BGC0222

BGC0222 is a novel prodrug of Irinotecan. BGC0222, as a PEG-cRGD-conjugated Irinotecan (HY-16562) derivative, could slowly and steadily release Irinotecan (HY-16562). BGC0222 binds to αVβ3 with IC50 values of 4.25 μM (αVβ3) and 58.7 μM (αVβ5). BGC0222 possesses the property of inducing neovascularization. BGC0222 exhibits good antiproliferation activity in many tumors[1].

C1241H2276N64O552

26927.36

O=C(NCCCC[C@@H](C(NCC(O[C@@]1(C(OCC2=C1C=C3C4=NC5=CC=C(C=C5C(CC)=C4CN3C2=O)OC(N6CCC(CC6)N7CCCCC7)=O)=O)CC)=O)=O)NC(COCCOCCOCCOCCOCCOCCNC(CC[C@@H]8NC([C@H](NC([C@@H](NC(CNC([C@@H](NC8=O)CCCNC(N)=N)=O)=O)CC(O)=O)=O)CC9=CC=CC=C9)=O)=O)=O)COCCOCC(COCCOCC(NCCCC[C@@H](C(NCC(O[C@@]%10(C(OCC%11=C%10C=C%12C%13=NC%14=CC=C(C=C%14C(CC)=C%13CN%12C%11=O)OC(N%15CCC(CC%15)N%16CCCCC%16)=O)=O)CC)=O)=O)NC(COCCOCCOCCOCCOCCOCCNC(CC[C@@H]%17NC([C@H](NC([C@@H](NC(CNC([C@@H](NC%17=O)CCCNC(N)=N)=O)=O)CC(O)=O)=O)CC%18=CC=CC=C%18)=O)=O)=O)=O)(COCCOCC(NCCCC[C@@H](C(NCC(O[C@@]%19(C(OCC%20=C%19C=C%21C%22=NC%23=CC=C(C=C%23C(CC)=C%22CN%21C%20=O)OC(N%24CCC(CC%24)N%25CCCCC%25)=O)=O)CC)=O)=O)NC(COCCOCCOCCOCCOCCOCCNC(CC[C@@H]%26NC([C@H](NC([C@@H](NC(CNC([C@@H](NC%26=O)CCCNC(N)=N)=O)=O)CC(O)=O)=O)CC%27=CC=CC=C%27)=O)=O)=O)=O)COCCOCC(NCCCC[C@@H](C(NCC(O[C@@]%28(C(OCC%29=C%28C=C%30C%31=NC%32=CC=C(C=C%32C(CC)=C%31CN%30C%29=O)OC(N%33CCC(CC%33)N%34CCCCC%34)=O)=O)CC)=O)=O)NC(COCCOCCOCCOCCOCCOCCNC(CC[C@@H]%35NC([C@H](NC([C@@H](NC(CNC([C@@H](NC%35=O)CCCNC(N)=N)=O)=O)CC(O)=O)=O)CC%36=CC=CC=C%36)=O)=O)=O)=O

Integrin; Peptide-Drug Conjugates (PDCs)

Room temperature