PKMYT1-IN-16
PKMYT1-IN-16 is an orally active and selective PKMYT1 kinase inhibitor with IC50 = 2.3 nM. PKMYT1-IN-16 blocks CDK1 inhibitory phosphorylation and reduces CDK1 phosphorylation, and inhibits DDR1, EPHA2, SRC, and CSF1R. PKMYT1-IN-16 in combination with CHK1 inhibitors exhibits synergistic antiproliferative activity, disrupts cell cycle checkpoints, aggravates DNA damage, and induces apoptosis (apoptosis). PKMYT1-IN-16 can be used for research on triple-negative breast cancer (TNBC) and ovarian cancer.
For research use only. We do not sell to patients.
- Formula: C20H18ClN3O3
- Molecular Weight:383.83
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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 2.3 nM (IC50) |
CDK1/cyclinB1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCC1569 | IC50 |
>2 μM
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Antiproliferative activity against human HCC1569 cells assessed by cell-based assay with IC50 > 2 μM.
Antiproliferative activity against human HCC1569 cells assessed by cell-based assay with IC50 > 2 μM.
|
42753957 |
| MDA-MB-231 | IC50 |
>2 μM
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Antiproliferative activity against human MDA-MB-231 cells assessed by cell-based assay with IC50 > 2 μM.
Antiproliferative activity against human MDA-MB-231 cells assessed by cell-based assay with IC50 > 2 μM.
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42753957 |
| OVCAR-3 | IC50 |
>2 μM
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Antiproliferative activity against human OVCAR3 cells assessed by cell-based assay with IC50 > 2 μM.
Antiproliferative activity against human OVCAR3 cells assessed by cell-based assay with IC50 > 2 μM.
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42753957 |
In Vitro
PKMYT1-IN-16 exhibited IC50 values of 172.3 nM (DDR1), 39.0 nM (EPHA2), 23.5 nM (SRC), 164.0 nM (CSF1R), and >1000 nM (BTK) in HTRF kinase assays[1].
PKMYT1-IN-16 has a LogD of 3.8, a kinetic solubility of 134.3 μM, a liver microsomal CLint of 42.0/52.0/21.4 μL/min/mg protein, a mouse/human PPB of 97.8/99.1%, a Caco-2 Papp of 8.1 × 10-6 cm/s, and an efflux ratio of 0.4[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
- Western Blot
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Protocol for Cell Cycle
- Breast Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
- Kinase activity and phosphorylation assays
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Apoptosis Solutions
- Protocol for Kinase activity and phosphorylation assays
- Genotoxicity/Mutagenicity Study
Parmacokinetics
Chemical Information
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Molecular Weight 383.83
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Formula C20H18ClN3O3
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SMILES
CC1=C(C(C)=C(C=C1)O)C2=C(C(C(N)=O)=C(N=C2)OC3=CC=C(C=C3)Cl)N
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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-16 Related Classifications
HY-189676 Related Classifications
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