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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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PKMYT1 4.4 nM (IC50) |
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.
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.
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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