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Art. -Nr.: HY-120279A

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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. Nr.: 1169211-37-3
Formel: C₂₉H₂₈N₆O₂
Molecular Weight:492.57

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

CFI-400437 Chemical Structure

CAS. Nr.: 1169211-37-3

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

CFI-400437 is an indolinone-derived, ATP-competitive kinase inhibitor with high selectivity for PLK4 (IC₅₀ of 0.6 nM)^[1].

Alle Polo-like Kinase (PLK) Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	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	[PMID: 23829549]
MCF7	GI₅₀	<0.01 μM Compound: 6	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	[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	[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.

In Vivo

CFI-400437 (25 mg/kg, ip, once daily for 21 d) exhibits antitumor activity against MDA-MB-468 breast cancer mouse xenograft model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1169211-37-3
Molecular Weight 492.57
Formel C₂₉H₂₈N₆O₂
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
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CFI-400437

Alle Polo-like Kinase (PLK) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

CFI-400437 Related Classifications

HY-120279A Related Classifications