NVS-PAK1-1
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
250mg | $1350 | Check With Us |
500mg | $1950 | Check With Us |
1g | $2925 | Check With Us |
Cat #: V2849 CAS #: 1783816-74-9 Purity ≥ 98%
Description: NVS-PAK1-1 is a a specific allosteric PAK1 inhibitor discovered in a fragment-based screen.
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Molecular Weight (MW) | 479.93 |
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Molecular Formula | C23H25ClF3N5O |
CAS No. | 1783816-74-9 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: ≥125 mg/mLr |
Water: <1 mg/mLr | |
Ethanol: | |
SMILES Code | O=C(N1C[C@@H](NC2=NC3=CC(F)=CC=C3N(CC(F)F)C4=CC=C(Cl)C=C42)CC1)NC(C)C |
Synonyms | NVS-PAK1-1; NVSPAK11; NVS PAK1 1 |
Protocol | 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 |
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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) |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.0836 mL | 10.4182 mL | 20.8364 mL | 41.6727 mL |
5mM | 0.4167 mL | 2.0836 mL | 4.1673 mL | 8.3345 mL |
10mM | 0.2084 mL | 1.0418 mL | 2.0836 mL | 4.1673 mL |
20mM | 0.1042 mL | 0.5209 mL | 1.0418 mL | 2.0836 mL |
The molarity calculator equation
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The dilution calculator equation
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This equation is commonly abbreviated as: C1 V1 = C2 V2
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Step One: Enter information below
Dosage mg/kg
Average weight of animals g
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Number of animals
Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
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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 add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (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.