Art. -Nr.: HY-12300B

Ocifisertib fumarate

(Synonyms: CFI-400945 fumarate)

6 Cited Publications

Kundenbewertung

Based on 6 publication(s) in Google Scholar

CFI-400945 fumarate is a potent, selective and orally bioavailable PLK4 inhibitor with a K_i and an IC₅₀ of 0.26 nM and 2.8 nM, respectively.

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Reinheit: 98.69%
CAS. Nr.: 1616420-30-4
Formel: C₃₇H₃₈N₄O₇
Molecular Weight:650.72

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Ocifisertib fumarate Chemical Structure

CAS. Nr.: 1616420-30-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

CFI-400945 fumarate is a potent, selective and orally bioavailable PLK4 inhibitor with a K_i and an IC₅₀ of 0.26 nM and 2.8 nM, respectively.

IC₅₀ & Target^[1]

PLK4

2.8 nM (IC₅₀)

AURKA

140 nM (IC₅₀)

AURKB/INCENP

98 nM (IC₅₀)

TIE2/TEK

22 nM (IC₅₀)

TRKA

6 nM (IC₅₀)

TRKB

9 nM (IC₅₀)

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

Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	0.005 μM Compound: 48	Growth inhibition of human A549 cells after 5 days by SRB assay Growth inhibition of human A549 cells after 5 days by SRB assay	[PMID: 24867403]
BT-20	GI₅₀	0.058 μM Compound: 48	Growth inhibition of human BT20 cells after 5 days by SRB assay Growth inhibition of human BT20 cells after 5 days by SRB assay	[PMID: 24867403]
CAL-51	GI₅₀	0.26 μM Compound: 48	Growth inhibition of human CAL51 cells after 5 days by SRB assay Growth inhibition of human CAL51 cells after 5 days by SRB assay	[PMID: 24867403]
COLO 205	GI₅₀	0.017 μM Compound: 48	Growth inhibition of human COLO205 cells after 5 days by SRB assay Growth inhibition of human COLO205 cells after 5 days by SRB assay	[PMID: 24867403]
HCC1954	GI₅₀	0.005 μM Compound: 48	Growth inhibition of human HCC1954 cells after 5 days by SRB assay Growth inhibition of human HCC1954 cells after 5 days by SRB assay	[PMID: 24867403]
HCT-116	GI₅₀	0.004 μM Compound: 48	Growth inhibition of human HCT116 cells after 5 days by SRB assay Growth inhibition of human HCT116 cells after 5 days by SRB assay	[PMID: 24867403]
HMEC	GI₅₀	9 μM Compound: 48	Growth inhibition of human HMEC cells after 5 days by SRB assay Growth inhibition of human HMEC cells after 5 days by SRB assay	[PMID: 24867403]
MCF7	GI₅₀	0.008 μM Compound: 48	Growth inhibition of human MCF7 cells after 5 days by SRB assay Growth inhibition of human MCF7 cells after 5 days by SRB assay	[PMID: 24867403]
MDA-MB-231	GI₅₀	8.6 μM Compound: 48	Growth inhibition of human MDA-MB-231 cells after 5 days by SRB assay Growth inhibition of human MDA-MB-231 cells after 5 days by SRB assay	[PMID: 24867403]
MDA-MB-468	GI₅₀	0.006 μM Compound: 48	Growth inhibition of human MDA-MB-468 cells after 5 days by SRB assay Growth inhibition of human MDA-MB-468 cells after 5 days by SRB assay	[PMID: 24867403]
OVCAR-3	GI₅₀	0.018 μM Compound: 48	Growth inhibition of human OVCAR3 cells after 5 days by SRB assay Growth inhibition of human OVCAR3 cells after 5 days by SRB assay	[PMID: 24867403]
SK-BR-3	GI₅₀	5.3 μM Compound: 48	Growth inhibition of human SKBR3 cells after 5 days by SRB assay Growth inhibition of human SKBR3 cells after 5 days by SRB assay	[PMID: 24867403]
SW-620	GI₅₀	0.38 μM Compound: 48	Growth inhibition of human SW620 cells after 5 days by SRB assay Growth inhibition of human SW620 cells after 5 days by SRB assay	[PMID: 24867403]

In Vitro

CFI-400945 (compound 48) shows potent inhibitory activities against a panel of kinases, including PLK4, TRKA, TRKB, AURKA, AURKB/INCENP, and TIE2/TEK, with IC₅₀s of 2.8, 6, 9, 140, 98, 22 nM, and EC₅₀s of 12, 84, 88, 510, 102, 117 nM, respectively. CFI-400945 exhibits growth inhibition effects on breast, lung, ovarian and colon cancer cells. The IC₅₀s (in μM) are as follows: SKBr-3 (5.3), Cal-51 (0.26), BT-20 (0.058), A549 (0.005), OVCAR-3 (0.018), SW620 (0.38), Colo-205 (0.017), and HCT116+/+ (0.004) ^[1]. CFI-400945 inhibits autophosphorylation of PLK4 at serine 305 with an EC₅₀ value of 12.3 nM in cells overexpressing PLK4. Cancer cells treated with CFI-400945 exhibit effects consistent with PLK4 kinase inhibition, including dysregulated centriole duplication, mitotic defects, and cell death^[2].

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

In Vivo

Oral administration of CFI-400945 (3.0, 9.4 mg/kg) to mice bearing human cancer xenografts results in the significant inhibition of tumor growth at doses that are well tolerated. Increased antitumor activity is observed in PTEN-deficient compared to PTEN wild-type cancer xenografts. The maximum tolerated dose for once-daily administration of CFI-400945 is estimated to be 7.5-9.5 mg/kg^[2].

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

Chemical Information

CAS. Nr. 1616420-30-4
Appearance Solid
Molecular Weight 650.72
Formel C₃₇H₃₈N₄O₇
Color White to yellow
SMILES

OC(/C=C/C(O)=O)=O.O=C1[C@@]2(C3=CC(OC)=CC=C3N1)[C@H](C4=CC=C(C(/C=C/C5=CC=C(C=C5)CN6C[C@H](O[C@H](C6)C)C)=NN7)C7=C4)C2
Synonyms

CFI-400945 fumarate
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (6)

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Journal Impact Factor

Nat Nanotechnol

Therapeutically reprogrammed nutrient signalling enhances nanoparticulate albumin bound drug uptake and efficacy in KRAS-mutant cancer. [Abstract]

2021 Jul;16(7):830-839. PMID: 33958764
Cell Death Differ

GSDME acts as an epigenetic modifier to promote melanoma development via centriole biogenesis regulator PLK4. [Abstract]

2026 May 25. PMID: 42185629
J Integr Plant Biol

The mechanism of newly differentiated leaves of kale turning white in late autumn. [Abstract]

2026 Apr 2. PMID: 41928062
Int J Mol Med

MicroRNA‑126 suppresses the proliferation and migration of endothelial cells in experimental diabetic retinopathy by targeting polo‑like kinase 4. [Abstract]

2021 Jan;47(1):151-160. PMID: 33416109
J Cancer Res Clin Oncol

Anticancer effects of the PLK4 inhibitors CFI-400945 and centrinone in Ewing's sarcoma cells. [Abstract]

2020 Nov;146(11):2871-2883. PMID: 32770382
Ir J Med Sci

PLK4 inhibitor plus bortezomib exhibits a synergistic effect on treating multiple myeloma via inactivating PI3K/AKT signaling. [Abstract]

2023 Apr;192(2):561-567. PMID: 35508865

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (76.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5368 mL

7.6838 mL

15.3676 mL

5 mM

0.3074 mL

1.5368 mL

3.0735 mL

10 mM

0.1537 mL

0.7684 mL

1.5368 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (3.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (3.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.5 mg/mL (3.84 mM); Clear solution; Need warming

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

Active PLK4 is purified and used to measure PLK4 activity, using an indirect ELISA detection system. PLK1, PLK2, PLK3, AURKA, and AUKB/INCENP compound inhibition are determined using FRET-based homogeneous assay kits from Invitrogen. The assays are performed with ATP concentrations of 25, 60, and 80 μM, respectively, for PLK1, PLK2, and PLK3 and ATP concentrations of 20 and 128 μM, respectively, for AURKA and AURKB/INCENP^[1].

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

Cell Assay^[2]

MDA-MB-468, MCF-7, HCC1954, MDA-MB-231, SKBr-3, Cal-51, and BT-20 breast cancer cells are treated with 10 nM to 50 μM CFI-400945 for 5 days. Cell viability is measured using SRB assay^[2].

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

Animal Administration^[2]

Mice: To treat an established tumor, CFI-400945 and the vehicle (water) are administered by oral gavage (2.5-20 mg/kg), and 5-FU and carboplatin are administered by intraperitoneal injection to mice as described in the text. Animal weights are monitored daily, and tumor volume is measured three times per week^[2].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Sampson PB, et al. The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor agent. J Med Chem. 2015 Jan 8;58(1):147-69. [Content Brief]

[2]. Mason JM, et al. Functional characterization of CFI-400945, a Polo-like kinase 4 inhibitor, as a potential anticancer agent. Cancer Cell. 2014 Aug 11;26(2):163-76. [Content Brief]

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.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.5368 mL	7.6838 mL	15.3676 mL	38.4190 mL
	5 mM	0.3074 mL	1.5368 mL	3.0735 mL	7.6838 mL
	10 mM	0.1537 mL	0.7684 mL	1.5368 mL	3.8419 mL
	15 mM	0.1025 mL	0.5123 mL	1.0245 mL	2.5613 mL
	20 mM	0.0768 mL	0.3842 mL	0.7684 mL	1.9209 mL
	25 mM	0.0615 mL	0.3074 mL	0.6147 mL	1.5368 mL
	30 mM	0.0512 mL	0.2561 mL	0.5123 mL	1.2806 mL
	40 mM	0.0384 mL	0.1921 mL	0.3842 mL	0.9605 mL
	50 mM	0.0307 mL	0.1537 mL	0.3074 mL	0.7684 mL
	60 mM	0.0256 mL	0.1281 mL	0.2561 mL	0.6403 mL

Keywords

Ocifisertib fumarate

6 Cited Publications

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Ocifisertib fumarate

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Ocifisertib fumarate

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

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Ocifisertib fumarate

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Ocifisertib fumarate

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

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Ocifisertib fumarate Related Classifications

HY-12300B Related Classifications