BiochemProbe — Life Science Research Reagents

CEP-28122 free base · Synonyms: CEP 28122 · CEP28122

CEP-28122, a diaminopyrimidine derivative, is a potent, selective, and orally active ALK inhibitor.

For research use only. Not for human or veterinary use.

Target Anaplastic lymphoma kinase (ALK)
Research area Cancer
Purity >98% Stock Inquire
Data Sheet SDS COA

CEP-28122 structure

CAS No.: 1022958-60-6

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
100 mg USD 598.00 BP-02493-100mg In stock Get quote
250 mg USD 950.00 BP-02493-250mg In stock Get quote
500 mg USD 1,200.00 BP-02493-500mg In stock Get quote
1 g USD 1,900.00 BP-02493-1g In stock Get quote
2 g USD 2,900.00 BP-02493-2g In stock Get quote
5 g Inquire BP-02493-5g In stock Inquire
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Description

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

Biological activity

In Vitro CEP-28122 (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. CEP-28122 (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. In Vivo CEP-28122 (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

Identifiers

SMILES
COC1=C(NC2=NC=C(Cl)C(N[C@@H]3[C@@H]4C[C@@H](C=C4)[C@@H]3C(N)=O)=N2)C=CC2=C1CC[C@H](CC2)N1CCOCC1
InChIKey
LAJAFFLJAJMYLK-CVOKMOJFSA-N

Specifications

MW (average)
539.0690
Formula
C28H35ClN6O3
CAS No.
1022958-60-6
Physical state
Solid
Color
White to off-white
Shipping
—
Storage
—

Solubility

Soluble in DMSO

Documents

References

[1].Cheng M, 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):670-679.

Same target

Search Anaplastic lymphoma kinase (ALK)

Same research area

Search Cancer