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PROTAC SOS1 degrader-1
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
PROTAC SOS1 degrader-1图片
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
PROTAC SOS1degrader-1 是一种有效的PROTAC SOS1激动剂，DC50为 98.4 nM。PROTAC SOS1 Degrader-1 在各种 KRAS 突变的癌细胞中显示出抗增殖活性。PROTAC SOS1 Degrader-1 具有抗肿瘤作用，且具有低毒性。
生物活性

PROTACSOS1 degrader-1 is a potentPROTACSOS1agonist with anDC50of 98.4 nM.PROTACSOS1 degrader-1 shows antiproliferation activity incancercells with various KRAS mutations.PROTACSOS1 degrader-1 shows antitumor effect with low toxicity[1].

IC50& Target

DC50: 98.4 nM (SOS1)[1]

体外研究
(In Vitro)

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[1].
PROTAC SOS1 degrader-1 (0-2000 nM; 24 h) exhibits SOS1 degradation activity with an DC50of 98.4 nM in a dose- and time-dependent manner in NCI-H358 cells[1].
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[1].
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[1].

Western Blot Analysis[1]

Cell Line:NCI-H358 cells
Concentration:0-2000 nM
Incubation Time:0-24 h
Result:Decreased the expression of SOS1 in a dose- and time-dependent manner in NCI-H358 cells.

RT-PCR[1]

Cell Line:NCI-H358 cells
Concentration:1 μM
Incubation Time:24, 48, 72 h
Result:Showed no effffect on SOS2 mRNA expression.

Cell Proliferation Assay[1]

Cell Line:NCI-H358, MIA-PaCa2, AsPC-1, SK-LU-1, SW620, A549 cells
Concentration:0-10000 nM
Incubation Time:7 days
Result:Showed anti-proliferation activity with an IC50s of 0.525, 0.218, 0.307, 0.115, 0.199, 0.232 μM and DC50s of 0.098, 0.255, 0.119, 0.104, 0.125, 0.022 μM for NCI-H358, MIA-PaCa2, AsPC-1, SK-LU-1, SW620, A549 cells, respectively.
体内研究
(In Vivo)

PROTAC SOS1 degrader-1 (10 mg/kg; i.p.) shows good PK profile with low toxicity[1].
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[1].
Pharmacokinetic Parameters of PROTAC SOS1 degrader-1 in BALB/c mice[1].

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.[1].

Animal Model:Male BALB/c mice[1]
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) and maximum concentration (Cmax= 1221 ng/mL) in mouse plasma.
Animal Model:6-8 weeks, BALB/c mice[1]
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)[1]
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)[1]
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.
分子量

1051.79

Formula

C57H76ClFN10O4S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.