1. Antibody-drug Conjugate/ADC Related Immunology/Inflammation
  2. Antibody-Drug Conjugates (ADCs) Interleukin Related
  3. Camidanlumab tesirine

Camidanlumab tesirine (ADCT 301) is an ADC comprising HuMax-TAC, a human IgG1 mAb directed against human CD25, stochastically conjugated through a dipeptide cleavable linker to a pyrrolobenzodiazepine (PBD) dimer warhead. Camidanlumab tesirine has a drug–antibody ratio (DAR) of 2.3. Camidanlumab tesirine binds human CD25 with picomolar affinity. Camidanlumab tesirine has highly potent and selective cytotoxicity against a panel of CD25-expressing human lymphoma cell lines.

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Camidanlumab tesirine Chemical Structure

Camidanlumab tesirine Chemical Structure

CAS No. : 1853239-04-9

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Description

Camidanlumab tesirine (ADCT 301) is an ADC comprising HuMax-TAC, a human IgG1 mAb directed against human CD25, stochastically conjugated through a dipeptide cleavable linker to a pyrrolobenzodiazepine (PBD) dimer warhead. Camidanlumab tesirine has a drug–antibody ratio (DAR) of 2.3. Camidanlumab tesirine binds human CD25 with picomolar affinity. Camidanlumab tesirine has highly potent and selective cytotoxicity against a panel of CD25-expressing human lymphoma cell lines[1].

In Vitro

Camidanlumab tesirine (ADCT 301; 3, 10 ng/mL; 48 hours) resultes in a dose-dependent G2-M arrest reaching a maximum at 48 hours[1].
Camidanlumab tesirine (10 ng/mL; 24-96 hours) induces apoptosis[1].
Camidanlumab tesirine has the GI50 values ranged from 0.04-2.94 ng/mL in the CD25-positive lines. GI50 values in the CD25-negative lines are >1,000 ng/mL. The nonbinding ADC gives GI50 values >1,000 ng/mL in both antigen-expressing and nonexpressing lines[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: Karpas 299 cell
Concentration: 3, 10 ng/mL
Incubation Time: 48 hours
Result: Resulted in a dose-dependent G2-M arrest reaching a maximum at 48 hours as evidenced by a decreased percentage of cells in G0-G1 and an increased percentage in G2-M compared with untreated control.

Apoptosis Analysis[1]

Cell Line: Karpas 299 cell
Concentration: 10 ng/mL
Incubation Time: 24, 48, 60, 72 and 96 hours
Result: The peak of the early apoptosis marker Annexin-V on the cell surface of Karpas 299 cells was observed between 60 and 72 hours.
In Vivo

Camidanlumab tesirine (ADCT 301; 0.1-0.6 mg/kg/day; iv; 60 days) delayed tumor growth in a dose-dependent fashion[1].
Camidanlumab tesirine has the half-life of 7.3 days by analysis of the conjugated antibody with DAR component ≥1[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6- to 8-week-old female Fox Chase SCID mice subcutaneous CD25-expressing Karpas 299 cells[1]
Dosage: 0.1, 0.2, 0.4, 0.6 mg/kg
Administration: IV; daily; 60 days
Result: Delayed tumor growth in a dose-dependent fashion with the 0.6 mg/kg cohort demonstrating 10 of 10 tumor-free survivors at day 60.
CAS No.
SMILES

[Camidanlumab tesirine]

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Camidanlumab tesirine
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HY-141599
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