1. Protein Tyrosine Kinase/RTK
  2. ALK
  3. CEP-28122 mesylate salt

CEP-28122 mesylate salt 

Cat. No.: HY-18030A Purity: 99.85%
Handling Instructions

CEP-28122 mesylate salt, a diaminopyrimidine derivative, is a potent, selective, and orally bioavailable ALK inhibitor, with an IC50 value of 1.9 nM for recombinant ALK kinase activity. CEP-28122 has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 mesylate salt has good pharmacodynamic and pharmacokinetic activity.

For research use only. We do not sell to patients.

CEP-28122 mesylate salt Chemical Structure

CEP-28122 mesylate salt Chemical Structure

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 252 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 252 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 288 In-stock
Estimated Time of Arrival: December 31
50 mg USD 660 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

CEP-28122 mesylate salt, a diaminopyrimidine derivative, is a potent, selective, and orally bioavailable ALK inhibitor, with an IC50 value of 1.9 nM for recombinant ALK kinase activity. CEP-28122 has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 mesylate salt has good pharmacodynamic and pharmacokinetic activity[1].

In Vitro

CEP-28122 mesylate salt (3-3000 nM; 48 hours) treatment leads to concentration-dependent growth inhibition of Karpas-299 and Sup-M2 cells in culture, associates with concentration-related caspase 3/7 activation[1].
CEP-28122 mesylate salt (30-1000 nM; 2 hours) treatment leads to substantial suppression of phosphorylation of putative downstream effectors of ALK in Sup-M2 cells, indicating that the downstream signaling pathways are mediated by individual ALK fusion protein[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: Karpas-299, Sup-M2, Toledo and HuT-102 cells
Concentration: 10 nM, 100 nM, 1000 nM, 10000 nM
Incubation Time: 48 hours
Result: Treatment led to concentration-dependent growth inhibition of Karpas-299 and Sup-M2 cells in culture.

Western Blot Analysis [1]

Cell Line: Sup-M2 cells
Concentration: 30 nM, 100 nM, 300 nM, 1000 nM
Incubation Time: 2 hours
Result: Resulted in substantial suppression of phosphorylation of putative downstream effectors of ALK, including Stat-3, Akt, and ERK1/2 in Sup-M2 cells.
In Vivo

CEP-28122 mesylate salt (3-30 mg/kg; oral gavage; twice a day; 12 days) produces dose-dependent antitumor activity in Sup-M2 subcutaneous tumor xenografts in SCID mice.In contrast, CEP-28122 has no antitumor activity in nu/nu mice bearing HCT116, suggesting that the antitumor activity of CEP-28122 in NPM-ALK–positive Sup-M2 tumor models is due to sustained NPM-ALK inhibition in tumors [1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female SCID mice bearing Sup-M2 subcutaneous tumor xenografts and nu/nu mice bearing HCT116 aged 6-8 week old[1]
Dosage: 3 mg/kg, 10 mg/kg and 30 mg/kg
Administration: oral gavage; twice a day; 12 days
Result: CEP-28122 produced dose-dependent antitumor activity in Sup-M2 subcutaneous tumor xenografts in SCID mice. In contrast, CEP-28122 had no antitumor activity in nu/nu mice bearing HCT116.
Molecular Weight

635.17

Formula

C₂₉H₃₉ClN₆O₆S

SMILES

O=C([[email protected]]1[[email protected]](C2)([H])C=C[[email protected]]2([H])[[email protected]]1NC3=NC(NC4=CC=C5C(CC[[email protected]@H](N6CCOCC6)CC5)=C4OC)=NC=C3Cl)N.O=S(C)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 6.4 mg/mL (10.08 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5744 mL 7.8719 mL 15.7438 mL
5 mM 0.3149 mL 1.5744 mL 3.1488 mL
10 mM 0.1574 mL 0.7872 mL 1.5744 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

CEP-28122CEP28122CEP 28122ALKAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Inhibitorinhibitorinhibit

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CEP-28122 mesylate salt
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HY-18030A
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