| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
WZ4003 is a novel, potent and highly specific inhibitor of NUAK kinases. It exhibits little inhibition against 139 other kinases but inhibits NUAK1 and NUAK2 with IC50s of 20 nM and 100 nM in cell-base assays.
| Targets |
NUAK1 (IC50 = 20 nM); NUAK2 (IC50 = 100 nM)
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|---|---|
| ln Vitro |
WZ4003 (3–10 μM) significantly reduces MYPT1 phosphorylation caused by NUAK1 in HEK-293 cells that are overexpressing wild-type NUAK1. Furthermore, WZ4003 (10 μM) inhibits MYPT1 Ser445 phosphorylation as well as cell migration, invasion, and proliferation to a similar extent as NUAK1 knockout in MEFs or knockdown in U2OS cells.[1] While having a significantly lower cellular IC50 against T790M-containing Ba/F3 cells, WZ4003 also shows a high, specific affinity to the L858R/T790M mutant EGFR. [2]
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| ln Vivo |
NA
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| Enzyme Assay |
The reactions take place in a 50 μL reaction volume for 30 min at 30°C, and they are stopped by sprinkling 40 μL of the reaction mix onto P81 paper and then immediately submerging it in 50 mM orthophosphoric acid. Three 50 mM orthophosphoric acid washings are performed on the samples, followed by one acetone rinse and air drying. Cerenkov counting is used to measure the [γ-32P]ATP incorporation into Sakamototide caused by kinases. One unit of activity is the amount of time it took to catalyze the incorporation of 1 nmol of [32P]phosphate into the substrate over the course of one hour.
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| Cell Assay |
In 96-well plates, colorimetric cell proliferation assays are conducted. U2OS cells and MEFs are initially seeded with 2000 and 3000 cells, respectively, per well. Over the course of five days, the proliferation assays are performed with or without 10 M HTH-01-015 or WZ4003.
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| Animal Protocol |
NA;
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| References |
| Molecular Formula |
C25H29CLN6O3
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|---|---|
| Molecular Weight |
496.9892
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| Exact Mass |
496.199
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| Elemental Analysis |
C, 60.42; H, 5.88; Cl, 7.13; N, 16.91; O, 9.66
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| CAS # |
1214265-58-3
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| Related CAS # |
1214265-58-3
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| Appearance |
White to beige solid powder
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| SMILES |
CCC(=O)NC1=CC(=CC=C1)OC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCN(CC4)C)OC
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| InChi Key |
SDGJBAUIGHSMRI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H29ClN6O3/c1-4-23(33)28-17-6-5-7-19(14-17)35-24-20(26)16-27-25(30-24)29-21-9-8-18(15-22(21)34-3)32-12-10-31(2)11-13-32/h5-9,14-16H,4,10-13H2,1-3H3,(H,28,33)(H,27,29,30)
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| Chemical Name |
N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]propanamide
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| Synonyms |
WZ 4003; WZ4003; WZ-4003
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| HS Tariff Code |
2934.99.9001
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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: ~7 mg/mL (~14.1 mM)
Water: <1 mg/mL Ethanol: <1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.03 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.03 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 25.0 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 | 2.0121 mL | 10.0606 mL | 20.1211 mL | |
| 5 mM | 0.4024 mL | 2.0121 mL | 4.0242 mL | |
| 10 mM | 0.2012 mL | 1.0061 mL | 2.0121 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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