2. PROTAC MAPK/ERK Pathway GPCR/G Protein
  3. PROTACs Ras
  4. (4S)-PROTAC SOS1 degrader-1

(4S)-PROTAC SOS1 degrader-1 是一种有效的 PROTAC SOS1 降解剂。(4S)-PROTAC SOS1 degrader-1 以剂量依赖性方式降低 pERK 和 RAS-GTP 的表达水平。(4S)-PROTAC SOS1 degrader-1 在体内显著抑制肿瘤生长。

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(4S)-PROTAC SOS1 degrader-1 Chemical Structure

(4S)-PROTAC SOS1 degrader-1 Chemical Structure

CAS No. : 2913176-81-3

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(4S)-PROTAC SOS1 degrader-1 的其他形式现货产品:

Customer Review

Other Forms of (4S)-PROTAC SOS1 degrader-1:

(4S)-PROTAC SOS1 degrader-1 相关抗体

Top Publications Citing Use of Products

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K-Ras H-Ras N-Ras Ras

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target[1]

K-RAS

 

体外研究
(In Vitro)

(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[1].
(4S)-PROTAC SOS1 degrader-1 (24 h) degrades SOS1 in a dose- and time-dependent manner in NCI-H358 cells[1].
(4S)-PROTAC SOS1 degrader-1 (9.8-2500 nM; 24 h) does not induce SOS2 and KRAS degradation in NCI-H358 cells[1].
(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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

(4S)-PROTAC SOS1 degrader-1 相关抗体:

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].

MCE 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
CAS 号
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.
纯度 & 产品资料
参考文献

(4S)-PROTAC SOS1 degrader-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

(4S)-PROTAC SOS1 degrader-12913176-81-3PROTACsRasAntitumorNCI-H358 tumor xenograftsNCI-H358 cellspERKRAS-GTPKRASInhibitorinhibitorinhibit

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