2. PROTAC GPCR/G Protein MAPK/ERK Pathway Apoptosis
  3. PROTACs Ras Apoptosis
  4. CH091138

CH091138 是一种强效且具有选择性的 KRASG12D PROTAC 降解剂，其在 HeLa 和 AsPC-1 细胞的 DC50 值分别为 148.3 和 469.8 nM。CH091138 能依靠VHL 介导的泛素-蛋白酶体系统，选择性地降解外源性和内源性的 KRASG12D，而不降解 KRASWT 或其他 KRAS 突变体 (G12C/G12S/G12V)。CH091138 具有强大的抗肿瘤活性，可诱导肿瘤细胞凋亡 (apoptosis)。CH091138 可用于胰腺癌和结肠癌的研究。(粉色：KRASG12D 配体 (HY-175144)；蓝色：VHL E3 连接酶配体 (HY-138678)；黑色：连接物；VHL E3 连接酶配体 + 连接物 (HY-136006B))。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CH091138 Chemical Structure

CH091138 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

CH091138 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:

查看所有亚型
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

CH091138 is a potent and selective KRASG12D PROTAC degrader with DC50s of 148.3 nM in HeLa cells and 469.8 nM in AsPC-1 cells. CH091138 selectively degrades exogenous and endogenous KRASG12D but not KRASWT or other KRAS mutants (G12C/G12S/G12V), depending on the VHL-mediated ubiquitin-proteasome system. CH091138 exhibits potent anti-tumor activity and induces cancer cell apoptosis. CH091138 can be used for the study of pancreatic cancer and colon cancer. (Pink: KRASG12D ligand(HY-175144); Blue: VHL E3 ligase ligand (HY-138678); Black: Linker; VHL E3 ligase ligand + Linker (HY-136006B))[1].

IC50 & Target

KRas G12C

 

KRas G12D

 

KRas G12V

 

NEP108

3.8 μM (DC50)

体外研究
(In Vitro)

CH091138 (0-30 μM, 24 h) 能够阻断携带 KRASG12D 突变的 AsPC1 细胞中的 KRAS 下游信号通路[1]。
CH091138 (0.01-100 μM, 3 days) 在 KRASG12D 突变体 AsPC1 细胞中的 GI50 为 0.75 μM[1]。
CH091138 (1-30 μM, 24 h) 能抑制 AsPC-1 的迁移和侵袭[1]。
CH091138 (1-10 μM, 24 h-21 d) 能够抑制 AsPC-1 的集落形成，并诱导其凋亡[1]。
CH091138 (0-100 μM, 5 days) 对携带 KRASG12D 突变的患者来源的组织块 (PDOs) 的生长抑制作用比对野生型 KRAS 的组织块更强[1]。

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

CH091138 相关抗体:

Western Blot Analysis[1]

Cell Line: AsPC1-cells
Concentration: 0, 10, 30 μM
Incubation Time: 24 h
Result: Effectively inhibited KRAS-dependent downstream pathways p-AKT, p-MEK and p-ERK1/2 level.
Had no effect on other KRAS mutant cells.

Cell Viability Assay[1]

Cell Line: Patient-derived organoids (PDOs) with wild-type KRAS (COL-032-T and COL-047-T) and KRASG12D mutation (COL-018-T and COL-049-T)
Concentration: 0, 16.7 and 50 μM
Incubation Time: 5 days
Result: Exhibited an IC50 of 12.62-33.13 μM for KRASG12D PDO.
Exhibited an IC50 >50 μM for KRASWT PDO.
体内研究
(In Vivo)

CH091138 (60 mg/kg , i.p., 每 3 天 1 次，持续 29 天) 在 AsPC-1 肿瘤移植模型中具有显著的体内抗肿瘤活性，且体重变化很小[1]。

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

Animal Model: Xenograft model bearing AsPC-1 cells established in five-week-old female Balb/C nude mice[1]
Dosage: 60 mg/kg
Administration: Intraperitoneal injection (i.p.) once every three days for 29 days
Result: Achieved 61.8 % tumor growth inhibition.
Significantly decreased the average tumor weight and size.
Caused a decrease in KRAS level by up to 76.04 %.
分子量

1065.31

Formula

C59H69FN10O6S
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

CH091138 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:

CH091138CH 091138CH-091138PROTACsRasApoptosisKRASSelective KRAS G12D degraderMutant selectiveTargeted protein degradationVHL PROTACPancreatic cancerInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
CH091138
目录号：
HY-175025
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z