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PKMYT1-IN-9
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Catalog No. T206301Cas No. 3055031-36-9
PKMYT1-IN-9 is a highly selective, orally active inhibitor of PKMYT1 with an IC50 of 4.4 nM. It exhibits greater selectivity for PKMYT1 compared to WEE1, for which the IC50 is 32.4 μM. Additionally, PKMYT1-IN-9 demonstrates antitumor activity.
PKMYT1-IN-9
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Catalog No. T206301Cas No. 3055031-36-9
PKMYT1-IN-9 is a highly selective, orally active inhibitor of PKMYT1 with an IC50 of 4.4 nM. It exhibits greater selectivity for PKMYT1 compared to WEE1, for which the IC50 is 32.4 μM. Additionally, PKMYT1-IN-9 demonstrates antitumor activity.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | PKMYT1-IN-9 is a highly selective, orally active inhibitor of PKMYT1 with an IC50 of 4.4 nM. It exhibits greater selectivity for PKMYT1 compared to WEE1, for which the IC50 is 32.4 μM. Additionally, PKMYT1-IN-9 demonstrates antitumor activity. |
| Targets&IC50 | PKMYT1:4.4 nM |
| In vitro | PKMYT1-IN-9 (Compound 36) exhibits a significant antiproliferative effect on the HCC1569 cell line (CC50: 0.31 μM), but a weaker effect on the KYSE30 cell line (CC50: >30 μM). It strongly inhibits the EPHA1 kinase (IC50: 10.1 nM), while showing much lower efficacy against six other kinases (ABL1, ABL2, BRAF, CSF1R, LCK, and SRC) with an IC50 of >60 nM. Additionally, PKMYT1-IN-9 has no reaction with GSH, does not inhibit hERG, and shows a low inhibition rate on CYP enzymes (<50%). It also demonstrates a high clearance rate in human and mouse liver microsomes (77.3 mL/min/kg at 1 mg/kg IV). |
| In vivo | PKMYT1-IN-9 (Compound 36) administered at 15 mg/kg orally twice daily for 21 days effectively inhibits tumor growth by 53% in female NOD-SCID mice carrying xenografts derived from HCC1569 tumors (CDX model). |
| Molecular Weight | 323.324 |
| Formula | C17H14FN5O |
| Cas No. | 3055031-36-9 |
| Smiles | O=C1NC=2C(=NC=C(C2C)C)C(=C1N)C3=CC=C(F)C=4NN=CC34 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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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 stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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