2748001-89-8

2748001-89-8 structure

Name: BT8009
Chemical Name: BT8009
CAS Number: 2748001-89-8
Molecular Formula:
Molecular Weight:
Catalog: Research Areas Cancer
Create Date: 2023-08-27 06:58:37
Modify Date: 2023-08-27 06:58:37
BT8009 is a Nectin-4 targeting toxin conjugate with a Kd value of 2.5 nmol/L for human Nectin-4 (hNectin-4) extra-cellular domain (ECD). BT8009 consists of a Nectin-4-binding bicyclic peptide, a cleavable linker system and monomethylauristatin E (MMAE). BT8009 can be used for the research of advanced and metastatic urothelial cancer[1].

Name	BT8009

Description	BT8009 is a Nectin-4 targeting toxin conjugate with a Kd value of 2.5 nmol/L for human Nectin-4 (hNectin-4) extra-cellular domain (ECD). BT8009 consists of a Nectin-4-binding bicyclic peptide, a cleavable linker system and monomethylauristatin E (MMAE). BT8009 can be used for the research of advanced and metastatic urothelial cancer[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Others >> Others
In Vitro	BT8009 与 MDA-MB-468 细胞膜上表达的内源性 Nectin-4 具有 “表观亲和性” 结合浓度为 12.9 nmol/L[1]。
In Vivo	BT8009 (1，2 和 3 mg/kg；静脉注射，每周 1 次，5 次) 在三阴性乳腺癌和非小细胞肺癌小鼠异种移植物模型中显示出抗肿瘤作用[1]。 BT8009 对大鼠的最大耐受剂量 (MTD) 为 5 mg/kg，非人灵长类动物为 1.5 mg/kg 在 5 周剂量的条件下[1]。 Animal Model: CDX (triple-negative breast cancer) mouse models and PDX (non–small cell lung) xenograft mouse models[1] Dosage: 1, 2 and 3 mg/kg Administration: Intravenous injection, 1, 2 and 3 mg/kg , once a week for 5 doses Result: Dose-dependently inhibited tumor growth in CDX and PDX models, and showed full tumor regressions at the dose of 3 mg/kg with no tumor regrowth in subsequent weeks without treatment.
References	[1]. Rigby M, et al. BT8009; A Nectin-4 Targeting Bicycle Toxin Conjugate for Treatment of Solid Tumors. Mol Cancer Ther. 2022 Dec 2;21(12):1747-1756.

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