Sacituzumab tirumotecan

您当前的位置：

Sacituzumab tirumotecan (Synonyms:SKB264; MK-2870;芦康沙妥珠单抗)

目录号 : KM32920 纯度 : 97%

Data Sheet 产品使用指南

Sacituzumab tirumotecan (SKB264) 是一种抗体-药物偶联物，同时是靶向 TROP2 的拓扑异构酶 I 抑制剂载荷递送剂，其 TROP2 EC50 为 2.787 ng/mL，TROP2 Kd 为 0.3083 nM，拓扑异构酶 I IC50 为 0.7 μM。Sacituzumab tirumotecan 由人源化抗 TROP2 抗体 Sacituzumab、毒性分子和 linker 偶联物是 TL033 TFA。Sacituzumab tirumotecan 可用于转移性三阴性乳腺癌、转移性非小细胞肺癌的相关研究。

规格	价格	是否有货	数量
1mg		In-stock

加入购物车大包装询价

Other Forms of Rapamycin:

Sacituzumab tirumotecan In-stock
Propyzamide In-stock
Betazole hydrochloride In-stock
Magnoloside B In-stock
House Dust Mite Extract, from D.pteronyssinus In-stock

KKL Med 的所有产品和服务仅用于科学研究，不能被用于人体，兽医，我们也不向个人提供产品和服务。

生物活性

Sacituzumab tirumotecan (SKB264) is an antibody-drug conjugate and TROP2-directed, topoisomerase I inhibitor payload-delivering agent, with a TROP2 EC50 of 2.787 ng/mL, TROP2 Kd of 0.3083 nM, and topoisomerase I IC50 of 0.7 μM. Sacituzumab tirumotecan is composed of the humanized anti-TROP2 antibody Sacituzumab, the drug-linker conjugate for ADC is TL033 TFA. Sacituzumab tirumotecan can be used for the research of metastatic triple-negative breast cancer, and metastatic non-small cell lung cancer.

IC₅₀&Target

TROP2

2.787 ng/mL (EC₅₀)

TROP2

0.3083 nM (Kd)

TOP1

0.7 μM (IC₅₀)

体外研究

Anti-cancer Cell Cycle Regulation
Sacituzumab tirumotecan (SKB264) (treated for 72 hours) can inhibit the growth of TROP2 positive HCC1806, NCI-N87, BxPC-3, Calu-3, and NCI-H23 (TROP2+) cells, with IC50 values ranging from 1.281-18.83 nM.

Others
The EC50 of Sacituzumab tirumotecan (SKB264) binding to human TROP2 protein is 2.787 ng/mL, which is similar to its monoclonal antibody binding activity.
Sacituzumab tirumotecan can bind to TROP2 positive HCC1806 and NCI-N87 cells, with EC50 values of 11.21 nM and 6.213 nM, respectively.
Sacituzumab tirumotecan (50 μg/mL; 144 h) has stable properties in human and crab eating monkey plasma. After incubation at a concentration of 50 μ g/mL for 144 h, its drug release rate can reach 70%.
Sacituzumab tirumotecan (0.0823-2.22 nM; 120 s association, 600 s dissociation) Binding to human TROP2 protein with a Kd value of 0.3083 nM.

体内研究

Anti-cancer
Sacituzumab tirumotecan (SKB264) (1-10 mg/kg; intravenous injection; Twice a week; 6 times in total) showed a dose-dependent anti-tumor effect in the HCC1806 breast cancer CDX model, and the TGI range under the test dose was 75.6% to 105.0%.
Sacituzumab tirumotecan (1-10 mg/kg; i.v.; twice weekly; 6 times) has a stronger anti-tumor effect than IMMU-132 at the same dose in the HCC1806 breast cancer CDX model.
Sacituzumab tirumotecan (0.3-3 mg/kg; intravenous injection; Twice a week; In the NCI-N87 gastric cancer CDX model, a dose-dependent anti-tumor effect was observed with a TGI ranging from 78.4% to 151.2% at the tested dose.
Sacituzumab tirumotecan (SKB264) (0.5-5 mg/kg; i.v.; twice weekly; 6 times) showed a dose-dependent antitumor activity in the BR1282 breast cancer PDX model, and the TGI range was 44.0% to 104.8% at the test dose.
Sacituzumab tirumotecan (1-10 mg/kg; intravenous injection; Twice a week; In the TROP2 positive gastric cancer PDX model (IHC ≥ 1+), efficacy was demonstrated 6 times in total, with TGI>100% at a dose of 3 mg/kg in the tested positive model.

Animal Model:	BALB/c nude (female)
Dosage:	1, 3, 10 mg/kg
Administration:	i.v.; twice weekly; 6 times
Result:	Reported tumor growth inhibition (TGI) of 75.6% (1 mg/kg), 98.5% (3 mg/kg), and 105.0% (10 mg/kg) on day 24 after first dose.\nReported tumor growth inhibition (TGI) of 81.06% (1 mg/kg), 189.46% (3 mg/kg), and 188.86% (10 mg/kg) on day 21 after treatment initiation; these values were higher than corresponding doses of IMMU-132.

Animal Model:

BALB/c nude (female)

Dosage:

0.3, 1, 3 mg/kg

Administration:

i.v.; twice weekly; 6 times

Result:

Reported tumor growth inhibition (TGI) of 78.4% (0.3 mg/kg), 139.2% (1 mg/kg), and 151.2% (3 mg/kg) on day 24 after first dose.

Animal Model:

BALB/c nude

Dosage:

0.5, 1.5, 5 mg/kg

Administration:

i.v.; twice weekly; 6 times

Result:

Reported tumor growth inhibition (TGI) of 44.0% (0.5 mg/kg), 92.6% (1.5 mg/kg), and 104.8% (5 mg/kg) on day 24 after first dose.

Animal Model:

NCG

Dosage:

1, 3, 10 mg/kg

Administration:

i.v.; twice weekly; 6 times

Result:

Achieved tumor growth inhibition (TGI) exceeding 100% at 3 mg/kg in all three TROP2-positive models (0406022, A11068, 0501116); observed no antitumor effect in the TROP2-negative model (A19058) at 3 mg/kg.

分子量

157907 (average)

中文名称

芦康沙妥珠单抗

运输条件

Shipping with dry ice.

储存方式

-80°C, protect from light

纯度： 97%

Data Sheet

产品使用指南

暂无相关参考文献

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 0 篇科研文献

The molarity calculator equation

The dilution calculator equation

动物实验计算换算器