KY216
KY216 (Tubulin polymerization-IN-41) is a potent tubulin polymerization inhibitor with the IC50 of 2.61 μM. KY216 targets the Colchicine-binding site of tubulin. KY216 can be used for the study of non-small cell lung cancer (NSCLC) and breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 2804026-81-9
- Formula: C20H16Cl2N2O5
- Molecular Weight:435.26
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
8.7 nM
Compound: C3
|
Antiproliferative activity against human HCT-116 cells measured after 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells measured after 72 hrs by MTT assay
|
[PMID: 36471625] |
| HT-29 | IC50 |
8.3 nM
Compound: C3
|
Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTT assay
Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTT assay
|
[PMID: 36471625] |
| K562 | IC50 |
6.3 nM
Compound: C3
|
Antiproliferative activity against human K562 cells measured after 72 hrs by MTT assay
Antiproliferative activity against human K562 cells measured after 72 hrs by MTT assay
|
[PMID: 36471625] |
| MCF7 | IC50 |
9.2 nM
Compound: C3
|
Antiproliferative activity against human MCF7 cells measured after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells measured after 72 hrs by MTT assay
|
[PMID: 36471625] |
KY216 (compound C3) displays remarkable antiproliferative activities with IC50 values of 6.3 nM, 9.2 nM, 8.3 nM, and 8.7 nM for K562, MCF-7, HT29, and HCT116 cells, respectively. Additionally, KY216 shows marked activity against Paclitaxel-resistant MCF-7 cells and A549 cells[1].
KY216 (compound C3; 5-20 nM) downregulates the expression of acetyl-α-tubulin (Ac-α-tubulin) and upregulated the expression of detyrosinated-α-tubulin (DeY-α-tubulin) in a concentration-dependent manner[1].
KY216 (compound C3; 5-20 nM; 24 hours) could arrest cancer cells in the G2/M phase, and induces MCF-7 cells apoptosis in a concentration-dependent manner[1].
KY216 (compound C3; 5-20 nM; 24 hours) reduces Ser216 phosphorylation, resulting in cdc2 Tyr15 dephosphorylation and Thr161 phosphorylation, which ultimately leads to the activation of subsequent cdc2/cyclin B1 complex[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells
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Concentration:5 nM, 10 nM, 20 nM
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Incubation Time:24 h
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Result:Could arrest cancer cells in the G2/M phase.
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Cell Line:MCF-7 cells
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Concentration:5 nM, 10 nM, 20 nM
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Incubation Time:24 h
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Result:Induced MCF-7 cells apoptosis.
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Cell Line:MCF-7 cells
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Concentration:5 nM, 10 nM, 20 nM
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Incubation Time:24 h
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Result:Induced cdc25c activation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Five-week-old female athymic nude mice injected with MCF-7 cells[1]
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Dosage:5, 10, and 20 mg/kg
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Administration:Intraperitoneal injection; every two days; for 21 consecutive days
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Result:Exhibited the significant potency of tumor growth inhibition in a dose dependence without weight loss in the drug-treated period.
Chemical Information
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CAS No. 2804026-81-9
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Molecular Weight 435.26
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Formula C20H16Cl2N2O5
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SMILES
O=C(N1[C@@H](C2=CC3=C(C=C2C[C@H]14)OCCO3)C5=CC(Cl)=C(C(Cl)=C5)OC)NC4=O
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Synonyms
Tubulin polymerization-IN-41
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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
[1]. Jiafu Leng, et al. Discovery of Novel N-Heterocyclic-Fused Deoxypodophyllotoxin Analogues as Tubulin Polymerization Inhibitors Targeting the Colchicine-Binding Site for Cancer Treatment. J Med Chem. 2022 Dec 22;65(24):16774-16800. [Content Brief]
[2]. He XY, et al. KY216-tubulin complex captures VASH2 to inhibit NSCLC metastasis. Nat Commun. 2025 Dec 4. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)