Dovitinib (TKI258) Lactate
(Synonyms:多韦替尼;4-氨基-5-氟-3-[6-(4-甲基-1-哌嗪基)-1H-苯并咪唑-2-基]-2(1H)-喹啉酮 2-羟基丙酸盐一水物;多韦替尼, TKI-258;多韦替尼Dovitinib TKI-258;多韦替尼乳酸盐;多韦替尼优势推荐量大从优;DOVI锡IB;丙酸,2-羟基-,复合物 4-氨基-5-氟-3-[6-(4-甲基-1-哌嗪基)-1H-苯并咪唑-2-基]-2(1H)-喹啉酮,水合物 (1:1:1);多维替尼)
目录号 : KG10781
CAS No. : 915769-50-5
纯度 : 98%
Description:
IC50: ~10 nmol/L for FGFR1–3
Fibroblast growth factor receptor 1 (FGFR1) and FGFR2 amplifications are observed in approximately 10% of breast cancers and are related to poor outcomes. Dovitinib (TKI258) is an oral tyrosine kinase inhibitor (TKI) against FGFR1–3, VEGFR1–3, and platelet-derived growth factor receptor (PDGFR).
In vitro: Dovitinib decreased the concentrations of pFRS2 and pERK/MAPK in a dose-dependent manner in FGFR1 amplified and FGFR2 amplified cell lines. The IC50 for cell growth inhibition was 190 and 180 nmol/L in MDA-MB-134 and SUM52, respectively. Conversely, IC50 values were more than 2,000 nmol/L in the 11 breast cancer cell lines that had neither FGFR1 nor FGFR2 amplification .
In vivo: In vivo model (HBCx-2 breast cancer primary xenograft, with 8 FGFR1 gene copies), dovitinib prevented tumor growth at the 30 mg/kg dose and caused tumor regression at the 50 mg/kg dose. Similarly, dovitinib caused tumor regression in HBCx-3 xenografts when administered at a dose of 40 mg/kg daily until day 35 .
Clinical trial: Eighty-one patients were enrolled in the trial. Unconfirmed response or stable disease for over 6 months was observed in 5 and 1 patient(s) with FGFR1-amplified/HR-positive and FGFR1-nonamplified/HR-positive breast cancer. When qPCR-identified amplifications in FGFR1, FGFR2, or FGF3 were grouped to define an FGF pathway–amplified breast cancer in HR-positive patients, the mean reduction in target lesions was 21.1% compared with a 12.0% increase in patients that did not present with FGF pathway–amplified breast cancer .
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分子式 |
C24H29FN6O5
|
分子量 |
500.52
|
CAS号 |
915769-50-5
|
中文名称 |
多韦替尼
|
储存方式 |
Store at -20°C
|