WF-47-JS03 |
| カタログ番号GC61381 |
WF-47-JS03 は、KIF5B-RET トランスフェクト Ba/F3 細胞および CCDC6-RET トランスフェクト LC-2/ad 肺癌細胞に対してそれぞれ 1.7 nM および 5.3 nM の IC50 を持つ強力かつ選択的な RET キナーゼ阻害剤です。 WF-47-JS03 は、キナーゼ挿入ドメイン受容体 (KDR) に対して 500 倍を超える選択性を示します。効果的な脳浸透。
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Cas No.: 2561413-77-0
Sample solution is provided at 25 µL, 10mM.
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WF-47-JS03 is a potent and selective RET kinase inhibitor with IC50s of 1.7 nM and 5.3 nM for KIF5B-RET transfected Ba/F3 cells, CCDC6-RET transfected LC-2/ad lung cancer cells, respectively. WF-47-JS03 demonstrates >500-fold selectivity against kinase insert domain receptor (KDR). Effective brain penetration[1].
WF-47-JS03 inhibits Tel-KDR transfected Ba/F3 cells, and Ba/F3 wild-type cell lines with IC50s of 0.99 and 1.5 μM, respectively[1].
WF-47-JS03 significantly inhibits tumor growth in RIE KIF5B-RET xenograft mice and is well tolerated at 1, 3, and 10 mg/kg in the 10 day study[1]. Animal Model: Female 6-8 week old Harlan Foxn1 nude mice with RIE-RET-KIF5B transgenic cell line
[1]. Casey J N Mathison , et al. Efficacy and Tolerability of Pyrazolo[1,5- a]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma. ACS Med Chem Lett. 2020 Feb 12;11(4):558-565.
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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