产品
编 号：F756795
分子式：C57H76ClFN10O4S
分子量：1051.79
分子式：C57H76ClFN10O4S
分子量：1051.79
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CAS No: 2913176-81-3
产品详情
生物活性：
(4S)-PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 significantly inhibits the tumor growth in vivo.
体内研究：
PROTAC SOS1 degrader-2 (10, 20 mg/kg; i.p., daily for 21 days ) significantly inhibits the tumor growth in vivo with a good safety profile.Animal Model:BALB/c nude mice (NCI-H358 tumor xenografts)
Dosage:10, 20 mg/kg
Administration:I.p.; daily, 21 days
Result:Significantly inhibited the tumor growth in vivo with a good safety profile.
体外研究：
(4S)-PROTAC SOS1 degrader-1 (compound 9d) (0.1, 1 μM) shows a potent SOSI degradation activity with an SOS1 protein degradation of 56.2 and 92.5% at 0.1 and 1 μM in NCI-H358 cells, respectively.(4S)-PROTAC SOS1 degrader-1 (24 h) degrades SOS1 in a dose- and time-dependent manner in NCI-H358 cells.(4S)-PROTAC SOS1 degrader-1 (9.8-2500 nM; 24 h) does not induce SOS2 and KRAS degradation in NCI-H358 cells.(4S)-PROTAC SOS1 degrader-1 (7.8-2000 nM; 24 h) decreases the expression of pERK and RAS-GTP level in NCI-H358 cells in a dose-dependent manner.
(4S)-PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 significantly inhibits the tumor growth in vivo.
体内研究：
PROTAC SOS1 degrader-2 (10, 20 mg/kg; i.p., daily for 21 days ) significantly inhibits the tumor growth in vivo with a good safety profile.Animal Model:BALB/c nude mice (NCI-H358 tumor xenografts)
Dosage:10, 20 mg/kg
Administration:I.p.; daily, 21 days
Result:Significantly inhibited the tumor growth in vivo with a good safety profile.
体外研究：
(4S)-PROTAC SOS1 degrader-1 (compound 9d) (0.1, 1 μM) shows a potent SOSI degradation activity with an SOS1 protein degradation of 56.2 and 92.5% at 0.1 and 1 μM in NCI-H358 cells, respectively.(4S)-PROTAC SOS1 degrader-1 (24 h) degrades SOS1 in a dose- and time-dependent manner in NCI-H358 cells.(4S)-PROTAC SOS1 degrader-1 (9.8-2500 nM; 24 h) does not induce SOS2 and KRAS degradation in NCI-H358 cells.(4S)-PROTAC SOS1 degrader-1 (7.8-2000 nM; 24 h) decreases the expression of pERK and RAS-GTP level in NCI-H358 cells in a dose-dependent manner.
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