Rogaratinib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Rogaratinib 是一种成纤维细胞生长因子受体 (FGFR) 的异常抑制剂。 Rogaratinib 是一种口服、选择性、有效的 FGFR-1、-2 和 -3 激酶活性抑制剂。

Rogaratinib is an aberrant inhibitor of fibroblast growth factor receptor (FGFR). Rogaratinib is as an orally available, selective and potent inhibitor of FGFR-1, -2 and -3 kinase activity. A novel pan-FGFR inhibitor, rogaratinib, in biochemical, cellular and in vivo efficacy studies in a variety of preclinical cancer models.?In vitro kinase activity assays demonstrate that rogaratinib potently and selectively inhibits the activity of FGFRs 1, 2, 3 and 4.?In line with this, rogaratinib reduced proliferation in FGFR-addicted cancer cell lines of various cancer types including lung, breast, colon and bladder cancer.?FGFR and ERK phosphorylation interruption by rogaratinib treatment in several FGFR-amplified cell lines suggests that the anti-proliferative effects are mediated by FGFR/ERK pathway inhibition.

Of the 24 cell lines, 2 FGFR1-amplified lung cancer (LC) cell lines, H1581 and DMS114, show extreme sensitivity to Rogaratinib (BAY1163877) (GI50 values ranging from 36 to 244?nM).Treatment with Rogaratinib results in a significant decrease in colonies formed by H1581P cells, but not by H1581AR and BR cells. Ectopic expression of Met significantly induces resistance to Rogaratinib in MTT assays. Met overexpression induces activation of downstream extracellular signal-regulated kinase 1/2 (ERK1/2) and AKT, which cannot be abrogated by Rogaratinib treatment.

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BAY1163877

Angiogenesis

FGFR

FGFR

Cancer

Carcinoma, Transitional Cell

1443530-05-9

466.56

C23H26N6O3S

>98% (HPLC)

DMSO : 5.5 mg/mL (11.78 mM; Need ultrasonic)

COCC1=C(CN2CCNC(=O)C2)N2N=CN=C(N)C2=C1C1=CC2=C(S1)C(OC)=CC(C)=C2

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(-20℃)

With Ice Pack

≥ 2 years