Product Name :
CPI-169
Description:
CPI-169 (R) is a novel and potent EZH2 inhibitor.
CAS:
1802175-07-0
Molecular Weight:
528.66
Formula:
C27H36N4O5S
Chemical Name:
1-[(1R)-1-[1-(ethanesulfonyl)piperidin-4-yl]ethyl]-N-[(4-methoxy-6-methyl-2-oxo-1, 2-dihydropyridin-3-yl)methyl]-2-methyl-1H-indole-3-carboxamide
Smiles :
C[C@H](C1CCN(CC1)S(=O)(=O)CC)N1C2=CC=CC=C2C(C(=O)NCC2=C(C=C(C)NC2=O)OC)=C1C
InChiKey:
LHGUZCKPFXXVPV-GOSISDBHSA-N
InChi :
InChI=1S/C27H36N4O5S/c1-6-37(34,35)30-13-11-20(12-14-30)18(3)31-19(4)25(21-9-7-8-10-23(21)31)27(33)28-16-22-24(36-5)15-17(2)29-26(22)32/h7-10,15,18,20H,6,11-14,16H2,1-5H3,(H,28,33)(H,29,32)/t18-/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:
CPI-169 (R) is a novel and potent EZH2 inhibitor.|Product information|CAS Number: 1802175-07-0|Molecular Weight: 528.66|Formula: C27H36N4O5S|Synonym:|CPI169 R-enantiomer|CPI 169 R-enantiomer|Chemical Name: 1-[(1R)-1-[1-(ethanesulfonyl)piperidin-4-yl]ethyl]-N-[(4-methoxy-6-methyl-2-oxo-1, 2-dihydropyridin-3-yl)methyl]-2-methyl-1H-indole-3-carboxamide|Smiles: C[C@H](C1CCN(CC1)S(=O)(=O)CC)N1C2=CC=CC=C2C(C(=O)NCC2=C(C=C(C)NC2=O)OC)=C1C|InChiKey: LHGUZCKPFXXVPV-GOSISDBHSA-N|InChi: InChI=1S/C27H36N4O5S/c1-6-37(34,35)30-13-11-20(12-14-30)18(3)31-19(4)25(21-9-7-8-10-23(21)31)27(33)28-16-22-24(36-5)15-17(2)29-26(22)32/h7-10,15,18,20H,6,11-14,16H2,1-5H3,(H,28,33)(H,29,32)/t18-/m1/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : ≥ 100 mg/mL (189.Vasopressin MedChemExpress 16 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.2,8-Dihydroxyadenine Autophagy |Shelf Life: ≥12 months if stored properly.PMID:32561351 |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:|CPI-169 (CPI 169 R-enantiomer) inhibits the catalytic activity of PRC2 with an IC50 of In Vivo:|CPI-169 (CPI 169 R-enantiomer) (200 mpk, s.c. BID) is well tolerated in mice with no observed toxic effect or body weight loss. CPI-169 treatment leads to tumor growth inhibition (TGI) of an EZH2 mutant KARPAS-422 DLBCL xenograft. CPI-169 (100 mpk, BID) with a single dose of CHOP leads tumors to rapidly regress and become unpalpable. In mice bearing KARPAS-422 xenografts, CPI-169 (200 mg/kg, s.c.) effectively suppresses H3K27me3 levels and results in lymphoma tumor regression without affecting body weight or causing any overt adverse effects.|References:|Vidya Balasubramanian, et al. CPI-169, a novel and potent EZH2 inhibitor, synergizes with CHOP in vivoand achieves complete regression in lymphoma xenograft models. Cancer Res October 1, 2014 74; 1697Bradley WD, et al. EZH2 inhibitor efficacy in non-Hodgkin’s lymphoma does not require suppression of H3K27 monomethylation. Chem Biol. 2014 Nov 20;21(11):1463-75Products are for research use only. Not for human use.|
