CFI-400437
CFI-400437 is an indolinone-derived, ATP-competitive kinase inhibitor with high selectivity for PLK4 (IC50 of 0.6 nM).
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- CAS No.: 1169211-37-3
- Formule: C29H28N6O2
- Masse moléculaire:492.57
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCC1954 | GI50 |
2.3 μM
Compound: 50
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Antiproliferative activity against human HCC1954 cells assessed as growth inhibition after 5 days by SRB assay
Antiproliferative activity against human HCC1954 cells assessed as growth inhibition after 5 days by SRB assay
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[PMID: 23829549] |
| MCF7 | GI50 |
<0.01 μM
Compound: 6
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Cytotoxicity against human MCF7 cells after 5 days by SRB assay
Cytotoxicity against human MCF7 cells after 5 days by SRB assay
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[PMID: 24867403] |
| MCF7 | GI50 |
0.01 μM
Compound: 50
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Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 5 days by SRB assay
Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 5 days by SRB assay
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[PMID: 23829549] |
| MDA-MB-231 | GI50 |
<0.01 μM
Compound: 50
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Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 5 days by SRB assay
Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 5 days by SRB assay
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[PMID: 23829549] |
| MDA-MB-231 | GI50 |
<0.01 μM
Compound: 6
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Cytotoxicity against human MDA-MB-231 cells after 5 days by SRB assay
Cytotoxicity against human MDA-MB-231 cells after 5 days by SRB assay
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[PMID: 24867403] |
| MDA-MB-468 | GI50 |
<0.01 μM
Compound: 50
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Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition after 5 days by SRB assay
Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition after 5 days by SRB assay
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[PMID: 23829549] |
| MDA-MB-468 | GI50 |
<0.01 μM
Compound: 6
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Cytotoxicity against human MDA-MB-468 cells after 5 days by SRB assay
Cytotoxicity against human MDA-MB-468 cells after 5 days by SRB assay
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[PMID: 24867403] |
| SK-BR-3 | GI50 |
2.3 μM
Compound: 50
|
Antiproliferative activity against human SKBR3 cells assessed as growth inhibition after 5 days by SRB assay
Antiproliferative activity against human SKBR3 cells assessed as growth inhibition after 5 days by SRB assay
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[PMID: 23829549] |
| SK-BR-3 | GI50 |
2.3 μM
Compound: 6
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Cytotoxicity against human SKBR3 cells after 5 days by SRB assay
Cytotoxicity against human SKBR3 cells after 5 days by SRB assay
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[PMID: 24867403] |
In Vitro
CFI-400437 is a potent inhibitor of MCF-7, MDA-MB-468 and MDA-MB231 cell growth[1].
CFI-400437 inhibits Aurora A, Aurora B, KDR and FLT-3 with IC50s of 0.37, 0.21, 0.48, and 0.18 µM, respectively, i.e. two orders of magnitude higher than its IC50 of 0.6 nM against PLK4[1].
CFI-400437 inhibits both AURKB and AURKC at concentrations <15 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Chemical Information
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CAS No. 1169211-37-3
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Masse moléculaire 492.57
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Formule C29H28N6O2
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SMILES
O=C1NC2=C(C=C(OC)C=C2)/C1=C\C3=CC4=C(C=C3)C(/C=C/C5=CC=C(N6CCN(C)CC6)N=C5)=NN4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
Références
[1]. Radoslaw Laufer, et al. The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. J Med Chem. 2013 Aug 8;56(15):6069-87. [Content Brief]
[2]. Amreena Suri, et al. Evaluation of Protein Kinase Inhibitors with PLK4 Cross-Over Potential in a Pre-Clinical Model of Cancer. Int J Mol Sci. 2019 Apr 29;20(9):2112. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CFI-400437 Related Classifications
HY-120279A Related Classifications
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