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 Pureza: 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

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Ifinatamab deruxtecan

Ifinatamab deruxtecan Estructura química

No. CAS : 2484870-92-8

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Descripciòn

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).
Ensayo clínico
No. CAS
Appearance

Liquid

Color

Colorless to light yellow

SMILES

[Ifinatamab deruxtecan]

Envío

Shipping with dry ice.

Almacenamiento

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

Pureza y Documentación

Purity: 99.29%

Referencias
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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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Nombre del producto:
Ifinatamab deruxtecan
Cat. No.:
HY-P3371
Cantidad:
MCE Japan Authorized Agent: