AD57

Names

[ CAS No. ]:
1093380-42-7

[ Name ]:
AD57

Biological Activity

[Description]:

AD57 is an orally active multikinase inhibitor, inhibits RET, BRAF, S6K and Src, with greatly reduces mTOR activity[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Src

Signaling Pathways >> MAPK/ERK Pathway >> Raf

Signaling Pathways >> MAPK/ERK Pathway >> Ribosomal S6 Kinase (RSK)

[Target]

Braf

[In Vitro]

AD57 (0.2 nM) 显著抑制了 ptc > dRetMEN2B 在果蝇幼虫中的致死率[1]。 AD57 (0.1 nM) 通过减少 erk 基因剂量提高 ptc > dRetMEN2B 在果蝇中的存活率[1]。

[In Vivo]

AD57 抑制 RETMEN2 模型中 MEN2B (MZ-CRC-1) 和 MEN2A (TT) 患者来源细胞系的生存能力[1]。 AD57 (20 mg/kg) 在常规小鼠异种移植模型中显著抑制 TT 基肿瘤生长，无明显细胞毒性[1]。

[References]

[1]. Dar AC, et al. Chemical genetic discovery of targets and anti-targets for cancer polypharmacology. Nature. 2012 Jun 6;486(7401):80-4.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₂H₂₀F₃N₇O

[ Molecular Weight ]:
455.44

Related Compounds

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