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Lonafranib

Chemical Structure : Lonafranib

CAS No.: 193275-84-2

Lonafranib (SCH 66336)

Catalog No.: PC-20251Not For Human Use, Lab Use Only.

Lonafranib (SCH 66336) is a potent, selective and orally active farnesyl protein transferase (FPT) inhibitor with IC50 of 1.9 nM, 5.2 nM and 2.8 nM for H-ras, K-ras-4B and N-ras, respectively.

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Biological Activity

Lonafranib (SCH 66336) is a potent, selective and orally active farnesyl protein transferase (FPT) inhibitor with IC50 of 1.9 nM, 5.2 nM and 2.8 nM for H-ras, K-ras-4B and N-ras, respectively.
SCH 66336 potently inhibits Ha-Ras processing in whole cells and blocks the transformed growth properties of fibroblasts and human tumor cell lines expressing activated Ki-Ras proteins.
SCH 66336 also blocked anchorage-independent growth of many human tumor lines that lack an activated ras oncogene.
SCH 66336 cauesed significant tumor regression in Ha-Ras transgenic mouse model.

Physicochemical Properties

M.Wt 559.62
Formula C31H31F2N5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-((S)-4-acryloyl-2-methylpiperazin-1-yl)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(2-isopropyl-4-methylpyridin-3-yl)-1,8-naphthyridin-2(1H)-one

References

1. Liu M, et al. Cancer Res. 1998 Nov 1;58(21):4947-56.

2. Njoroge FG, et al. J Med Chem. 1998 Nov 19;41(24):4890-902.

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