2. Isotope-Labeled Compounds
  3. Research Area
  4. Internal standard Product for ADC New Drug Development

Internal standard Product for ADC New Drug Development

Antibody-drug conjugates (ADCs) are targeted drugs composed of antibodies, linkers and cytotoxic molecules. Unlike chemotherapy, ADCs target and kill tumor cells without harming healthy cells, by integrating the antigen specificity of monoclonal antibodies (mAbs) with antibody fragments. The ADC cytotoxin (also known as the payload) is the most important component, as it determines the potency of the ADCs to kill cancer cells. It is the "bullet" responsible for destroying cancer cells[1].

 

Figure 1 ADC drug

Isotope-labeled cytotoxin (such as MMAE-d8, Exatecan-d5 mesylate) have become the gold standard for quantitative detection due to the no matrix effects and high sensitivity in LCMS. This can provide important data support for their pharmacokinetics, biodistribution and facilitate the development of ADC new drugs[2].

 

References:

[1] Nat Rev Drug Discov. 2021 Aug;20(8):583-584.

[2] J Labelled Comp Radiopharm. 2014 May 15;57(5):350-7.

Internal standard Product for ADC New Drug Development (27):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-13631AS
    Exatecan-d5 mesylate 2819276-88-3 99.82%
    Exatecan-d5 (mesylate) is deuterium labeled Exatecan mesylate. Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL[1].
    Exatecan-d<sub>5</sub> mesylate
  • HY-15162A
    MMAE-d8 2070009-72-0 99.29%
    MMAE-d8 is a deuterated labeled MMAE, a potent mitotic inhibitor and a tubulin inhibitor.
    MMAE-d<sub>8</sub>
  • HY-13631DS
    Dxd-d5 98.84%
    Dxd-d5 is a deuterium labeled Dxd. Dxd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) [1].
    Dxd-d<sub>5</sub>
  • HY-13704S
    SN-38-d3 718612-49-8 99.07%
    SN-38-d3 is the deuterium labeled SN-38. SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively[1][2][3][4].
    SN-38-d<sub>3</sub>
  • HY-13442AS
    Eribulin-d3 mesylate
    Eribulin-d3 (mesylate) is a deuterium labeled Eribulin mesylate. Eribulin mesylate is a microtubule targeting agent that is used for the research of cancer[1][2].
    Eribulin-d<sub>3</sub> mesylate
  • HY-153891S
    Deruxtecan 2-hydroxypropanamide-d5
    Deruxtecan 2-hydroxypropanamide-d5 is a deuterated isotope of Deruxtecan 2-hydroxypropanamide (HY-153891) .
    Deruxtecan 2-hydroxypropanamide-d<sub>5</sub>
  • HY-13631AS1
    Exatecan-d3 mesylate
    Exatecan-d3 (DX8951f-d3) mesylate is deuterium-labeled Exatecan (mesylate) (HY-13631A).
    Exatecan-d<sub>3</sub> mesylate
  • HY-15579AS
    MMAF-d8 hydrochloride 99.70%
    MMAF-d8 (hydrochloride)e is a deuterated form of MMAF hydrochloride, which is a microtubule disrupting agent.
    MMAF-d<sub>8</sub> hydrochloride
  • HY-B0015S
    Paclitaxel-d5 1129540-33-5 ≥98.0%
    Paclitaxel-d5 is a deuterium-labeled Paclitaxel. Paclitaxel is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization[1].
    Paclitaxel-d<sub>5</sub>
  • HY-12454S
    DM4-d6 99.11%
    DM4-d6 is deuterium labeled DM4. DM4 is is an antitubulin agent that inhibit cell division. DM4 can be used in the preparation of antibody agent conjugate.
    DM4-d<sub>6</sub>
  • HY-15575S
    VcMMAE-d8
    VcMMAE-d8 is an isotope of VcMMAE (HY-15575). VcMMAE-d8 is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).
    VcMMAE-d<sub>8</sub>
  • HY-12522S
    PF-06380101-d8 99.37%
    PF-06380101-d8 is a deuterium labeled PF-06380101. PF-06380101, an Auristatin microtubule inhibitor, is a cytotoxic Dolastatin 10 analogue[1].
    PF-06380101-d<sub>8</sub>
  • HY-14519S
    Methotrexate-d3 432545-63-6 ≥99.0%
    Methotrexate-d3 (Amethopterin-d3) is the deuterium labeled Methotrexate. Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia)[1][2][3].
    Methotrexate-d<sub>3</sub>
  • HY-16560S
    Camptothecin-d5 1329616-37-6 99.61%
    Camptothecin-d5 is the deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM[1]. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells[2][3].
    Camptothecin-d<sub>5</sub>
  • HY-B0015S1
    Paclitaxel-d5 (benzoyloxy) 1261254-56-1 98.12%
    Paclitaxel-d5 (benzoyloxy) is the deuterium labeled Paclitaxel. Paclitaxel is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization. Paclitaxel can cause both mitotic arrest and apoptotic cell death. Paclitaxel also induces autophagy[1][2].
    Paclitaxel-d<sub>5</sub> (benzoyloxy)
  • HY-134423S
    Stearoyl coenzyme A-13C18 lithium
    Stearoyl coenzyme A-13C18 (lithium) is the 13C labeled Stearoyl coenzyme A lithium[1]. Stearoyl coenzyme A (Stearoyl-CoA) lithium is an active compound that can be used as a substrate for the determination of stearoyl-Coenzyme desaturase in microsomes[2].
    Stearoyl coenzyme A-<sup>13</sup>C<sub>18</sub> lithium
  • HY-156756S
    7-Hydroxymethyl-10,11-MDCPT-d5
    7-Hydroxymethyl-10,11-MDCPT-d5 is deuterium labeled 7-Hydroxymethyl-10,11-MDCPT, which is a is a payload that can be used for ADC synthesis.
    7-Hydroxymethyl-10,11-MDCPT-d<sub>5</sub>
  • HY-124547S
    2,4-D methyl ester-d3 2732917-35-8
    2,4-D methyl ester-d3 is the deuterium labeled Fmoc-Trp-OH[1].
    2,4-D methyl ester-d<sub>3</sub>
  • HY-124547S1
    2,4-D Methyl ester-d3-1 358731-20-1
    2,4-D Methyl ester-d3-1 is the deuterium labeled 2,4-D methyl ester[1].
    2,4-D Methyl ester-d<sub>3</sub>-1
  • HY-15581S
    MMAD-d8 98.95%
    MMAD-d8D is a deuterated form of MMAD, which is a microtubule disrupting agent.
    MMAD-d<sub>8</sub>