CEP-28122 methanesulfonic acid other

CEP-28122 mesylate hydrochloride, 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 Others

Purity >98% Stock Inquire

Data Sheet SDS COA

CEP-28122 methanesulfonic acid structure

CAS No.: 1354545-57-5

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
5 mg	USD 650.00	BP-02493A-5mg	In stock	Get quote
10 mg	USD 880.00	BP-02493A-10mg	In stock	Get quote
50 mg	USD 1,950.00	BP-02493A-50mg	In stock	Get quote
100 mg	Inquire	BP-02493A-100mg	In stock	Inquire
250 mg	Inquire	BP-02493A-250mg	In stock	Inquire

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Related forms

BP-02493 — CEP-28122

Description

CEP-28122 mesylate hydrochloride, a diaminopyrimidine derivative, is a potent, selective, and orally active ALK inhibitor with an IC50 value of 1.9 nM. CEP-28122 mesylate hydrochloride has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 mesylate hydrochloride has good pharmacodynamic and pharmacokinetic activity. CEP-28122 mesylate hydrochloride 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) mesylate hydrochloride 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) mesylate hydrochloride 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) mesylate hydrochloride 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: CS(O)(=O)=O.[H][C@@]12C[C@@]([H])(C=C1)[C@@H]([C@@H]2NC1=NC(NC2=CC=C3CC[C@@H](CCC3=C2OC)N2CCOCC2)=NC=C1Cl)C(N)=O
InChIKey: PIIIZYXUYVVFSN-WWQCAQLDSA-N

Specifications

MW (average): 635.1750
Formula: C₂₉H₃₉ClN₆O₆S
CAS No.: 1354545-57-5
Physical state: Solid
Color: White to off-white
Shipping: —
Storage: —

Solubility

Soluble in DMSO

Documents

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.

Same target

Search Anaplastic lymphoma kinase (ALK)

Same research area

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