CEP-37440
Based on 1 publication(s) in Google Scholar
CEP-37440 is a potent, orally active dual FAK/ALK inhibitor with IC50 values of 2.3 nM and 3.5 nM for FAK and ALK, respectively. CEP-37440 decreases the cell proliferation by blocking the autophosphorylation kinase activity of FAK1 (Tyr 397).
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- Pureza: 99.91%
- No. CAS: 1391712-60-9
- Fòrmula: C30H38ClN7O3
- Peso molecular:580.12
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) CEP-37440
More
Actividad biológica
IC50:2.3 nM (FAK) and 3.5 nM (ALK)[2]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KARPAS-299 | IC50 |
131 nM
Compound: (S)-27b
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Cytotoxicity against human KARPAS299 cells expressing NPM-ALK assessed as cell growth inhibition
Cytotoxicity against human KARPAS299 cells expressing NPM-ALK assessed as cell growth inhibition
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[PMID: 27527804] |
| NCI-H2228 | IC50 |
175 nM
Compound: (S)-27b
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Inhibition of EML4-ALK tyrosine phosphorylation in human NCI-H2228 cells
Inhibition of EML4-ALK tyrosine phosphorylation in human NCI-H2228 cells
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[PMID: 27527804] |
| NCI-H2228 | IC50 |
2900 nM
Compound: (S)-27b
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Cytotoxicity against human NCI-H2228 cells expressing EML4-ALK assessed as cell growth inhibition
Cytotoxicity against human NCI-H2228 cells expressing EML4-ALK assessed as cell growth inhibition
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[PMID: 27527804] |
| NCI-H3122 | IC50 |
1779 nM
Compound: (S)-27b
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Cytotoxicity against human NCI-H3122 cells expressing EML4-ALK assessed as cell growth inhibition
Cytotoxicity against human NCI-H3122 cells expressing EML4-ALK assessed as cell growth inhibition
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[PMID: 27527804] |
CEP-37440 (0-3000 nM; 0-192 h) decreases the proliferation of inflammatory breast cancer (IBC) cells in a dose-dependent manner[1].
CEP-37440 (1000 nM; 0-120 h) decreases phospho-FAK1 (Tyr 397) and maintains its low level over time in FC-IBC02, SUM 190, and KPL4[1].
CEP-37440 (0-3000 nM; Sup-M2 and Karpas-299 cells) induces proapoptotic caspases in a dose-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:FC-IBC02, KPL4, SUM190, MDA-IBC03 and SUM149 cells
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Concentration:0, 300, 1000, 2000 and 3000 nM
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Incubation Time:0, 24, 48, 72, 96, 120, 144, 168, and 192 hours
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Result:Reduced the proliferation of three out of five IBC cell lines at low concentration. Inhibited the proliferation almost completely at 3000 nM concentration.
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Cell Line:FC-IBC02, SUM 190, and KPL4 cells
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Concentration:1000 nM
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Incubation Time:0, 48, 72, 96 and 120 hours
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Result:Decreased phospho-FAK1 by half in FC-IBC02, SUM190, and KPL4 cells after 48 hours.
CEP-37440 (30 mg/kg; p.o; once, for 24 h) inhibits tyrosine phosphorylation in Sup-M2 xenografts mice[2].
CEP-37440 (55 mg/kg; p.o; once, for 24 h) inhibits FAK phosphorylation in CWR22 xenografts in Nude mice[2].
CEP-37440 (1-10 mg/kg; p.o and i.v.; CD-1 mouse, Sprague-Dawley (SD) rats) has good pharmacokinetic parameters[2].
Pharmacokinetic parameters in CD-1 mouse and Sprague-Dawley (SD) rats[2]
| PK parameter | CD-1 mouse | SD rat | |
| iv | dose (mg/kg) | 1 | 1 |
| iv | t1/2 (h) | 3.0 | 2 |
| iv | AUC0-∞ (ng*h/mL) | 1612 | 4005 |
| iv | Vd (L/kg) | 2.7 | 0.8 |
| iv | CL (mL/min/kg) | 10 | 4 |
| po | dose (mg/kg) | 10 | 5 |
| po | Cmax (ng/mL) | 1533 | 1340 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID/Beige with Sup-M2 xenografts[2]
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Dosage:3 mg/kg (b.i.d), 10 mg/kg (b.i.d), 30 mg/kg (b.i.d and q.d. ), and 55 mg/kg (q.d.)
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Administration:Oral administration; b.i.d and q.d., for 12 days
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Result:Inhibited tumor growth in a dose-dependent manner.
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Animal Model:SCID/Beige with Sup-M2 xenografts and Nu/Nu mice female with Sup-M2 xenografts[2]
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Dosage:30 mg/kg
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Administration:Oral administration; once, for 24 hours
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Result:Decreased NPM-ALK phosphorylation (>85%).
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Animal Model:Nu/Nu mice female with CWR22 xenografts[2]
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Dosage:55 mg/kg
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Administration:Oral administration; once, for 24 hours
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Result:Inhibited FAK phosphorylation in a time-dependent manner.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1391712-60-9
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Appearance Solid
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Peso molecular 580.12
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Fòrmula C30H38ClN7O3
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Color White to yellow
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SMILES
O=C(NC)C1=CC=CC=C1NC2=NC(NC3=CC=C4C(CCC[C@H](N5CCN(CCO)CC5)C4)=C3OC)=NC=C2Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Autophagy
PTK2/FAK inhibition triggers TMED9-mediated protective autophagy in pancreatic cancer cell via enhancing ERGIC-ERES contact. [Abstract]2026 May 29:1-15. PMID: 42144738
Solvente y solubilidad
DMSO : 100 mg/mL (172.38 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (4.31 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 (4.31 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.
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.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Salem I, et, al. The effects of CEP-37440, an inhibitor of focal adhesion kinase, in vitro and in vivo on inflammatory breast cancer cells. Breast Cancer Res. 2016 Mar 24;18(1):37. [Content Brief]
[2]. Ott GR, et, al. Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK). J Med Chem. 2016 Aug 25;59(16):7478-96. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7238 mL | 8.6189 mL | 17.2378 mL | 43.0945 mL |
| 5 mM | 0.3448 mL | 1.7238 mL | 3.4476 mL | 8.6189 mL | |
| 10 mM | 0.1724 mL | 0.8619 mL | 1.7238 mL | 4.3095 mL | |
| 15 mM | 0.1149 mL | 0.5746 mL | 1.1492 mL | 2.8730 mL | |
| 20 mM | 0.0862 mL | 0.4309 mL | 0.8619 mL | 2.1547 mL | |
| 25 mM | 0.0690 mL | 0.3448 mL | 0.6895 mL | 1.7238 mL | |
| 30 mM | 0.0575 mL | 0.2873 mL | 0.5746 mL | 1.4365 mL | |
| 40 mM | 0.0431 mL | 0.2155 mL | 0.4309 mL | 1.0774 mL | |
| 50 mM | 0.0345 mL | 0.1724 mL | 0.3448 mL | 0.8619 mL | |
| 60 mM | 0.0287 mL | 0.1436 mL | 0.2873 mL | 0.7182 mL | |
| 80 mM | 0.0215 mL | 0.1077 mL | 0.2155 mL | 0.5387 mL | |
| 100 mM | 0.0172 mL | 0.0862 mL | 0.1724 mL | 0.4309 mL |
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