Tilvestamab
(Synonyms: BGB149) 目录号 : GC68342Tilvestamab (BGB149) 是一种人源化抗 AXL 抗体，阻断 AXL 介导的细胞信号传导。Tilvestamab 在体外能显著抑制 Gas6 刺激诱导的 AXL 激活，并抑制 786-0-Luc RCC 细胞中下游 AXL 的磷酸化。Tilvestamab可用于癌症，尤其是 AXL 过度表达肾细胞癌的研究。
Cas No.:2226775-26-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Tilvestamab (BGB149) is a humanized anti-AXL antibody that blocks AXL-mediated cell signaling. Tilvestamab significantly inhibits Gas6-induced AXL activation in 786-0-Luc RCC cells and inhibits downstream AKT phosphorylation. Tilvestamab can be used in cancer research, particularly in AXL overexpressing renal cell carcinomas[1].
Tilvestamab (250 µM; 1 h) inhibits AXL phosphorylation in 786-0 cells[1].
Cell Viability Assay[1]
| Cell Line: | 786-0-Luc cells (Gas6- induced; Gas6 is a well characterized AXL ligand) |
| Concentration: | 250 µM |
| Incubation Time: | 1 h (pre-treat) |
| Result: | Drastically inhibited Gas6- induced AXL phosphorylation and decreased the level of pAKT. |
Tilvestamab (30 mg/kg; i.p.; twice a week) suppresses tumor growth by inhibiting AXL in orthotopic RCC model[1].
| Animal Model: | Female BALB/c athymic nude mice (8-week-old; orthotopic RCC model)[1]. |
| Dosage: | 30 mg/kg |
| Administration: | Intraperitoneal injection; twice a week |
| Result: | Significantly inhibited RCC growth down to about 1/3 of the volume. |
[1]. Chen TJ, et al. AXL targeting by a specific small molecule or monoclonal antibody inhibits renal cell carcinoma progression in an orthotopic mice model. Physiol Rep. 2021 Dec;9(23):e15140.
| Cas No. | 2226775-26-2 | SDF | Download SDF |
| 别名 | BGB149 | ||
| 分子式 | 分子量 | ||
| 溶解度 | 储存条件 | Store at -20°C | |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 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 | g | |
每只动物给药体积 | ul | |
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GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 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，
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 saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
AXL targeting by a specific small molecule or monoclonal antibody inhibits renal cell carcinoma progression in an orthotopic mice model
Physiol Rep 2021 Dec;9(23):e15140.PMID:34877810DOI:PMC8652404
AXL tyrosine kinase activation enhances cancer cell survival, migration, invasiveness, and promotes drug resistance. AXL overexpression is typically detected in a high percentage of renal cell carcinomas (RCCs) and is strongly associated with poor prognosis. Therefore, AXL inhibition represents an attractive treatment option in these cancers. In this preclinical study, we investigated the antitumor role of a highly selective small molecule AXL inhibitor bemcentinib (BGB324, BerGenBio), and a newly developed humanized anti-AXL monoclonal function blocking antibody Tilvestamab, (BGB149, BerGenBio), in vitro and an orthotopic RCC mice model. The 786-0-Luc human RCC cells showed high AXL expression. Both bemcentinib and Tilvestamab significantly inhibited AXL activation induced by Gas6 stimulation in vitro. Furthermore, Tilvestamab inhibited the downstream AKT phosphorylation in these cells. The 786-0-Luc human RCC cells generated tumors with high Ki67 and vimentin expression upon orthotopic implantation in athymic BALB/c nude mice. Most importantly, both bemcentinib and Tilvestamab inhibited the progression of tumors induced by the orthotopically implanted 786-0 RCC cells. Remarkably, their in vivo antitumor effectiveness was not significantly enhanced by concomitant administration of a multi-target tyrosine kinase inhibitor. Bemcentinib and Tilvestamab qualify as compounds of potentially high clinical interest in AXL overexpressing RCC.