GSK461364 analogue 1
GSK461364 analogue 1 is a thiophene-based PLK1 inhibitor with a PLK1 IC50 of 2 nM and a PLK3 IC50 of 630 nM. GSK461364 analogue 1 also acts as an inhibitor of Nek2 kinase (IC50: 21 nM). GSK461364 analogue 1 has a solubility of ≥190 μM in pH 7.4 PBS and a human plasma protein binding rate of 91.5%. GSK461364 analogue 1 can be used in studies related to colon cancer, lung cancer, breast cancer and ovarian cancer.
For research use only. We do not sell to patients.
- CAS No.: 929095-23-8
- Formula: C26H27ClN4O3S
- Molecular Weight:511.04
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PLK1 2 nM (IC50) |
PLK3 630 nM (IC50) |
NEK2 21 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
11 nM
Compound: 25
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Antiproliferative activity against human A549 cells after 72 hrs by luminescence-based cell viability assay
Antiproliferative activity against human A549 cells after 72 hrs by luminescence-based cell viability assay
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[PMID: 19237286] |
| COLO 205 | IC50 |
5 nM
Compound: 25
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Antiproliferative activity against human COLO205 cells after 72 hrs by luminescence-based cell viability assay
Antiproliferative activity against human COLO205 cells after 72 hrs by luminescence-based cell viability assay
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[PMID: 19237286] |
| HCT-116 | IC50 |
11 nM
Compound: 25
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Antiproliferative activity against human HCT116 cells after 72 hrs by luminescence-based cell viability assay
Antiproliferative activity against human HCT116 cells after 72 hrs by luminescence-based cell viability assay
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[PMID: 19237286] |
| HT-29 | IC50 |
3 nM
Compound: 25
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Antiproliferative activity against human HT-29 cells after 72 hrs by luminescence-based cell viability assay
Antiproliferative activity against human HT-29 cells after 72 hrs by luminescence-based cell viability assay
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[PMID: 19237286] |
| MX1 | IC50 |
9 nM
Compound: 25
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Antiproliferative activity against human MX1 cells after 72 hrs by luminescence-based cell viability assay
Antiproliferative activity against human MX1 cells after 72 hrs by luminescence-based cell viability assay
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[PMID: 19237286] |
| SK-OV-3 | IC50 |
11 nM
Compound: 25
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Antiproliferative activity against human SKOV3 cells after 72 hrs by luminescence-based cell viability assay
Antiproliferative activity against human SKOV3 cells after 72 hrs by luminescence-based cell viability assay
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[PMID: 19237286] |
GSK461364 analogue 1 (2 h) inhibits the proliferation of HCT116 colorectal cancer cells, with an IC50 of 11 nM[1].
GSK461364 analogue 1 (72 h) potently inhibits the proliferation of various human tumor cell lines (colon, lung, breast, ovary), with an IC50 value ranging from 3 to 11 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:COLO205, HT29, A549, MX-1, SKOV-3
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Concentration:/
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Incubation Time:72 h
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Result:Had IC50 of 5 nM (COLO205 ), 3 nM (HT29), 11 nM (A549), 9 nM (MX-1), 11 nM (SKOV-3).
Chemical Information
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CAS No. 929095-23-8
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Molecular Weight 511.04
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Formula C26H27ClN4O3S
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SMILES
O(C=1C=C2N(C=NC2=CC1)C3=CC(O[C@H](C)C4=C(Cl)C=CC=C4)=C(C(N)=O)S3)C5CCN(C)CC5
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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)
GSK461364 analogue 1 Related Classifications
HY-111090 Related Classifications
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