PKMYT1-IN-9
PKMYT1-IN-9 is a highly selective and orally active PKMYT1 inhibitor (IC50: 4.4 nM). PKMYT1-IN-9 shows more selective for PKMYT1 than WEE1 (IC50: 32.4 μM). PKMYT1-IN-9 exhibits antitumor activity.
For research use only. We do not sell to patients.
- CAS No.: 3055031-36-9
- Formula: C17H14FN5O
- Molecular Weight:323.32
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PKMYT1 4.4 nM (IC50) |
In Vitro
PKMYT1-IN-9 (Compound 36) (7 d) has strong antiproliferative effect on the HCC1569 cell lines (CC50: 0.31 μM) and weak antiproliferative effect on the KYSE30 cell lines (CC50: >30 μM)[1].
PKMYT1-IN-9 inhibits EPHA1 kinase (IC50: 10.1 nM), but is less potent on the other six kinases (ABL1, ABL2, BRAF, CSF1R, LCK, and SRC) (IC50: >60 nM)[1].
PKMYT1-IN-9 is non-GSH-reactive, non-hERG-inhibitory, has low CYP inhibition (<50%), and has high clearance in human and mouse liver microsomes (77.3 mL/min/kg at 1 mg/kg IV)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CCNE1-amplified cell line HCC1569-derived tumor xenograft (CDX) mouse model, female NOD-SCID mice (6–8 weeks old; Vital River)[1]
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Dosage:15 mg/kg
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Administration:Oral gavage (p.o.), twice daily for 21 d
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Result:Inhibited tumor growth (53%).
Slightly reduced the total body weight of mouse (10%).
Shows similar pCDK1 IC50 coverage as RP-6306 over 8 h in vitro.
The quantified tumor CDK1-pT14 level was 52%.
Chemical Information
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CAS No. 3055031-36-9
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Molecular Weight 323.32
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Formula C17H14FN5O
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SMILES
O=C1NC2=C(C)C(C)=CN=C2C(C3=CC=C(C4=C3C=NN4)F)=C1N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PKMYT1-IN-9 Related Classifications
HY-172759 Related Classifications
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