2. Cell Cycle/DNA Damage
  3. Wee1
  4. 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.

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PKMYT1-IN-9 Chemical Structure

PKMYT1-IN-9 Chemical Structure

CAS No. : 3055031-36-9

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PKMYT1-IN-9 Related Antibodies

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Description

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[1].

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.

PKMYT1-IN-9 Related Antibodies
Parmacokinetics[1]
Species Dose Route Indicator value
Mice 1 mg/kg i.v. CL 43.7 mL/min/kg
Mice 10 mg/kg p.o. AUC0-∞ 1602 ng·h/mL
Mice 1 mg/kg i.v. AUC0-∞ 349.3 ng·h/mL
Mice 10 mg/kg p.o. T1/2 0.77 hr
Mice 1 mg/kg i.v. Vss 0.90 L/kg
Mice 10 mg/kg p.o. Cmax 1923.7 ng/mL
Mice 1 mg/kg i.v. T1/2 0.26 hr
Mice 10 mg/kg p.o. Tmax 0.3 hr
Mice 1 mg/kg i.v. Cmax 898.0 ng/mL
Mice 10 mg/kg p.o. F 45.8 %
Mice 1 mg/kg i.v. Tmax 0.1 hr
In Vivo

PKMYT1-IN-9 (Compound 36) (15 mg/kg, p.o., twice daily for 21 d) can inhibit tumor growth (53%) in NOD-SCID female mice in the HCC1569-derived tumor xenograft (CDX) mouse model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CCNE1-amplified cell line HCC1569-derived tumor xenograft (CDX) mouse model, female NOD-SCID mice (6–8 weeks old; Vital River)[1]
Dosage: 15 mg/kg
Administration: Oral gavage (p.o.), twice daily for 21 d
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%.
Molecular Weight

323.32

Formula

C17H14FN5O
CAS No.
SMILES

O=C1NC2=C(C)C(C)=CN=C2C(C3=CC=C(C4=C3C=NN4)F)=C1N
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PKMYT1-IN-9 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PKMYT1-IN-93055031-36-9Wee1AntitumorHCC1569KYSE30HCC1569 xenograftCDX mouse modelInhibitorinhibitorinhibit

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