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Brentuximab vedotin

(Synonyms: 维布妥昔单抗;本妥昔单抗) 目录号 : GC68296

Brentuximab vedotin (cAC10-vcMMAE) 是一种抗体-药物偶联物 (ADC),由抗 CD30 抗体和 Monomethyl auristatin E (MMAE) 组成。Brentuximab vedotin 抑制 CD30 阳性细胞,其 IC50 值为 2.5 ng/mL。Brentuximab vedotin 可用于复发难治性霍奇金淋巴瘤的研究。

Brentuximab vedotin Chemical Structure

Cas No.:914088-09-8

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5mg
¥11,250.00
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Sample solution is provided at 25 µL, 10mM.

Description

IC50: 2.5 ng/mL (CD30)[2]

Brentuximab vedotin (cAC10-vcMMAE) is an antibody-drug conjugate (ADC) comprising an anti-CD30 antibody and the cytotoxic agent Monomethyl auristatin E (MMAE). Brentuximab vedotin inhibits CD30-positive cells with an IC50 of 2.5 ng/mL. Brentuximab vedotin can be used for the research of relapsed and refractory Hodgkin lymphoma[1][2].

Brentuximab vedotin (cAC10-vcMMAE) (1 μg/mL; 96 h) shows cytotoxicity to CD30+ in Karpas 299 cells[2].
Brentuximab vedotin (CAC10-VCMMAE) (1 μg/mL; 12, 24 and 48 h) selectively induces growth arrest in G2/M phase then lead to apoptotic cell death[2].

Cell Cytotoxicity Assay[2]

Cell Line: Karpas 299 cells
Concentration: 1 μg/mL
Incubation Time: 96 h
Result: Showed cytotoxicity to CD30+ Karpas 299 cells with an IC50 value of 2.5 ng/mL.

Cell Cycle Analysis[2]

Cell Line: L540 cells
Concentration: 1 μg/mL
Incubation Time: 12, 24, and 48 h
Result: Selectively induced growth arrest in G2/M phase to apoptotic cell death.

Brentuximab vedotin (cAC10-vcMMAE) (10-120 mg/kg; i.p. for 3 weeks) the maximum tolerated dose (MTD) is between 30 and 40 mg/kg[2].
Brentuximab vedotin (cAC10-vcMMAE) (0.3, 1 mg/kg; flanks injection; every 4 days for a total of 4 doses 1 mg/kg) induces tumor CD30 regression[2].

Animal Model: SCID mice[2]
Dosage: 10 to 120 mg/kg
Administration: Intravenous injection; 10 to 120 mg/kg; for 3 weeks
Result: Showed an maximum tolerated dose between 30 and 40 mg/kg.
Animal Model: SCID mice[2]
Dosage: 0.3 and 1 mg/kg
Administration: Flanks injection; 1 mg/kg every 4 days for a total of 4 doses; 0.3 mg/kg every 4 days for a total of 4 doses
Result: Induced complete and durable tumor regression, but 0.3 mg/kg provided lower therapy than 1 mg/kg dose.

[1]. Shea L, Mehta-Shah N. Brentuximab Vedotin in the Treatment of Peripheral T Cell Lymphoma and Cutaneous T Cell Lymphoma. Curr Hematol Malig Rep. 2020 Feb;15(1):9-19.
[2]. Francisco JA, et al. cAC10-vcMMAE, an anti-CD30-monomethyl auristatin E conjugate with potent and selective antitumor activity. Blood. 2003 Aug 15;102(4):1458-65.

化学性质

Cas No. 914088-09-8 SDF Download SDF
别名 维布妥昔单抗;本妥昔单抗
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