Brentuximab vedotin

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Brentuximab vedotin

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CAS NO:

914088-09-8

维布妥昔单抗；本妥昔单抗

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。

生物活性

Brentuximab vedotin (cAC10-vcMMAE) is an antibody-drug conjugate(ADC)comprising an anti-CD30antibody and the cytotoxic agent MonomethylauristatinE (MMAE). Brentuximab vedotin inhibitsCD30-positive cells with anIC₅₀of 2.5 ng/mL. Brentuximab vedotin can be used for the research of relapsed and refractory Hodgkin lymphoma^[1]^[2].

IC₅₀& Target

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

体外研究
(In Vitro)

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 IC₅₀value 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.

体内研究
(In Vivo)

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.

Clinical Trial

性状

Solid

CAS 号

914088-09-8

中文名称

维布妥昔单抗；本妥昔单抗

储存方式

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