CFI-400437
CFI-400437 is an indolinone-derived, ATP-competitive kinase inhibitor with high selectivity for PLK4 (IC50 of 0.6 nM).
For research use only. We do not sell to patients.
- CAS No.: 1169211-37-3
- Formula: C29H28N6O2
- Molecular Weight:492.57
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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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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCC1954 | GI50 |
2.3 μM
Compound: 50
|
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
|
[PMID: 24867403] |
| MCF7 | GI50 |
0.01 μM
Compound: 50
|
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
|
[PMID: 23829549] |
| MDA-MB-231 | GI50 |
<0.01 μM
Compound: 50
|
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
|
[PMID: 23829549] |
| MDA-MB-231 | GI50 |
<0.01 μM
Compound: 6
|
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
|
[PMID: 24867403] |
| MDA-MB-468 | GI50 |
<0.01 μM
Compound: 50
|
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
|
[PMID: 23829549] |
| MDA-MB-468 | GI50 |
<0.01 μM
Compound: 6
|
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
|
[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
|
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] |
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.
Chemical Information
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CAS No. 1169211-37-3
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Molecular Weight 492.57
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Formula 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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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]. 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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