Product Name :
CEP-28122 mesylate salt
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.
CAS:
2070009-30-0
Molecular Weight:
635.17
Formula:
C29H39ClN6O6S
Chemical Name:
(1S,2S,3R,4R)-3-[(5-chloro-2-{[(7S)-1-methoxy-7-(morpholin-4-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl]amino}pyrimidin-4-yl)amino]bicyclo[2.2.1]hept-5-ene-2-carboxamide; methanesulfonic acid
Smiles :
COC1C(=CC=C2CC[C@@H](CCC2=1)N1CCOCC1)NC1N=C(N[C@H]2[C@H]([C@H]3C[C@@H]2C=C3)C(N)=O)C(Cl)=CN=1.CS(O)(=O)=O
InChiKey:
PIIIZYXUYVVFSN-WWQCAQLDSA-N
InChi :
InChI=1S/C28H35ClN6O3.{{Tamoxifen} medchemexpress|{Tamoxifen} Apoptosis|{Tamoxifen} Protocol|{Tamoxifen} In stock|{Tamoxifen} manufacturer|{Tamoxifen} Autophagy} CH4O3S/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;1-5(2,3)4/h2-3,5,9,15,17-19,23-24H,4,6-8,10-14H2,1H3,(H2,30,36)(H2,31,32,33,34);1H3,(H,2,3,4)/t17-,18+,19+,23+,24-;/m1./s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
CEP-28122 mesylate salt, a diaminopyrimidine derivative, is a potent, selective, and orally bioavailable ALK inhibitor, with an IC50 value of 1.{{Hesperetin} MedChemExpress|{Hesperetin} Apoptosis|{Hesperetin} Purity & Documentation|{Hesperetin} Description|{Hesperetin} custom synthesis|{Hesperetin} Epigenetic Reader Domain} 9 nM for recombinant ALK kinase activity.PMID:24103058 CEP-28122 has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 mesylate salt has good pharmacodynamic and pharmacokinetic activity.|Product information|CAS Number: 2070009-30-0|Molecular Weight: 635.17|Formula: C29H39ClN6O6S|Chemical Name: (1S,2S,3R,4R)-3-[(5-chloro-2-{[(7S)-1-methoxy-7-(morpholin-4-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl]amino}pyrimidin-4-yl)amino]bicyclo[2.2.1]hept-5-ene-2-carboxamide; methanesulfonic acid|Smiles: COC1C(=CC=C2CC[C@@H](CCC2=1)N1CCOCC1)NC1N=C(N[C@H]2[C@H]([C@H]3C[C@@H]2C=C3)C(N)=O)C(Cl)=CN=1.CS(O)(=O)=O|InChiKey: PIIIZYXUYVVFSN-WWQCAQLDSA-N|InChi: InChI=1S/C28H35ClN6O3.CH4O3S/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;1-5(2,3)4/h2-3,5,9,15,17-19,23-24H,4,6-8,10-14H2,1H3,(H2,30,36)(H2,31,32,33,34);1H3,(H,2,3,4)/t17-,18+,19+,23+,24-;/m1./s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : ≥ 6.4 mg/mL (10.08 mM).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|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. 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.|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 .|Products are for research use only. Not for human use.|
