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KIF5B(E15)-RET(E12)-Long/BaF3

CBP73195

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I. Introduction
Cell Line Name: KIF5B(E15)-RET(E12)-Long/BaF3
Host Cell: BA/F3
Stability: 16 passages (in-house test, that not means the cell line will be instable beyond the passages we tested.)
Application: Anti-proliferation assay and PD assay
Freeze Medium: 90% FBS+10% DMSO
Complete Culture Medium: RPMI-1640+10%FBS+2ug/ml puromycin
Mycoplasma Status: Negative
 
II. Background

Chromosomal rearrangements involving the gene that encodes the RET tyrosine kinase are known oncogenic drivers in 1% to 2% of patients with non–small cell lung cancer (NSCLC). These RET rearrangements occur with characteristic partners, most commonly KIF5B, but also CCDC6, NCOA, TRIM33, CUX1, KIAA1217, FRMD4A, and KIAA1468. They are typically identified in young patients with adenocarcinoma histology and minimal smoking history. Therapeutic targeting of RET-fusion–driven NSCLCs has taken the form of treatment with broad-spectrum tyrosine kinase inhibitors with anti-RET activity, such as cabozantinib (Cabometyx; Cometriq), vandetanib (Caprelsa), lenvatinib (Lenvima), RXDX-105, and sunitinib (Sutent). Cabozantinib and vandetanib have been the most heavily studied multi-kinase inhibitors (MKIs), with response rates of 20% to 50% in largely pretreated patients with RET-rearranged NSCLC. Sunitinib has been used in fewer patients to date with initial results demonstrating a 22% response rate. RXDX-105 has exhibited uniquely impressive response rates (75%) in patients with non–KIF5B-RET-fusion NSCLC, compared with 0% response in patients with KIF5B-RET-fusion–positive NSCLC. BLU-667 has demonstrated an objective response rate of 50% in patients with RET-fusion positive NSCLC, and LOXO-292 reported a 74% ORR in patients with RET-fusion positive NSCLC. Notably, RXDX-105, BLU- 667, and LOXO-292 have all demonstrated some central nervous system activity in these early phase trials. Future directions of RET inhibition in patients with RET-rearranged NSCLC include additional clinical validation of the next generation RET-selective inhibitors RXDX-105, BLU-667, and LOXO-292 and comparing multikinase inhibitors with RET-selective inhibitors to determine the optimal sequencing of RET-targeted therapies.

 
III. Representative Data

1. WB of KIF5B-RET (K15, R12L)/BaF3

2. Anti-proliferation assay

Figure 2. CTG Proliferation Assay of BaF3 KIF5B-Ret (L) Cells (C2).

 

药靶模型联系方式: 华东销售经理:18240630236 全国销售经理:18066071954
诊断标准品联系方式: 华东销售经理:15000320447 华北销售经理:18131625521 华南销售经理:13484295986 华中&西南销售经理:13871580511 全国销售经理:13484295986

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