepared by addition of 50 nL of compound solution in 90% DMSO directly into the empty plate. Subsequently, 4.5 µL of the enzyme solution is added to each well and the resulting solution is pre-incubated at 30°C for 60 min, followed by addition of 4.5 µL of the peptide/ATP-solution. After 60 min incubation at 30°C, reactions are terminated by addition of 16 μL per well of the stop solution. Plates with terminated kinase reactions are transferred to the Caliper LC3000 workstations for reading. Product formation is measured in a microfluidic mobility shift assay. IC50 values are derived from percent inhibition values at different compound concentrations by non-linear regression analysis[1].

MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Références

  • [1]. Karpov AS, et al. Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor. ACS Med Chem Lett. 2015 May 22;6(7):776-81.  [Content Brief]

  • [1]. Karpov AS, et al. Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor. ACS Med Chem Lett. 2015 May 22;6(7):776-81.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0836 mL 10.4182 mL 20.8364 mL 52.0909 mL
5 mM 0.4167 mL 2.0836 mL 4.1673 mL 10.4182 mL
10 mM 0.2084 mL 1.0418 mL 2.0836 mL 5.2091 mL
15 mM 0.1389 mL 0.6945 mL 1.3891 mL 3.4727 mL
20 mM 0.1042 mL 0.5209 mL 1.0418 mL 2.6045 mL
25 mM 0.0833 mL 0.4167 mL 0.8335 mL 2.0836 mL
30 mM 0.0695 mL 0.3473 mL 0.6945 mL 1.7364 mL
40 mM 0.0521 mL 0.2605 mL 0.5209 mL 1.3023 mL
50 mM 0.0417 mL 0.2084 mL 0.4167 mL 1.0418 mL
60 mM 0.0347 mL 0.1736 mL 0.3473 mL 0.8682 mL
80 mM 0.0260 mL 0.1302 mL 0.2605 mL 0.6511 mL
100 mM 0.0208 mL 0.1042 mL 0.2084 mL 0.5209 mL
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NVS-PAK1-1 Related Classifications

Help & FAQs

Keywords:

NVS-PAK1-11783816-74-9PAKp21 activated kinasesInhibitorinhibitorinhibit

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