| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Anaplastic lymphoma kinase (ALK). CEP-28122 inhibits ALK with an IC50 of 1.9 ± 0.5 nM in an enzyme-based TRF assay. It is a potent inhibitor of recombinant ALK activity and cellular ALK tyrosine phosphorylation. CEP-28122 shows >300× selectivity over the insulin receptor. The compound is a diaminopyrimidine analogue that is a specific and orally bioactive ALK inhibitor (antagonist) with IC50 of 1.9 nM for recombinant ALK kinase activity.
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| ln Vitro |
CEP-28122 inhibits recombinant ALK activity and cellular ALK tyrosine phosphorylation. It induces concentration-dependent growth inhibition and cytotoxicity of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma cells. The compound demonstrates potent antiproliferative effects against ALK-driven cancer cell lines. CEP-28122 blocks ALK tyrosine phosphorylation in a dose-dependent manner in tumor xenografts in mice when treated at 30 mg/kg. It displays dose-dependent antitumor activity in ALK-positive ALCL, NSCLC, and neuroblastoma tumor xenografts in mice when administered orally at 30 mg/kg or higher.
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| ln Vivo |
CEP-28122 has demonstrated robust and selective pharmacologic efficacy against ALK-positive human tumor xenograft models in mice. It inhibits tumor growth in ALK-positive ALCL, NSCLC, and neuroblastoma models. The compound is orally active and has a favorable pharmacokinetic profile, supporting its in vivo efficacy. CEP-28122 blocks ALK tyrosine phosphorylation in a dose-dependent manner in tumor xenografts in mice when treated at 30 mg/kg. Administration of CEP-28122 was well tolerated in mice and rats.
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| Enzyme Assay |
Kinase assays for CEP-28122 are performed using a Flashplate assay. The assay uses 384-well Basic Flashplate as a solid platform. Plates are coated overnight at 4°C with dithiothreitol (DTT) at 100 μg/mL in PBS buffer. 5 μL of compound in 2% DMSO is added to each well, followed by 15 μL of kinase buffer master mix (50 mM Tris pH 7.5, 10 mM NaCl, 2.5 mM MgCl2, 1 mM MBP, 20 μM ATP, and 0.025 μCi/μL 33P-ATP). Finally, 250 ng per well of Aurora-A enzyme is added. The plate is incubated for 2 hours at room temperature. The reaction is stopped by washing with 10 mM sodium pyrophosphate. The plate is then read on a TopCount-NXTTM. The assay measures the inhibition of ALK enzymatic activity by CEP-28122.
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| Cell Assay |
Cellular assays for CEP-28122 involve treating ALK-positive cancer cell lines with the compound and assessing cell growth inhibition and cytotoxicity. The compound's ability to inhibit ALK tyrosine phosphorylation in cells is also evaluated. These assays typically measure cell viability and signaling pathway inhibition. CEP-28122 induces concentration-dependent growth inhibition and cytotoxicity of ALK-positive ALCL, NSCLC, and neuroblastoma cells. The compound's antiproliferative effects are assessed in various cancer cell lines.
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| Animal Protocol |
In vivo efficacy of CEP-28122 is evaluated in mouse xenograft models of ALK-positive human cancers. Tumor-bearing mice are administered the compound orally, and tumor growth inhibition is measured. The compound's pharmacokinetic profile and tolerability are also assessed in these studies. CEP-28122 displays dose-dependent antitumor activity in ALK-positive ALCL, NSCLC, and neuroblastoma tumor xenografts in mice when administered orally at 30 mg/kg or higher. Administration of CEP-28122 was well tolerated in mice and rats.
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| ADME/Pharmacokinetics |
CEP-28122 has a favorable pharmacokinetic profile that supports oral administration. It is orally active and demonstrates robust efficacy in vivo. The compound offers consistent 37–71% oral bioavailability across mouse and rat for reliable PK/PD translation. CEP-28122 is a highly potent and selective orally active ALK inhibitor with a favorable pharmaceutical and pharmacokinetic profile.
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| Toxicity/Toxicokinetics |
Administration of CEP-28122 was well tolerated in mice and rats. Specific toxicological data is not available in the provided references. As a preclinical candidate, its safety profile would be evaluated in standard toxicology studies to determine potential adverse effects and establish a safe dose range.
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| References | |
| Additional Infomation |
CEP-28122 is a research compound not approved for clinical use. It is a valuable tool for studying ALK-driven cancers and has shown efficacy in preclinical models of ALCL, NSCLC, and neuroblastoma. The compound's high potency and selectivity for ALK make it a promising candidate for further development. CEP-28122 is a diaminopyrimidine-derived, ATP-competitive small molecule.
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| Molecular Formula |
C28H35CLN6O3
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| Molecular Weight |
539.0689
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| Exact Mass |
538.245
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| Elemental Analysis |
C, 62.39; H, 6.54; Cl, 6.58; N, 15.59; O, 8.90
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| CAS # |
1022958-60-6
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| Related CAS # |
CEP-28122 mesylate salt
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| PubChem CID |
57325421
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| Appearance |
Solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
786.9±70.0 °C at 760 mmHg
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| Flash Point |
429.7±35.7 °C
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| Vapour Pressure |
0.0±2.7 mmHg at 25°C
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| Index of Refraction |
1.665
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| LogP |
1.47
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
38
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| Complexity |
858
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| Defined Atom Stereocenter Count |
5
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| SMILES |
ClC1=C([H])N=C(N([H])C2C([H])=C([H])C3=C(C=2OC([H])([H])[H])C([H])([H])C([H])([H])C([H])(C([H])([H])C3([H])[H])N2C([H])([H])C([H])([H])OC([H])([H])C2([H])[H])N=C1N([H])C1([H])C([H])(C(N([H])[H])=O)C2([H])C([H])=C([H])C1([H])C2([H])[H]
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| InChi Key |
LAJAFFLJAJMYLK-CVOKMOJFSA-N
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| InChi Code |
InChI=1S/C28H35ClN6O3/c1-37-25-20-8-7-19(35-10-12-38-13-11-35)6-4-16(20)5-9-22(25)32-28-31-15-21(29)27(34-28)33-24-18-3-2-17(14-18)23(24)26(30)36/h2-3,5,9,15,17-19,23-24H,4,6-8,10-14H2,1H3,(H2,30,36)(H2,31,32,33,34)/t17-,18+,19+,23+,24-/m1/s1
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| Chemical Name |
(1S,2S,3R,4R)-3-[[5-chloro-2-[[(7S)-4-methoxy-7-morpholin-4-yl-6,7,8,9-tetrahydro-5H-benzo[7]annulen-3-yl]amino]pyrimidin-4-yl]amino]bicyclo[2.2.1]hept-5-ene-2-carboxamide
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| Synonyms |
CEP28122; CEP28122; CEP 28122
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8550 mL | 9.2752 mL | 18.5505 mL | |
| 5 mM | 0.3710 mL | 1.8550 mL | 3.7101 mL | |
| 10 mM | 0.1855 mL | 0.9275 mL | 1.8550 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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