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APS6-45

CAS No. : 2188236-41-9

產(chǎn)品活性：APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity.

研究領(lǐng)域：GPCR/G Protein

作用靶點(diǎn)：Ras

In Vitro: APS6-45 (3-30 nM; 3 weeks) strongly suppresses TT human Medullary Thyroid Carcinoma (MTC) cells colony formation in a soft agar assay.
APS6-45 (1 μM; 1 h) strongly inhibits RAS pathway activity signaling in human MTC cell lines TT and MZ-CRC-1.

In Vivo: APS6-45 (10 mg/kg; p.o. daily for 30 d) inhibits growth of TT tumors in mice and does not affect body weight.
APS6-45 (0.1-160 mg/kg; a single p.o.) does not cause detectable toxic effects in mice.
APS6-45 (20 mg/kg; a single p.o.) exhibits long half-life (5.6 h), C_max (9.7 µM) and AUC_0-24 (123.7 µM?h) in mice.

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