Trastuzumab emtansine

For research use only. Not for therapeutic Use.

  • CAT Number: I037463
  • CAS Number: 1018448-65-1
  • Purity: 98%
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Trastuzumab emtansine (Cat.No:I037463) also known as ado-trastuzumab emtansine and sold under the trade name Kadcyla, is an antibody-drug conjugate consisting of the humanized monoclonal antibody trastuzumab covalently linked to the cytotoxic agent DM1.


Catalog Number I037463
CAS Number 1018448-65-1
Synonyms

Trastuzumab emtansine; ado-trastuzumab emtansine; Kadcyla; T-DM1; T-DM-1; T-DM 1

Purity 98%
Target JAK/STAT Signaling
Solubility To be determined
Appearance Solid powder
Storage Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
IUPAC Name N2'-(3-((1-((4-carboxycyclohexyl)methyl)-2,5-dioxo-3-pyrrolidinyl)thio)-1-oxopropyl)-N2'-deacetylmaytansine
SMILES [*]NC([C@@H]1CC[C@H](CC1)CN2C(CC(C2=O)SCCC(N([C@H](C(O[C@H]3CC(N(c4c(Cl)c(OC)cc(C/C(C)=C/C=C/[C@H]([C@]5(C[C@@H]([C@H]([C@@H]6O[C@@]36C)C)OC(N5)=O)O)OC)c4)C)=O)=O)C)C)=O)=O)=O
Reference

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3: Verma S, Miles D, Gianni L, Krop IE, Welslau M, Baselga J, Pegram M, Oh DY, Diéras V, Guardino E, Fang L, Lu MW, Olsen S, Blackwell K; EMILIA Study Group. Trastuzumab emtansine for HER2-positive advanced breast cancer. N Engl J Med. 2012 Nov 8;367(19):1783-91. doi: 10.1056/NEJMoa1209124. Epub 2012 Oct 1. Erratum in: N Engl J Med. 2013 Jun 20;368(25):2442. PMID: 23020162; PMCID: PMC5125250.
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5: Hunter FW, Barker HR, Lipert B, Rothé F, Gebhart G, Piccart-Gebhart MJ, Sotiriou C, Jamieson SMF. Mechanisms of resistance to trastuzumab emtansine (T-DM1) in HER2-positive breast cancer. Br J Cancer. 2020 Mar;122(5):603-612. doi: 10.1038/s41416-019-0635-y. Epub 2019 Dec 16. PMID: 31839676; PMCID: PMC7054312.
6: Tamura K, Tsurutani J, Takahashi S, Iwata H, Krop IE, Redfern C, Sagara Y, Doi T, Park H, Murthy RK, Redman RA, Jikoh T, Lee C, Sugihara M, Shahidi J, Yver A, Modi S. Trastuzumab deruxtecan (DS-8201a) in patients with advanced HER2-positive breast cancer previously treated with trastuzumab emtansine: a dose-expansion, phase 1 study. Lancet Oncol. 2019 Jun;20(6):816-826. doi: 10.1016/S1470-2045(19)30097-X. Epub 2019 Apr 29. Erratum in: Lancet Oncol. 2019 May 10;: PMID: 31047803.
7: Hurvitz SA, Martin M, Symmans WF, Jung KH, Huang CS, Thompson AM, Harbeck N, Valero V, Stroyakovskiy D, Wildiers H, Campone M, Boileau JF, Beckmann MW, Afenjar K, Fresco R, Helms HJ, Xu J, Lin YG, Sparano J, Slamon D. Neoadjuvant trastuzumab, pertuzumab, and chemotherapy versus trastuzumab emtansine plus pertuzumab in patients with HER2-positive breast cancer (KRISTINE): a randomised, open-label, multicentre, phase 3 trial. Lancet Oncol. 2018 Jan;19(1):115-126. doi: 10.1016/S1470-2045(17)30716-7. Epub 2017 Nov 23. PMID: 29175149.
8: Diéras V, Miles D, Verma S, Pegram M, Welslau M, Baselga J, Krop IE, Blackwell K, Hoersch S, Xu J, Green M, Gianni L. Trastuzumab emtansine versus capecitabine plus lapatinib in patients with previously treated HER2-positive advanced breast cancer (EMILIA): a descriptive analysis of final overall survival results from a randomised, open-label, phase 3 trial. Lancet Oncol. 2017 Jun;18(6):732-742. doi: 10.1016/S1470-2045(17)30312-1. Epub 2017 May 16. Erratum in: Lancet Oncol. 2017 Aug;18(8):e433. Erratum in: Lancet Oncol. 2018 Dec;19(12):e667. PMID: 28526536; PMCID: PMC5531181.
9: Emens LA, Esteva FJ, Beresford M, Saura C, De Laurentiis M, Kim SB, Im SA, Wang Y, Salgado R, Mani A, Shah J, Lambertini C, Liu H, de Haas SL, Patre M, Loi S. Trastuzumab emtansine plus atezolizumab versus trastuzumab emtansine plus placebo in previously treated, HER2-positive advanced breast cancer (KATE2): a phase 2, multicentre, randomised, double-blind trial. Lancet Oncol. 2020 Oct;21(10):1283-1295. doi: 10.1016/S1470-2045(20)30465-4. PMID: 33002436.
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