Cat. No.: HY-187562

PKMYT1-IN-15

PKMYT1-IN-15 is an orally active PKMYT1 inhibitor with an IC₅₀ of 6.02 nM. PKMYT1-IN-15 inhibits the phosphorylation of CDK1 at Thr14. As an antiproliferative agent, DNA damage inducer and antitumor agent, PKMYT1-IN-15 triggers replication-associated DNA damage and cell death in CCNE1-amplified cancer cells, and suppresses tumor growth in the OVCAR3 xenograft model. PKMYT1-IN-15 can be used for the research of CCNE1-amplified cancers (e.g., ovarian cancer, breast cancer).

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

Formula: C₁₈H₁₇F₃N₄O₃
Molecular Weight:394.35

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

PKMYT1-IN-15 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

PKMYT1

6.02 nM (IC₅₀)

CDK1

All Wee1 Isoforms :

PKMYT1

All CDK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
OVCAR-3	IC50	90.52 nM	Antiproliferative activity against human CCNE1-amplified OVCAR3 ovarian cancer cells assessed as reduction in cell proliferation incubated for 7 days by CTG assay. Antiproliferative activity against human CCNE1-amplified OVCAR3 ovarian cancer cells assessed as reduction in cell proliferation incubated for 7 days by CTG assay.	42526071
HCC1569	IC50	43.8 nM	Antiproliferative activity against human CCNE1-amplified HCC1569 breast cancer cells assessed as reduction in cell proliferation incubated for 7 days by CTG assay. Antiproliferative activity against human CCNE1-amplified HCC1569 breast cancer cells assessed as reduction in cell proliferation incubated for 7 days by CTG assay.	42526071
HCC1954	IC50	687.4 nM	Antiproliferative activity against human non-CCNE1-amplified HCC1954 cancer cells assessed as reduction in cell proliferation incubated for 7 days by CTG assay. Antiproliferative activity against human non-CCNE1-amplified HCC1954 cancer cells assessed as reduction in cell proliferation incubated for 7 days by CTG assay.	42526071
ZR-75-1	IC50	8489 nM	Antiproliferative activity against human non-CCNE1-amplified ZR-75-1 cancer cells assessed as reduction in cell proliferation incubated for 7 days by CTG assay. Antiproliferative activity against human non-CCNE1-amplified ZR-75-1 cancer cells assessed as reduction in cell proliferation incubated for 7 days by CTG assay.	42526071
SK-OV-3	IC50	676.4 nM	Antiproliferative activity against human non-CCNE1-amplified SK-OV-3 cancer cells assessed as reduction in cell proliferation incubated for 7 days by CTG assay. Antiproliferative activity against human non-CCNE1-amplified SK-OV-3 cancer cells assessed as reduction in cell proliferation incubated for 7 days by CTG assay.	42526071
HEK-293T	IC50	18.97 nM	Cellular PKMYT1 target engagement in human HEK-293T cells transfected with NanoLuc-PKMYT1 plasmid, measured via NanoBRET assay after 2 h incubation with compound and tracer K-10. Cellular PKMYT1 target engagement in human HEK-293T cells transfected with NanoLuc-PKMYT1 plasmid, measured via NanoBRET assay after 2 h incubation with compound and tracer K-10.	42526071
HEK-293T	IC50	1290.75 nM	Cellular WEE1 target engagement in human HEK-293T cells transfected with NanoLuc-WEE1 plasmid, measured via NanoBRET assay after 2 h incubation with compound and tracer. Cellular WEE1 target engagement in human HEK-293T cells transfected with NanoLuc-WEE1 plasmid, measured via NanoBRET assay after 2 h incubation with compound and tracer.	42526071
OVCAR-3	IC50	23.5 nM	Inhibition of CDK1 Thr14 phosphorylation in human OVCAR3 ovarian cancer cells, measured via AlphaLISA assay after 2 h incubation with compound. Inhibition of CDK1 Thr14 phosphorylation in human OVCAR3 ovarian cancer cells, measured via AlphaLISA assay after 2 h incubation with compound.	42526071
OVCAR-3	IC50	3973 nM	Inhibition of CDK1 Tyr15 phosphorylation in human OVCAR3 ovarian cancer cells, measured via AlphaLISA assay after 2 h incubation with compound. Inhibition of CDK1 Tyr15 phosphorylation in human OVCAR3 ovarian cancer cells, measured via AlphaLISA assay after 2 h incubation with compound.	42526071

In Vitro

PKMYT1-IN-15 (0-10000 nM; 7 days) potently inhibits the proliferation of CCNE1-amplified OVCAR3 and HCC1569 cells, with IC₅₀ values of 90.52 nM and 43.8 nM, respectively^[1].
PKMYT1-IN-15 (0-10000 nM; 7 days) inhibits the proliferation of non-CCNE1-amplified HCC1954, ZR-75-1 and SK-OV-3 cancer cells, with IC₅₀ values of 687.4 nM, 8489 nM and 676.4 nM, respectively, and exhibits reduced potency compared with CCNE1-amplified cell lines^[1].
PKMYT1-IN-15 (0-2 μM; 8 h) induces replication-associated DNA damage in OVCAR3 cells, with γH2AX levels increasing in a dose-dependent and time-dependent manner^[1].
PKMYT1-IN-15 (0.61-10000 nM; 2 h) selectively inhibits CDK1 Thr14 phosphorylation in OVCAR3 cells with an IC₅₀ of 23.5 nM, while its IC₅₀ for inhibiting CDK1 Tyr15 phosphorylation is 3973 nM^[1].
PKMYT1-IN-15 (6-A) inhibits purified recombinant WEE1 protein with an IC₅₀ of 286.3 nM, and exhibits selectivity over its inhibitory activity against PKMYT1^[1].
PKMYT1-IN-15 (2 h) binds to intracellular WEE1 in HEK-293T cells with an IC₅₀ of 1290.75 nM, exhibiting selective target-binding activity towards PKMYT1^[1].
PKMYT1-IN-15 (2 h) binds to intracellular PKMYT1 in HEK-293T cells, with an IC₅₀ of 18.97 nM^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

CCNE1-amplified OVCAR3, HCC1569 cells
Concentration:

10000
nM, 3333.33 nM, 1111.11 nM, 370.37 nM, 123.46 nM, 41.15 nM, 13.72
nM, 4.57 nM, 1.52 nM, 0.51 nM, and 0 nM
Incubation Time:

7 days
Result:

Potently inhibited OVCAR3 cell proliferation with an IC₅₀ of 90.52 nM.
Potently inhibited HCC1569 cell proliferation with an IC50 of 43.8 nM.

Cell Proliferation Assay^[1]

Cell Line:

Non-CCNE1-amplified HCC1954, ZR-75-1, SK-OV-3 cancer cells
Concentration:

10000
nM, 3333.33 nM, 1111.11 nM, 370.37 nM, 123.46 nM, 41.15 nM, 13.72
nM, 4.57 nM, 1.52 nM, 0.51 nM, and 0 nM
Incubation Time:

7 days
Result:

Inhibited proliferation of HCC1954 cells with an IC₅₀ of 687.4 nM.
Inhibited proliferation of ZR-75-1 cells with an IC₅₀ of 8489 nM.
Inhibited proliferation of SK-OV-3 cells with an IC₅₀ of 676.4 nM.
Showed reduced potency relative to CCNE1-amplified cell lines.

Western Blot Analysis^[1]

Cell Line:

OVCAR3 cells
Concentration:

0, 0.1, 0.25, 0.5, 1, 2 μM (8 h incubation); 2 μM (time-course incubation)
Incubation Time:

8 h (dose-response); 0, 0.5. 1, 2, 4, 8, 16, 24 h (time-course)
Result:

Induced a dose-dependent increase in γH2AX levels, indicating replication-associated DNA damage.
Induced a time-dependent increase in γH2AX levels, indicating replication-associated DNA damage.

Parmacokinetics

Species	Dose	Route	AUC_0-t	T_max	T_1/2	C_max	Bioavailability	CL	V_z
Mice^[1]	2 mg/kg	i.v.	674.91 μg/L·h	/	0.72 h	/	/	2.95 L/h/kg	3.1 L/kg
Mice^[1]	10 mg/kg	p.o.	1342.88 μg/L·h	0.25 h	1.05 h	1513.31 μg/L	39.8 %	/	/

In Vivo

PKMYT1-IN-15 (5-15 mg/kg; p.o.; twice daily, with 2 days off after 5 consecutive days of administration, repeated for 3 cycles) exhibits moderate anti-tumor activity in OVCAR3 xenograft NOG mice, with a TGI of 44.08% at the 15 mg/kg dose; combined administration with Gemcitabine (HY-17026) achieves nearly complete inhibition of tumor progression, with a TGI of 95.73%, and no obvious systemic toxicity is observed^[1].

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

Animal Model:

NOG mice (female/male not specified; treatment initiated when mean tumor size reached 100-200 mm³; subcutaneous inoculation of 10 million OVCAR3 cells)^[1]
Dosage:

5 mg/kg; 15 mg/kg; 15 mg/kg (in combination with 20 mg/kg Gemcitabine)
Administration:

p.o.; twice daily for 5 days followed by 2 days off, repeated for 3 cycles
Result:

Did not produce statistically significant tumor growth inhibition compared to vehicle control at 5 mg/kg.
Achieved a tumor growth inhibition (TGI) rate of 44.08% at 15 mg/kg.
Resulted in near-complete tumor progression inhibition with a TGI of 95.73% when combined with 20 mg/kg Gemcitabine.
Showed no statistically significant differences in key hematological and serum biochemical parameters between treated (single-agent or combination) and vehicle control groups.
Caused moderate body weight reduction in treated mice, but no acute toxicity was noted.
Exhibited comparable tumor and plasma concentrations to RP-6306 at 2 hours post-administration, with higher transient concentrations in liver and kidney that diminished by 4 hours post-dose.

Chemical Information

Molecular Weight 394.35
Formula C₁₈H₁₇F₃N₄O₃
SMILES

CN1C(C(F)(F)F)=CC2=C([N@]([C@]3=C(C)C=CC(O)=C3C)C(N)=C2C(N)=O)C1=O
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

Handling Instructions (2659 KB)

References

[1]. Zhang J, et al. Design, synthesis, and biological evaluation of pyrrolo[2,3-c]pyridin-7-one derivatives as PKMYT1 inhibitors targeting CCNE1-amplified cancers. Eur J Med Chem. 2026 Jul 24;318:119161.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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PKMYT1-IN-15

All Wee1 Isoforms

All CDK Isoforms