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编 号：F756797
分子式：C57H76ClFN10O4S
分子量：1051.79
分子式：C57H76ClFN10O4S
分子量：1051.79
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CAS No: 2913185-35-8
产品详情
生物活性：
PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity.
体内研究：
PROTAC SOS1 degrader-1 (10 mg/kg; i.p.) shows good PK profile with low toxicity.PROTAC SOS1 degrader-1 (0, 10, 20 mg/kg; i.p.; once a day for 3 weeks) shows significant anti-tumor activities in the xenograft mouse model.Pharmacokinetic Parameters of PROTAC SOS1 degrader-1 in BALB/c mice.compounddose (mg/kg)T1/2 (h) Tmax (h) Cmax (ng/mL) AUClast (h*ng/mL) AUCINF (h*ng/mL)MRTINF-obs(h)
9d108.64±0.310.250v±01221±1323895±3354420±36310.2±0.4
Male BALB/c mice; 10 mg/kg for i.p..Animal Model:Male BALB/c mice
Dosage:10 mg/kg (dissolved in solution containing dimethyl sulfoxide, PEG400, and 10%hydroxypropyl-β-cyclodextrin in water (5/5/90, v/v/v))
Administration:I.p.
Result:Showed good PK profile with high exposure (AUC0?∞ = 4420 h*ng/mL) andmaximum concentration (Cmax = 1221 ng/mL) in mouse plasma.
Animal Model:6-8 weeks, BALB/c mice
Dosage:0, 10, 20 mg/kg
Administration:I.p.; once a day for a week
Result:Showed low toxicity for mouse.
Animal Model:6-8 weeks, BALB/c nude mice (NCI-H358 tumor xenografts)
Dosage:0, 10, 20 mg/kg
Administration:I.p.; once a day for 3 weeks;
Result:Inhibited the tumor growth by 72.5 and 86.1% at 10 and 20 mg/kg, respectively.
Animal Model:6-8 weeks, BALB/c nude mice (NCI-H358 tumor xenografts)
Dosage:0, 20, 50 mg/kg
Administration:Intratumoral injection; twice-weekly for 5 weeks
Result:Significantly prevented tumor growth in vivo with a good safety profile.
体外研究：
PROTAC SOS1 degrader-1 (compound 9d) (0.1, 1 μM) shows SOSI degradation activity with an SOS1 protein degradation of 56.2 and 92.5% at 0.1 and 1 μM, respectively.PROTAC SOS1 degrader-1 (0-2000 nM; 24 h) exhibits SOS1 degradation activity with an DC50 of 98.4 nM in a dose- and time-dependent manner in NCI-H358 cells.PROTAC SOS1 degrader-1 (0-2500 nM; 24 h) dose-dependently reduced the SOS1 protein level but showed no effect on SOS2 and KRAS up to 2.5 μM in NCI-H358 and AsPc-1 cells.PROTAC SOS1 degrader-1 (0-2000 nM; 24 h) reduces the expression of KRAS-GTP, induced ERK phosphorylation with an IC50value of 72.3 nM, and significantly increases the pERK level after 6-24 h.
PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity.
体内研究：
PROTAC SOS1 degrader-1 (10 mg/kg; i.p.) shows good PK profile with low toxicity.PROTAC SOS1 degrader-1 (0, 10, 20 mg/kg; i.p.; once a day for 3 weeks) shows significant anti-tumor activities in the xenograft mouse model.Pharmacokinetic Parameters of PROTAC SOS1 degrader-1 in BALB/c mice.compounddose (mg/kg)T1/2 (h) Tmax (h) Cmax (ng/mL) AUClast (h*ng/mL) AUCINF (h*ng/mL)MRTINF-obs(h)
9d108.64±0.310.250v±01221±1323895±3354420±36310.2±0.4
Male BALB/c mice; 10 mg/kg for i.p..Animal Model:Male BALB/c mice
Dosage:10 mg/kg (dissolved in solution containing dimethyl sulfoxide, PEG400, and 10%hydroxypropyl-β-cyclodextrin in water (5/5/90, v/v/v))
Administration:I.p.
Result:Showed good PK profile with high exposure (AUC0?∞ = 4420 h*ng/mL) andmaximum concentration (Cmax = 1221 ng/mL) in mouse plasma.
Animal Model:6-8 weeks, BALB/c mice
Dosage:0, 10, 20 mg/kg
Administration:I.p.; once a day for a week
Result:Showed low toxicity for mouse.
Animal Model:6-8 weeks, BALB/c nude mice (NCI-H358 tumor xenografts)
Dosage:0, 10, 20 mg/kg
Administration:I.p.; once a day for 3 weeks;
Result:Inhibited the tumor growth by 72.5 and 86.1% at 10 and 20 mg/kg, respectively.
Animal Model:6-8 weeks, BALB/c nude mice (NCI-H358 tumor xenografts)
Dosage:0, 20, 50 mg/kg
Administration:Intratumoral injection; twice-weekly for 5 weeks
Result:Significantly prevented tumor growth in vivo with a good safety profile.
体外研究：
PROTAC SOS1 degrader-1 (compound 9d) (0.1, 1 μM) shows SOSI degradation activity with an SOS1 protein degradation of 56.2 and 92.5% at 0.1 and 1 μM, respectively.PROTAC SOS1 degrader-1 (0-2000 nM; 24 h) exhibits SOS1 degradation activity with an DC50 of 98.4 nM in a dose- and time-dependent manner in NCI-H358 cells.PROTAC SOS1 degrader-1 (0-2500 nM; 24 h) dose-dependently reduced the SOS1 protein level but showed no effect on SOS2 and KRAS up to 2.5 μM in NCI-H358 and AsPc-1 cells.PROTAC SOS1 degrader-1 (0-2000 nM; 24 h) reduces the expression of KRAS-GTP, induced ERK phosphorylation with an IC50value of 72.3 nM, and significantly increases the pERK level after 6-24 h.
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