KIF18A-IN-20
KIF18A-IN-20 is an orally active KIF18A inhibitor with an IC50 of 52 nM. KIF18A-IN-20 targets the plus-end-directed mitotic kinesin KIF18A, regulating chromosome alignment and spindle dynamics, and inhibits the proliferation of chromosomally unstable OVCAR-3 ovarian cancer cells with EC50 = 3.4 nM. KIF18A-IN-20 achieves tumor regression in xenograft models without causing body weight loss. KIF18A-IN-20 can be used for research related to ovarian cancer.
For research use only. We do not sell to patients.
- CAS No.: 3120750-94-6
- Formula: C28H33F2N7O3S
- Molecular Weight:585.67
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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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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| OVCAR-3 | EC50 |
3.4 nM
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Antiproliferative activity against CIN-high human OVCAR-3 high-grade serous ovarian cancer cells assessed by nuclear count assay.
Antiproliferative activity against CIN-high human OVCAR-3 high-grade serous ovarian cancer cells assessed by nuclear count assay.
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42715868 |
| JIMT-1 | EC50 |
15.0 nM
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Antiproliferative activity against CIN-high human JIMT-1 breast cancer cells.
Antiproliferative activity against CIN-high human JIMT-1 breast cancer cells.
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42715868 |
| BT-549 | EC50 |
280.0 nM
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Antiproliferative activity against CIN-high human BT-549 breast cancer cells.
Antiproliferative activity against CIN-high human BT-549 breast cancer cells.
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42715868 |
| HCT-116 | EC50 |
>2000 nM
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Weak antiproliferative activity against human HCT116 colorectal cancer cells with EC50 > 2000 nM.
Weak antiproliferative activity against human HCT116 colorectal cancer cells with EC50 > 2000 nM.
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42715868 |
In Vitro
KIF18A-IN-20 is metabolically stable in HLM and MLM, with parent compound remaining at 80.40% and 86.99% at 60 minutes, respectively[1].
KIF18A-IN-20 exhibited low to moderate CYP inhibition against the tested CYP subtypes at 10 μM, with the highest inhibition rates observed for CYP 2C8 (54.29%) and CYP 2C9 (49.51%)[1].
KIF18A-IN-20 has negligible inhibitory effect on hERG (0.07% at 10 μM)[1].
KIF18A-IN-20 exhibits low P-gp-mediated efflux in Caco-2 cells, with an efflux ratio of 1.59[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 1 × 107 OVCAR-3 cells in 100 μL)[1]
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Dosage:5 mg/kg QD, PO; 20 mg/kg QD, PO; 40 mg/kg QD, PO
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Administration:PO; QD; 21 days
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Result:Achieved tumor growth inhibition of 97.5% at 5 mg/kg, 97.5% at 20 mg/kg, and 96.9% at 40 mg/kg.
Tumor weights were 0.014 g at 5 mg/kg, 0.014 g at 20 mg/kg, and 0.017 g at 40 mg/kg.
Maximal tumor growth inhibition was ≈ 97% at all tested doses.
No body-weight loss was observed.
Chemical Information
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CAS No. 3120750-94-6
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Molecular Weight 585.67
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Formula C28H33F2N7O3S
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SMILES
O=S(NC1=CC=C(C(NC2=CN3C(C(N4CCC(F)(F)CC4)=N2)=NC=C3)=O)C(N5C[C@H]6C7(CC7)[C@H](CC6)C5)=C1)(C)=O
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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)
KIF18A-IN-20 Related Classifications
HY-189647 Related Classifications
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