2. Cell Cycle/DNA Damage
  3. CDK
  4. PKMYT1-IN-13

PKMYT1-IN-13 is a potent, orally active and selective PKMYT1 inhibitor that inhibits PKMYT1 with IC50 values < 10.0 nM in ADP-Glo assay and 19.9 nM in NanoBRET cellular assay. PKMYT1-IN-13 exhibits high selectivity over WEE1. PKMYT1-IN-13 shows selective antiproliferative activity in CCNE1-amplified cells, while showing minimal wild-type effects. PKMYT1-IN-13 shows antitumor efficacy in HCC1569 mouse xenografts. PKMYT1-IN-13 can be used for the research of CCNE1-amplified cancers, such as gastric, ovarian, and breast cancer.

For research use only. We do not sell to patients.

PKMYT1-IN-13

PKMYT1-IN-13 Chemical Structure

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PKMYT1-IN-13 Related Antibodies

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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Description

PKMYT1-IN-13 is a potent, orally active and selective PKMYT1 inhibitor that inhibits PKMYT1 with IC50 values < 10.0 nM in ADP-Glo assay and 19.9 nM in NanoBRET cellular assay. PKMYT1-IN-13 exhibits high selectivity over WEE1. PKMYT1-IN-13 shows selective antiproliferative activity in CCNE1-amplified cells, while showing minimal wild-type effects. PKMYT1-IN-13 shows antitumor efficacy in HCC1569 mouse xenografts. PKMYT1-IN-13 can be used for the research of CCNE1-amplified cancers, such as gastric, ovarian, and breast cancer[1].

IC50 & Target[1]

CDK1

8.7 nM (IC50)

PKMYT1

19.9 nM (IC50)

In Vitro

PKMYT1-IN-13 (compound 20) (7 days) displays potent antiproliferative activity in CCNE1-amplified cell lines (HCC1569, MKN1, OVCAR-3, AsPc-1, SW837, SW1463, and DLD-1 FBXW7-/-) with IC50 values of 29.4, 32.8, 43.5, 83.5, 45.9, 87.8, and 328.5 nM, repectively, while showing minimal effects on their wild-type counterparts (SK-OV-3 cells (IC50= 13672 nM) and DLD-1 parent cells (IC50 > 25000 nM))[1].
PKMYT1-IN-13 (2 h) inhibits the phosphorylation of CDK1 at Thr14 in HCC1569 cells, with an IC50 of 8.7 nM[1].
PKMYT1-IN-13 exhibits favorable safety profiles (low CYP inhibition, time-dependent inhibition (TDI), hERG activity) and high kinase selectivity, achieving a selectivity score of S (10) = 0.03 across a panel of 217 kinases[1].

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

PKMYT1-IN-13 Related Antibodies
Parmacokinetics
Species Dose Route CL Vdss T1/2 AUC0-t Tmax Cmax F AUClast AUCinf
Mice[1] 2 nM i.v. 2.76 mL/min/kg 0.75 L/kg 8.05 h 11528 ng·h/mL / / / / /
Mice[1] 10 nM p.o. / / / 25763 ng·h/mL 0.42 h 16580 ng/mL 43.0 % / /
Rat[1] 1 nM i.v. 7.24 mL/min/kg 0.53 L/kg 2.06 h 2278 ng·h/mL / / / / /
Rat[1] 10 nM p.o. / / / 6826 ng·h/mL 0.25 h 3924 ng/mL 30 % / /
Dog[1] 1 nM i.v. 8.09 mL/min/kg 2.00 L/kg 4.30 h 2053 ng·h/mL / / / / /
Dog[1] 4 nM p.o. / / / 3416 ng·h/mL 0.67 h 709 ng/mL 47.6 % / /
Rat[1] 100 nM p.o. / / / / 0.25 h 3899 ng/mL / 25765 ng·h/mL 26901 ng·h/mL
Rat[1] 30 nM p.o. / / / / / 1104 ng/mL 14 % 9780 ng·h/mL 9858 ng·h/mL
Rat[1] 200 nM p.o. / / / / / 2721 ng/mL 5 % 24783 ng·h/mL 27136 ng·h/mL
In Vivo

PKMYT1-IN-13 (compound 20) (10 and 20 mg/kg; p.o.; twice daily for 26 days) exhibits dose-dependent antitumor efficacy in the HCC1569 xenograft mouse model[1].

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

Animal Model: Female NOD-SCID (6-8 weeks old) subcutaneoously implanted with HCC1569 cells[1]
Dosage: 10; 20 mg/kg
Administration: p.o.; twice daily for 26 days
Result: Induced dose-dependent tumor growth inhibition (TGI) with 66% TGI at 10 mg/kg and 86% TGI at 20 mg/kg.
Showed sustained inhibition of pCDK1(T14) over 24 hours postdose.
Maintained unbound plasma concentrations above the pCDK1(T14) IC90 threshold for most of the dosing interval.
Was tolerated at both dose levels, with a mean body weight loss of 8%.
Molecular Weight

424.45

Formula

C24H20N6O2
SMILES

N#CC1=C(CNC2=O)C(C3=C4C2=C(N)[N@@]([C@@]5=C(C)C=CC(O)=C5C)C4=NC(C)=N3)=CC=C1
Shipping

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-13 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-13CDKCyclin dependent kinaseCDK1 pThr14NOD-SCID miceWEE1HCC1569 xenograftsCCNE1-amplified cellsCCNE1-amplified cancersHCC1569 mouse xenograftgastric cancerbreast cancerovarian cancerInhibitorinhibitorinhibit

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