Cat. No.: HY-18030A

CEP-28122 mesylate salt

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CEP-28122 mesylate salt, a diaminopyrimidine derivative, is a potent, selective, and orally active ALK inhibitor with an IC₅₀ value of 1.9 nM. CEP-28122 mesylate salt has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 mesylate salt has good pharmacodynamic and pharmacokinetic activity. CEP-28122 mesylate salt can be used for the study of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma cells.

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

Purity: 99.92%
CAS No.: 2070009-30-0
Formula: C₂₉H₃₉ClN₆O₆S
Molecular Weight:635.17

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

CEP-28122 mesylate salt Chemical Structure

CAS No.: 2070009-30-0

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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

In Vitro

CEP-28122 (3-3000 nM; 48 hours) mesylate salt 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 (30-1000 nM; 2 hours) mesylate salt 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].

MedChemExpress (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 (3-30 mg/kg; oral gavage; twice a day; 12 days) mesylate salt 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].

MedChemExpress (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:

Produced dose-dependent antitumor activity in Sup-M2 subcutaneous tumor xenografts in SCID mice. Had no antitumor activity in nu/nu mice bearing HCT116.

Chemical Information

CAS No. 2070009-30-0

Appearance Solid

Molecular Weight 635.17

Formula C₂₉H₃₉ClN₆O₆S

Color White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 6.4 mg/mL (10.08 mM; Need ultrasonic and warming; 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)

SDS (252 KB)

English - EN (252 KB)

Français - FR (252 KB)

Deutsch - DE (252 KB)

Norwegian - NO (252 KB)

Español - ES (252 KB)

Swedish - SV (252 KB)

Italian - IT (252 KB)

Korean - KR (252 KB)

Portuguese - PT (252 KB)

COA (2659 KB)

Elemental Analysis Report (2659 KB)

HNMR (2659 KB)

CNMR (2659 KB)

RP-HPLC (2659 KB)

NP-HPLC (2659 KB)

MS (2659 KB)

LCMS (2659 KB)

IR (2659 KB)

GC (2659 KB)

OR (2659 KB)

SDS-PAGE (2659 KB)

SEC-HPLC (2659 KB)

Other Report (2659 KB)

Handling Instructions (2659 KB)

References

[1]. Mangeng Cheng, 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. Mol Cancer Ther. 2012 Mar;11(3):670-9. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg

DMSO 1 mM 1.5744 mL 7.8719 mL 15.7438 mL 39.3595 mL

5 mM 0.3149 mL 1.5744 mL 3.1488 mL 7.8719 mL

10 mM 0.1574 mL 0.7872 mL 1.5744 mL 3.9360 mL

CEP-28122 mesylate salt Related Classifications

HY-18030A Related Classifications

Protein Tyrosine Kinase/RTK

Anaplastic lymphoma kinase (ALK)

Disease Areas

Cancer Blood or Cardio-cerebrovascular Disease Respiratory Disease

Lung Cancer Respiratory Cancer Leukemia/Lymphoma/Myeloma Blood Disease

Non-Small Cell Lung Cancer

Cancer

Cancer Targeted Therapy

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Keywords

CEP-28122
2070009-30-0
CEP28122
CEP 28122
Anaplastic lymphoma kinase (ALK)
diaminopyrimidine derivative
ALK inhibitor
orally active
anaplastic large-cell lymphoma (ALCL)
non-small cell lung cancer (NSCLC)
and neuroblastoma cells
Inhibitor
inhibitor
inhibit

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