An orally active ALK inhibitor
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CEP-28122

Item No. 18406

Technical Information
Formal Name
(1S,2S,3R,4R)-3-[[5-chloro-2-[[(7S)-6,7,8,9-tetrahydro-1-methoxy-7-(4-morpholinyl)-5H-benzocyclohepten-2-yl]amino]-4-pyrimidinyl]amino]-bicyclo[2.2.1]hept-5-ene-2-carboxamide
CAS Number
1022958-60-6
Molecular Formula
C28H35ClN6O3
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 12 mg/mLDMSO: 30 mg/mLDMSO:PBS(pH 7.2) (1:2): 0.3 mg/mL
λmax
274 nm
SMILES
COC1=C(NC2=NC=C(Cl)C(N[C@@H]3[C@H](C4)C=C[C@H]4[C@@H]3C(N)=O)=N2)C=CC5=C1CC[C@@H](N6CCOCC6)CC5
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
InChi Key
LAJAFFLJAJMYLK-CVOKMOJFSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    CEP-28122 is a potent inhibitor of anaplastic lymphoma kinase (ALK; IC50 = 1.9 nM) that less potently inhibits other tyrosine and serine/threonine kinases.1 It blocks the phosphorylation of ALK and other ALK substrates in cells and induces concentration-dependent growth inhibition or cytotoxicity of ALK-positive cancer cells.1 CEP-28122 is orally active, inhibiting ALK tyrosine phosphorylation in tumor xenografts in mice for more than 12 hours following single oral dosing at 30 mg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chang, M., Quail, M.R., Gingrich, D.E., et alCEP-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. 11(3), 670-679 (2012).