PROTAC SOS1 degrader-2

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PROTAC SOS1 degrader-2 

PROTAC SOS1 degrader-2 是一种有效的 PROTAC SOS1 降解剂。 PROTAC SOS1 Degrader-2 以剂量依赖性方式降低 pERK 和 RAS-GTP 的表达水平。PROTAC SOS1degrader-2 在体内显著抑制肿瘤生长。

PROTAC SOS1 degrader-2

PROTAC SOS1 degrader-2 Chemical Structure

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生物活性

PROTAC SOS1 degrader-2 is a potent PROTAC SOS1 degrader. PROTAC SOS1 degrader-2 decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. PROTAC SOS1 degrader-2 significantly inhibits the tumor growth in vivo[1].

IC50 & Target[1]

K-RAS

 

体外研究
(In Vitro)

PROTAC SOS1 degrader-2 (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[1].
PROTAC SOS1 degrader-2 (24 h) degrades SOS1 in a dose- and time-dependent manner in NCI-H358 cells[1].
PROTAC SOS1 degrader-2 (9.8-2500 nM; 24 h) does not induce SOS2 and KRAS degradation in NCI-H358 cells[1].
PROTAC SOS1 degrader-2 (7.8-2000 nM; 24 h) decreases the expression of pERK and RAS-GTP level in NCI-H358 cells in a dose-dependent manner[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: NCI-H358 cells
Concentration: 7.8, 15.6, 31.2, 62.5, 125, 250, 500, 1000, 2000 nM
Incubation Time: 24 h
Result: Showed a potent degradation activity with an EC50 of 98.4 nM in NCI-H358 cells.

RT-PCR[1]

Cell Line: NCI-H358 cells
Concentration: 1 µM
Incubation Time: 24, 48, 72 h
Result: Showed the SOS2 mRNA level remained constant during the incubation period.

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: Inhibited the cell growth with IC50s of 0.525, 0.218, 0.307, 0.115, 0.199, 0.232 µM (EC50s 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-2 (10, 20 mg/kg; i.p., daily for 21 days ) significantly inhibits the tumor growth in vivo with a good safety profile[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice (NCI-H358 tumor xenografts)[1]
Dosage: 10, 20 mg/kg
Administration: I.p.; daily, 21 days
Result: Significantly inhibited the 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.
参考文献

  • [1]. Zhou C,et al. Discovery of the First-in-Class Agonist-Based SOS1 PROTACs Effective in Human Cancer Cells Harboring Various KRAS Mutations. J Med Chem. 2022; 65(5):3923-3942.

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