CEP-28122 |
| Catalog No.GC15145 |
anaplastic lymphoma kinase (ALK) inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1022958-60-6
Sample solution is provided at 25 µL, 10mM.
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IC50: 1.9 nM: blocks anaplastic lymphoma kinase (ALK).
CEP-28122, a highly potent, selective, orally bioavailable inhibitor of ALK, dampens the phosphorylation of ALK and ALK substrates in cells and triggers cytotoxicity or growth inhibition of ALK-positive cancer cells with a favorable pharmaceutical and pharmacokinetic profile and selective pharmacologic efficacy. CEP-28122 blocks ALK tyrosine phosphorylation in tumor xenografts in mice. ALK, which is constitutively activated in many human cancer types because of point mutations, gene amplification, and chromosomal translocations, has emerged as an excellent molecular target for cancer therapy.
In vitro: CEP-28122, concentration-dependently, triggered growth inhibition/cytotoxicity of ALK-positive anaplastic large-cell lymphoma (ALCL) via inhibiting nucleophosmin (NPM) -ALK tyrosine (664) phosphorylation. Due to the CEP-28122 treatment, EML4-ALK tyrosine phosphorylation was blocked in non-small cell lung cancer (NSCLC) NCI-H2228 and NCI-H3122 cells and full-length ALK receptor tyrosine phosphorylation was inhibited in neuroblastoma cell line NB-1 cells [1].
In vivo: Severe combined immunodeficient (SCID) mice bearing Sup-M2 (B) or nu/nu mice bearing colon carcinoma HCT-116 (C) subcutaneous tumor xenografts were administered orally with CEP-28122 at 3, 10, or 30 mg/kg for 24 days. CEP-28122 showed inhibition of ALK tyrosine phosphorylation in a dose-dependent manner in tumor xenografts in mice when treated at 30 mg/kg. Moreover, CEP-28122 displayed dose-dependent antitumor activity in ALK-positive ALCL, NSCLC, and neuroblastoma tumor xenografts in mice when administered orally at 30 mg/kg or higher [1].
Reference:
[1]. Cheng, M., Quail, M., Gingrich, D., Ott, G., Lu, L., & Wan, W. et al. CEP-28122, a Highly Potent and Selective Orally Active Inhibitor of Anaplastic Lymphoma Kinase with Antitumor Activity in Experimental Models of Human Cancers. Molecular Cancer Therapeutics. 2011; 11(3): 670-679.
| Cas No. | 1022958-60-6 | SDF | |
| Chemical Name | (1S,2S,3R,4R)-3-[[5-chloro-2-[[(7S)-6,7,8,9-tetrahydro-1-methoxy-7-(4-morpholinyl)-5H-benzocyclohepten-2-yl]amino]-4-pyrimidinyl]amino]-bicyclo[2.2.1]hept-5-ene-2-carboxamide | ||
| Canonical SMILES | COC1=C(NC2=NC=C(Cl)C(N[C@@H]3[C@H](C4)C=C[C@H]4[C@@H]3C(N)=O)=N2)C=CC5=C1CC[C@@H](N6CCOCC6)CC5 | ||
| Formula | C28H35ClN6O3 | M.Wt | 539.1 |
| Solubility | ≤30mg/ml in DMSO;12mg/ml in dimethyl formamide | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8549 mL | 9.2747 mL | 18.5494 mL |
| 5 mM | 0.371 mL | 1.8549 mL | 3.7099 mL |
| 10 mM | 0.1855 mL | 0.9275 mL | 1.8549 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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