A reactive drug-linker molecule containing Dxd
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Deruxtecan

Item No. 43189

Technical Information
Formal Name
N-[6-(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)-1-oxohexyl]glycylglycyl-L-phenylalanyl-N-[[2-[[(1S,9S)-9-ethyl-5-fluoro-2,3,9,10,13,15-hexahydro-9-hydroxy-4-methyl-10,13-dioxo-1H,12H-benzo[de]pyrano[3′,4′:6,7]indolizino[1,2-b]quinolin-1-yl]amino]-2-oxoethoxy]methyl]-glycinamide
CAS Number
1599440-13-7
Synonyms
  • Maleimidocaproyl-Gly-Gly-Phe-Gly-Dxd
  • Mc-GGFG-Dxd
Molecular Formula
C52H56FN9O13
Formula Weight
Purity
≥98%
A solid
DMSO: Slightly soluble: 0.1-1 mg/mlEthanol: Insolulble
SMILES
O=C(C=CC1=O)N1CCCCCC(NCC(NCC(N[C@@H](CC2=CC=CC=C2)C(NCC(NCOCC(N[C@@H]3C4=C5C(C(N6C5)=CC([C@](O)(C(OC7)=O)CC)=C7C6=O)=NC8=CC(F)=C(C)C(CC3)=C84)=O)=O)=O)=O)=O)=O
InChi Code
InChI=1S/C52H56FN9O13/c1-3-52(73)33-19-38-48-31(24-62(38)50(71)32(33)25-75-51(52)72)47-35(14-13-30-28(2)34(53)20-36(60-48)46(30)47)58-43(67)26-74-27-57-41(65)22-56-49(70)37(18-29-10-6-4-7-11-29)59-42(66)23-55-40(64)21-54-39(63)12-8-5-9-17-61-44(68)15-16-45(61)69/h4,6-7,10-11,15-16,19-20,35,37,73H,3,5,8-9,12-14,17-18,21-27H2,1-2H3,(H,54,63)(H,55,64)(H,56,70)(H,57,65)(H,58,67)(H,59,66)/t35-,37-,52-/m0/s1
InChi Key
WXNSCLIZKHLNSG-MCZRLCSDSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Deruxtecan is a reactive drug-linker molecule containing the exatecan derivative Dxd (Item No. 41699) and a maleimidocaproyl (Mc) linker.1 It has been linked to the anti-HER2 antibody trastuzumab as an antibody-drug conjugate (ADC) to target Dxd to tumor cells. Deruxtecan linked to trastuzumab binds to HER2 in a cell-free assay, is cytotoxic to breast cancer cells in vitro, and induces tumor regression in a BT474 breast cancer mouse xenograft model. Formulations containing deruxtecan conjugated to tumor-targeting antibodies have been used in the treatment of cancer.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Conilh, L., Fournet, G., Fourmaux, E., et alExatecan antibody drug conjugates based on a hydrophilic polysarcosine drug-linker platform. Pharmaceuticals (Basel) 14(3), 247 (2021).