APS6-45

Research use only, not for human use.

APS6-45 inhibits RAS/MAPK signaling and exhibits anti-tumor activity.

APS6-45 inhibits RAS/MAPK signaling and exhibits anti-tumor activity.

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.

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), Cmax (9.7 μM) and AUC0-24 (123.7 μM?h) in mice. Animal Model:Female nude mice (6 weeks) are implanted with TT cellsDosage:10 mg/kgAdministration:P.o. daily for 30 days Result:Led to partial or complete responses in 75% and was well tolerated.Animal Model:Male ICR mice (6 weeks of age)Dosage:20 mg/kg (Pharmacokinetic Analysis)Administration:A single p.o.Result:T1/2=5.6 h, Cmax=9.7 μM,AUC0-24=123.7 μM?h.

——

MAPK/ERK Signaling

p38 MAPK

MAPK|Ras

——

——

2188236-41-9

548.4

C23H16F8N4O3

>98% (HPLC)

DMSO:240mg/mL (437.67mM)

O=C(NC)C1=NC=CC(OC2=CC=C(NC(NC3=CC(C(C(F)(F)F)(F)C(F)(F)F)=CC=C3F)=O)C=C2)=C1

——

(-20℃)

With Ice Pack

≥ 2 years