1. Antibody-drug Conjugate/ADC Related Cell Cycle/DNA Damage Apoptosis
  2. Antibody-Drug Conjugates (ADCs) Topoisomerase Apoptosis
  3. Ifinatamab deruxtecan

Ifinatamab deruxtecan  (Synonyms: DS-7300a; MABX-9001a; I-DXd)

Cat. No.: HY-P3371 Purity: 98.98%
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Ifinatamab deruxtecan (DS-7300a) is a B7-H3-targeting Antibody-drug conjugate (ADC), which is composed of a humanized anti-B7-H3 monoclonal antibody, an enzymatically cleavable peptide-based linker, and Exatecan derivative (DXd) (HY-13631D). Ifinatamab deruxtecan is a DNA Topoisomerase I inhibitor. Ifinatamab deruxtecan induces Apoptosis. DS-7300a exerts potent antitumor activities against B7-H3-expressing tumors. against rhabdomyosarcoma, endometrial adenocarcinoma and lung adenocarcinoma. Ifinatamab deruxtecan does not exert direct immunomodulatory effects

For research use only. We do not sell to patients.

Ifinatamab deruxtecan

Ifinatamab deruxtecan Chemical Structure

CAS No. : 2484870-92-8

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Description

Ifinatamab deruxtecan (DS-7300a) is a B7-H3-targeting Antibody-drug conjugate (ADC), which is composed of a humanized anti-B7-H3 monoclonal antibody, an enzymatically cleavable peptide-based linker, and Exatecan derivative (DXd) (HY-13631D). Ifinatamab deruxtecan is a DNA Topoisomerase I inhibitor. Ifinatamab deruxtecan induces Apoptosis. DS-7300a exerts potent antitumor activities against B7-H3-expressing tumors. against rhabdomyosarcoma, endometrial adenocarcinoma and lung adenocarcinoma. Ifinatamab deruxtecan does not exert direct immunomodulatory effects[1][2][3][4]

IC50 & Target[2]

Topoisomerase I

 

In Vitro

Ifinatamab deruxtecan inhibits the growth of B7-H3-expressing cancer cells in vitro, but not of B7-H3-negative cancer cells[1].
Ifinatamab deruxtecan (6 days) potently and selectively inhibits the growth of B7-H3-expressing RH-41 and MFE-280 cancer cells in vitro, with no activity against B7-H3-negative CCRF-CEM cells[2].
Ifinatamab deruxtecan (10 μg/mL; 72 hours) induces DNA damage and apoptosis in B7-H3-expressing RH-41 cancer cells in vitro[2].

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

Western Blot Analysis[2]

Cell Line: Human rhabdomyosarcoma (RH-41) cells
Concentration: 10 μg/mL
Incubation Time: 72 h
Result: Induced phosphorylation of Chk1 (a DNA damage marker) in RH-41 cells. Induced cleavage of PARP (an apoptosis marker) in RH-41 cells.
Parmacokinetics
Species Dose Route T1/2 (Elimination)
Cynomolgus Monkey[2] 0.3 mg/kg i.v. 77.76 h
Cynomolgus Monkey[2] 1 mg/kg i.v. 122.64 h
Cynomolgus Monkey[2] 3 mg/kg i.v. 189.36 h
Cynomolgus Monkey[2] 10 mg/kg i.v. 115.44 h
In Vivo

Ifinatamab deruxtecan (3-10 mg/kg; i.v.; days 0 and 14) exerts potent dose-dependent antitumor activity against rhabdomyosarcoma xenografts in mice, achieving 90% and 98% TGI at 3 mg/kg and 10 mg/kg, respectively[2].
Ifinatamab deruxtecan (0.3-3 mg/kg; i.v.; days 0 and 14) exerts potent antitumor activity against endometrial adenocarcinoma xenografts in mice, achieving 67% TGI at 0.3 mg/kg and complete tumor growth inhibition (100% TGI) at 1 mg/kg and 3 mg/kg[2].
Ifinatamab deruxtecan (1-10 mg/kg; i.v.; days 0 and 14) exerts potent dose-dependent antitumor activity against lung adenocarcinoma xenografts in mice[2].

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

Animal Model: CAnN.Cg-Foxn1nu/CrlCrlj (lung adenocarcinoma xenograft model)[2]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: i.v.; days 0 and 14
Result: Achieved tumor growth inhibition (TGI) of 71% at 1 mg/kg compared to vehicle control group (P < 0.001).\nAchieved tumor growth inhibition (TGI) of 95% at 3 mg/kg compared to vehicle control group (P < 0.001).\nAchieved tumor growth inhibition (TGI) of 99% at 10 mg/kg compared to vehicle control group (P < 0.001).
Clinical Trial
CAS No.
Appearance

Liquid

Color

Colorless to light yellow

SMILES

[Ifinatamab deruxtecan]

Shipping

Shipping with dry ice.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Purity: 99.29%

References
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Ifinatamab deruxtecan
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