Bafetinib (NS-187) is an experimental cancer drug developed by Nippon Shinyaku and licensed to CytRx. It is an inhibitor of Lyn and Bcr-Abl. [1] It reached phase II clinical trials in 2010.

Bafetinib is an orally active Lyn/Bcr-Abl tyrosine kinase inhibitor. Bafetinib enhances the activity of several pro-apoptotic Bcl-2 homology (BH) 3-pure proteins (Bim, Bad, Bmf, and Bik) through intrinsic apoptotic pathways regulated by the Bcl-2 family, and induces apoptosis of Ph + leukemia cells. Bafetinib has antitumor activity.

Bafetinib is an orally active 2-phenylaminopyrimidine derivative with potential antineoplastic activity. INNO-406 specifically binds to and inhibits the Bcr/Abl fusion protein tyrosine kinase, an abnormal enzyme produced by Philadelphia chromosomal translocation associated with chronic myeloid leukemia (CML).

Bafetinib as a Sensitizing Agent for Cancer Chemotherapy. Bafetinib (NS-187, or INNO-406) is a BCR-ABL/Lyn dual TKI developed by Nippon Shinyaku. Bafetinib is currently under phase II clinical trials for treatment of relapsed or refractory B-cell chronic lymphocytic leukemia (B-CLL) (ClinicalTrials.gov Identifier: NCT01144260).

Bafetinib (NS-187, INNO-406) is a second-generation tyrosine kinase inhibitor in development by CytRx under license from Nippon Shinyaku for treating Bcr-Abl+ leukemia's, including chronic myelogenous leukemia (CML) and Philadelphia+ acute lymphoblastic leukemia.

巴非替尼: 一种Bcr-Abl抑制剂、LYN抑制剂药物，由LadRx Corp. (LadRx Corp.)公司最早进行研发，目前全球最高研发状态为无进展，作用机制: Bcr-Abl抑制剂 (bcr-abl酪氨酸激酶抑制剂),LYN抑制剂 (酪氨酸蛋白激酶Lyn抑制剂)，治疗领域: 肿瘤,免疫系统疾病,血液及淋巴系统疾病,泌尿生殖系统 …

2016年5月9日 · Discovered by structure-based virtual screening algorithms, bafetinib, a Bcr-Abl/Lyn tyrosine kinase inhibitor, was found to have inhibitory effects on both ABCB1- and ABCG2-mediated MDR in this...

Bafetinib是有效的双重Bcr-Abl/Lyn酪氨酸激酶选择性抑制剂。 Bafetinib抑制Abl和Lyn，IC50分别为5.8 nM和19 nM。此外, Bafetinib抑制WT Bcr-Abl自磷酸化，也抑制其下游激酶活性，作用于K562和293T 细胞时，IC50分别为11 nM 和 22 nM。在体外, Bafetinib 抑制Bcr-Abl阳性细胞系生长，包括K562, KU812, 和BaF3/wt 细胞，而对Bcr-Abl-阴性U937 细胞系增殖没有作用效果。 而且，Bafetinib作用于 Bcr-Abl点突变细胞系，如 BaF3/E255K细胞，具有抗增殖效果，这种作用 …

Bafetinib (NS-187, INNO-406) 是 CytRx 在 Nippon Shinyaku 许可下开发的第二代酪氨酸激酶抑制剂，用于治疗 Bcr-Abl + 白血病，包括慢性粒细胞白血病 (CML) 和费城 + 急性淋巴细胞白血病。

Bafetinib (INNO-406, NS-187, NS187)，又称巴氟替尼或巴非替尼，是Bcr-Abl/Lyn抑制剂，IC 50 为5.8 nM和19 nM，具有抗肿瘤活性。 产品性质