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Lys-Nε-SPDB-DM4

  CAS No.: 1280215-91-9   Cat No.: BADC-01467 4.5  

Lys-Nε-SPDB-DM4 is a drug-linker conjugate consisting of the potent tubulin inhibitor DM4 and the linker Lys-Nε-SPDB for the preparation of antibody-drug conjugates (ADCs).

Lys-Nε-SPDB-DM4

Structure of 1280215-91-9

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Category
ADC Cytotoxin
Molecular Formula
C48H72ClN5O13S2
Molecular Weight
1026.69

* For research and manufacturing use only. We do not sell to patients.

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Synonyms
DM4-spdb-L-lysine; Lys-Nepsilon-SPDB-DM4
IUPAC Name
(2S)-2-amino-6-[4-[[5-[[(2S)-1-[[(1S,2R,3S,5S,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl]oxy]-1-oxopropan-2-yl]-methylamino]-2-methyl-5-oxopentan-2-yl]disulfanyl]butanoylamino]hexanoic acid
Canonical SMILES
CC1C2CC(C(C=CC=C(CC3=CC(=C(C(=C3)OC)Cl)N(C(=O)CC(C4(C1O4)C)OC(=O)C(C)N(C)C(=O)CCC(C)(C)SSCCCC(=O)NCCCCC(C(=O)O)N)C)C)OC)(NC(=O)O2)O
InChI
InChI=1S/C48H72ClN5O13S2/c1-28-15-13-17-36(64-10)48(62)27-35(65-45(61)52-48)29(2)42-47(6,67-42)37(26-40(57)54(8)33-24-31(23-28)25-34(63-9)41(33)49)66-44(60)30(3)53(7)39(56)19-20-46(4,5)69-68-22-14-18-38(55)51-21-12-11-16-32(50)43(58)59/h13,15,17,24-25,29-30,32,35-37,42,62H,11-12,14,16,18-23,26-27,50H2,1-10H3,(H,51,55)(H,52,61)(H,58,59)/b17-13+,28-15+/t29-,30+,32+,35+,36-,37+,42+,47+,48+/m1/s1
InChIKey
VUAUZOXSQKWNNO-NBSRGMMNSA-N

Lys-Nε-SPDB-DM4 is a novel antibody-drug conjugate (ADC) designed to target cancer cells expressing specific antigens, combining the specificity of an antibody with the cytotoxic power of the drug DM4. The structure includes a linker molecule (SPDB) that attaches the cytotoxic agent DM4 to the lysine residue at the epsilon position (Nε) of the antibody. DM4 is a potent maytansinoid derivative, which inhibits microtubule polymerization, ultimately leading to cell cycle arrest and apoptosis in rapidly dividing cancer cells. The ADC approach allows for selective delivery of DM4 directly to tumor cells, enhancing therapeutic efficacy while minimizing systemic toxicity.

One of the key applications of Lys-Nε-SPDB-DM4 is in the treatment of solid tumors, including breast, ovarian, and non-small cell lung cancers (NSCLC). These cancers often express specific tumor-associated antigens, such as HER2, which can be targeted by Lys-Nε-SPDB-DM4. The antibody component of the ADC selectively binds to these antigens, allowing DM4 to be delivered directly to the tumor site. By targeting tumor cells more precisely than conventional chemotherapy, this approach helps to reduce collateral damage to healthy tissues, potentially leading to fewer side effects and improved patient outcomes.

Another significant application of Lys-Nε-SPDB-DM4 is in the treatment of hematological malignancies, such as non-Hodgkin lymphoma (NHL) and leukemia. Like solid tumors, many B-cell malignancies express tumor-specific antigens that can be targeted by Lys-Nε-SPDB-DM4. For example, the targeting of CD19 or CD20 on B cells in lymphoma could allow for the effective delivery of DM4 to malignant cells, leading to selective cytotoxicity. Clinical research is exploring these applications to expand the therapeutic uses of Lys-Nε-SPDB-DM4 in the treatment of hematologic cancers.

Lys-Nε-SPDB-DM4 is also being studied in combination with other cancer therapies, such as immune checkpoint inhibitors or other chemotherapeutic agents. The combination of Lys-Nε-SPDB-DM4 with these therapies could enhance its efficacy by stimulating an immune response against the tumor while also directly killing cancer cells through DM4 delivery. This synergistic approach may help overcome resistance to monotherapies and improve long-term survival rates in patients with difficult-to-treat cancers. Clinical trials are ongoing to assess the safety and efficacy of these combination regimens.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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