| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
GSK-1520489A targets PKMYT1 (protein kinase, membrane-associated tyrosine/threonine 1), a kinase involved in cell cycle regulation. PKMYT1 phosphorylates and inhibits CDC2/cyclin B complexes, regulating the G2/M transition of the cell cycle. By inhibiting PKMYT1 with IC50 = 115 nM and Ki = 10.94 nM, GSK-1520489A may promote cell cycle progression and induce cell death in cancer cells.
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| ln Vitro |
Treatment with GSK-1520489A (4 µM, for 24 hours) inhibited Cdk1's phosphorylation of Tyr15 [1].
In vitro, GSK-1520489A inhibits PKMYT1 with IC50 = 115 nM and Ki = 10.94 nM. It is an active PKMYT1 inhibitor. The compound is being developed for the treatment of hematologic malignancies including CLL and MCL. Specific in vitro cell-based data are limited. |
| ln Vivo |
In vivo, GSK-1520489A is being developed for the treatment of hematologic malignancies. Specific in vivo efficacy data are limited in publicly available sources. The compound is under investigation for cancer research applications.
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| Enzyme Assay |
In vitro kinase assays are used to characterize GSK-1520489A's inhibition of PKMYT1. The kinase is incubated with the compound and ATP substrate, and kinase activity is measured by phosphorylation of a peptide substrate. IC50 = 115 nM and Ki = 10.94 nM are determined from dose-response curves.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: HT29 Cell Tested Concentrations: 4 µM Incubation Duration: 24 hrs (hours) Experimental Results: Cdk1 phosphorylation at tyrosine is diminished compared to uninhibited reactions. Cell-based assays for GSK-1520489A are conducted in hematologic malignancy cell lines. Cells are treated with the compound at various concentrations, and cell viability, proliferation, and apoptosis are assessed. Cell cycle analysis is performed by flow cytometry. These assays characterize the compound's anti-cancer activity. |
| Animal Protocol |
In vivo animal experiments with GSK-1520489A are conducted in xenograft models of hematologic malignancies. The compound is administered, and tumor growth inhibition is assessed. PKMYT1 inhibition and downstream signaling are evaluated in tumor tissues. Specific protocols are not extensively documented.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of GSK-1520489A have not been extensively characterized. The compound has molecular weight 425.50 and molecular formula C21H23N5O3S. Storage: appropriately. Specific PK parameters such as half-life, Cmax, and bioavailability have not been reported.
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| Toxicity/Toxicokinetics |
Safety and toxicology data for GSK-1520489A are limited. The compound is for research use only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling the compound. The compound should be stored properly and disposed of in accordance with applicable regulations.
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| References | |
| Additional Infomation |
GSK-1520489A has CAS number 1042433-41-9, molecular formula C21H23N5O3S, and molecular weight 425.50. It is a PKMYT1 inhibitor with IC50 = 115 nM and Ki = 10.94 nM. It is being developed for hematologic malignancies including CLL and MCL. Purity: ≥98%. Not for human use; for research purposes only.
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| Molecular Formula |
C21H23N5O3S
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|---|---|
| Molecular Weight |
425.50
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| Exact Mass |
425.152
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| CAS # |
1042433-41-9
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| PubChem CID |
44526249
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| Appearance |
White to off-white solid powder
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| LogP |
3.3
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
668
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(NC2=NC(NC3=CC(=CC=C3)CS(=O)(C)=O)=NC=C2C)C=CC=CC=1C(=O)NC
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| InChi Key |
AKHLCKMEVWGDGL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H23N5O3S/c1-14-12-23-21(24-16-8-6-7-15(11-16)13-30(3,28)29)26-19(14)25-18-10-5-4-9-17(18)20(27)22-2/h4-12H,13H2,1-3H3,(H,22,27)(H2,23,24,25,26)
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| Chemical Name |
N-methyl-2-[[5-methyl-2-[3-(methylsulfonylmethyl)anilino]pyrimidin-4-yl]amino]benzamide
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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 : ~35.71 mg/mL (~83.92 mM ()
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.89 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 20.8 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 | 2.3502 mL | 11.7509 mL | 23.5018 mL | |
| 5 mM | 0.4700 mL | 2.3502 mL | 4.7004 mL | |
| 10 mM | 0.2350 mL | 1.1751 mL | 2.3502 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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