Ocifisertib fumarate
Based on 6 publication(s) in Google Scholar
CFI-400945 fumarate is a potent, selective and orally bioavailable PLK4 inhibitor with a Ki and an IC50 of 0.26 nM and 2.8 nM, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.69%
- No. CAS: 1616420-30-4
- Fòrmula: C37H38N4O7
- Peso molecular:650.72
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Ocifisertib fumarate
More- Nat Nanotechnol. 2021 Jul;16(7):830-839. [Abstract]
- Cell Death Differ. 2026 May 25. [Abstract]
- J Integr Plant Biol. 2026 Apr 2. [Abstract]
- Int J Mol Med. 2021 Jan;47(1):151-160. [Abstract]
- J Cancer Res Clin Oncol. 2020 Nov;146(11):2871-2883. [Abstract]
- Ir J Med Sci. 2023 Apr;192(2):561-567. [Abstract]
Actividad biológica
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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) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | GI50 |
0.005 μM
Compound: 48
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Growth inhibition of human A549 cells after 5 days by SRB assay
Growth inhibition of human A549 cells after 5 days by SRB assay
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[PMID: 24867403] |
| BT-20 | GI50 |
0.058 μM
Compound: 48
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Growth inhibition of human BT20 cells after 5 days by SRB assay
Growth inhibition of human BT20 cells after 5 days by SRB assay
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[PMID: 24867403] |
| CAL-51 | GI50 |
0.26 μM
Compound: 48
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Growth inhibition of human CAL51 cells after 5 days by SRB assay
Growth inhibition of human CAL51 cells after 5 days by SRB assay
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[PMID: 24867403] |
| COLO 205 | GI50 |
0.017 μM
Compound: 48
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Growth inhibition of human COLO205 cells after 5 days by SRB assay
Growth inhibition of human COLO205 cells after 5 days by SRB assay
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[PMID: 24867403] |
| HCC1954 | GI50 |
0.005 μM
Compound: 48
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Growth inhibition of human HCC1954 cells after 5 days by SRB assay
Growth inhibition of human HCC1954 cells after 5 days by SRB assay
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[PMID: 24867403] |
| HCT-116 | GI50 |
0.004 μM
Compound: 48
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Growth inhibition of human HCT116 cells after 5 days by SRB assay
Growth inhibition of human HCT116 cells after 5 days by SRB assay
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[PMID: 24867403] |
| HMEC | GI50 |
9 μM
Compound: 48
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Growth inhibition of human HMEC cells after 5 days by SRB assay
Growth inhibition of human HMEC cells after 5 days by SRB assay
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[PMID: 24867403] |
| MCF7 | GI50 |
0.008 μM
Compound: 48
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Growth inhibition of human MCF7 cells after 5 days by SRB assay
Growth inhibition of human MCF7 cells after 5 days by SRB assay
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[PMID: 24867403] |
| MDA-MB-231 | GI50 |
8.6 μM
Compound: 48
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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
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[PMID: 24867403] |
| MDA-MB-468 | GI50 |
0.006 μM
Compound: 48
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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
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[PMID: 24867403] |
| OVCAR-3 | GI50 |
0.018 μM
Compound: 48
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Growth inhibition of human OVCAR3 cells after 5 days by SRB assay
Growth inhibition of human OVCAR3 cells after 5 days by SRB assay
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[PMID: 24867403] |
| SK-BR-3 | GI50 |
5.3 μM
Compound: 48
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Growth inhibition of human SKBR3 cells after 5 days by SRB assay
Growth inhibition of human SKBR3 cells after 5 days by SRB assay
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[PMID: 24867403] |
| SW-620 | GI50 |
0.38 μM
Compound: 48
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Growth inhibition of human SW620 cells after 5 days by SRB assay
Growth inhibition of human SW620 cells after 5 days by SRB assay
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[PMID: 24867403] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1616420-30-4
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Appearance Solid
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Peso molecular 650.72
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Fòrmula C37H38N4O7
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Color White to yellow
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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
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Synonyms
CFI-400945 fumarate
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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
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Most Recent
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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
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
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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.
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.
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.
Pureza y Documentación
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Ficha de datos (279 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
Ocifisertib fumarate Related Classifications
HY-12300B Related Classifications
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