2. PROTAC MAPK/ERK Pathway GPCR/G Protein
  3. PROTACs Ras
  4. SIAIS562055

SIAIS562055 是一种有效的基于 cereblon 的 SOS1 PROTAC，Kd 为 95.9 nM。SIAIS562055 表现出持续降解 SOS1 和抑制下游 ERK 通路。SIAIS562055 有效阻断了 KRASG12C 或 KRASG12D 与 SOS1 的结合，IC50 值分别为 95.7 nM 和 134.5 nM。SIAIS562055 表现出强大的抗癌活性。（粉色：SOS1 配体 (HY-168638)；黑色：连接子 (HY-W539874)；蓝色：E3 连接酶配体 (HY-W076696)）。

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SIAIS562055 Chemical Structure

SIAIS562055 Chemical Structure

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SIAIS562055 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Ras 亚型特异性产品:

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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

SIAIS562055 is a potent cereblon-based SOS1 PROTAC with a Kd of 95.9 nM. SIAIS562055 exhibits sustained degradation of SOS1 and inhibition of downstream ERK pathways. SIAIS562055 effectively blocked the binding of KRASG12C or KRASG12D to SOS1, with the IC50 values of 95.7 nM and 134.5 nM, respectively. SIAIS562055 exhibits potent anticancer activity. (Pink: SOS1 ligand (HY-168638); Black: linker (HY-W539874); Blue: E3 ligase ligand (HY-W076696))[1].

IC50 & Target[1]

Cereblon

 

SOS1

95.9 nM (Kd)

体外研究
(In Vitro)

SIAIS562055 (10-1000 nM; 24 小时) 表现出持续降解 SOS1 和抑制下游 ERK 通路，具有优异的抗增殖活性[1]。

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

SIAIS562055 相关抗体:

Western Blot Analysis[1]

Cell Line: NCI-H358 and GP2d cells
Concentration: 10 nM, 100 nM, 1000 nM
Incubation Time: 24 h
Result: Exhibited sustained degradation of SOS1 and inhibition of downstream ERK pathways.
体内研究
(In Vivo)

SIAIS562055（20-50 mg/kg；腹腔注射；每日；持续 3 周）在 KRAS 突变异种移植中表现出良好的抗肿瘤效力[1]。

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

Animal Model: Female BALB/c mice (6-7-week-old) injected with MIA PaCa-2 cells[1]
Dosage: 20 mg/kg; 40 mg/kg; 50 mg/kg
Administration: ip; daily; for 3 weeks
Result: Displayed promising antitumor potency.
分子量

918.12

Formula

C49H62F3N7O5S
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

SIAIS562055 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

SIAIS562055SIAIS 562055SIAIS-562055PROTACsRasPROTAC SOS1 degraderKRASG12DKRASG12CERK pathwaysInhibitorinhibitorinhibit

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产品名称：
SIAIS562055
目录号：
HY-168637
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