CEP-37440 |
| Katalog-Nr.GC15273 |
CEP-37440 ist ein potenter, oral aktiver dualer FAK/ALK-Inhibitor mit IC50-Werten von 2,3 nM und 3,5 nM fÜr FAK bzw. ALK. CEP-37440 verringert die Zellproliferation, indem es die Autophosphorylierungskinase-AktivitÄt von FAK1 (Tyr 397) blockiert.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1391712-60-9
Sample solution is provided at 25 µL, 10mM.
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IC50: 1000 nM for the proliferation in SUM190 cell lines
The focal adhesion kinase FAK1 is a cytoplasmic tyrosine kinase that localizes to focal adhesions, and controls a number of cell pathways including proliferation, viability and survival. Anaplastic lymphoma kinase 1 (ALK-1) is a member of the insulin receptor tyrosine kinase family. ALK mutations have also been implicated in the pathogenesis of non-small cell lung cancer (NSCLC) and other solid tumors. CEP-37440 is a highly selective and potent dual inhibitor of ALK and FAK1.
In vitro: 300 nM CEP-37440 was able to decrease the proliferation of the triple negative FC-IBC02 cell line and, 1000 nM CEP-37440 was able to complete inhibit the proliferation of these cells. Genes involved in functions such as cellular growth and proliferation, cell cycle, cell death and survival and cellular movement and cell-to cell signaling and interaction were differentially regulated by CEP-37440 in sensitive IBC cell lines. Among them, TGFβ1 and MMP3 were down-regulated and DKK3, CAV1 and TFPI2 were up-regulated by CEP-37440, which might be probalby caused by its dual inhibition of ALK and FAK1 [1].
In vivo: In FC-IBC02 orthotopic breast cancer xenograft models, CEP-37440 was able to reduce the growth of the primary tumor and inhibit the development of spontaneous metastases in brain [1].
Clinical trials: CEP-37440 is a dual ALK/FAK inhibitor currently under investigation in a phase I trial to determine its MTD in patients with advanced or metastatic solid tumors (NCT01922752).
Reference:
[1] Abstract 3232: CEP-37440, a highly selective and potent dual inhibitor of ALK and FAK1 inhibits the proliferation of inflammatory breast cancer cells. Proceedings: AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA
| Cas No. | 1391712-60-9 | SDF | |
| Chemical Name | (Z)-2-((E)-(5-chloro-2-(((S)-6-(4-(2-hydroxyethyl)piperazin-1-yl)-1-methoxy-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)amino)pyrimidin-4(3H)-ylidene)amino)-N-methylbenzimidic acid | ||
| Canonical SMILES | C/N=C(O)/C1=CC=CC=C1/N=C(N2)\C(Cl)=CN=C2NC3=C(OC)C(CCC[C@@](N4CCN(CCO)CC4)([H])C5)=C5C=C3 | ||
| Formula | C30H38ClN7O3 | M.Wt | 580.12 |
| Löslichkeit | ≥ 9.25mg/mL in DMSO with gentle warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7238 mL | 8.6189 mL | 17.2378 mL |
| 5 mM | 0.3448 mL | 1.7238 mL | 3.4476 mL |
| 10 mM | 0.1724 mL | 0.8619 mL | 1.7238 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)
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