2. PROTAC GPCR/G Protein MAPK/ERK Pathway Stem Cell/Wnt
  3. PROTACs Ras ERK
  4. PROTAC KRAS G12D degrader 1

PROTAC KRAS G12D degrader 1 

目录号: HY-161176 纯度: 98.32%
COA 产品使用指南 技术支持

PROTAC KRAS G12D degrader 1 是一种选择性 PROTAC KRASG12D 降解剂。PROTAC KRAS G12D degrader 1 可抑制 KRASG12D 突变细胞的增殖，并抑制 ERK 磷酸化。PROTAC KRAS G12D degrader 1 可抑制携带 AsPC-1 移植瘤小鼠的肿瘤生长。PROTAC KRAS G12D degrader 1 可用于研究 KRASG12D 驱动的癌症。(粉色：KRAS 配体 (HY-175892)，蓝色：VHL 配体 (HY-112078)，黑色：连接子，E3 连接酶配体-连接子偶联物 (HY-175893))。

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

PROTAC KRAS G12D degrader 1

PROTAC KRAS G12D degrader 1 Chemical Structure

CAS No. : 3033583-54-6

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 价格 是否有货 数量
1 mg ￥3200
In-stock
5 mg 现货 询价
10 mg 现货 询价
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

PROTAC KRAS G12D degrader 1 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

查看 ERK 亚型特异性产品:

查看所有亚型
ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC KRAS G12D degrader 1 is a selective PROTAC KRASG12D degrader. PROTAC KRAS G12D degrader 1 inhibits proliferation of KRASG12D-mutant cells and suppresses ERK phosphorylation. PROTAC KRAS G12D degrader 1 inhibits tumor growth in mice bearing AsPC-1 xenografts. PROTAC KRAS G12D degrader 1 can be used for the study of KRASG12D-driven cancers.(Pink: KRAS ligand (HY-175892), Blue: VHL Ligand (HY-112078), Black: Linker, E3 ligase ligand-linker conjugate (HY-175893))[1].

IC50 & Target[1]

VHL

 

KRas G12D

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
AGS IC50
31.36 nM
Compound: 8o
Antiproliferative activity against human AGS cells harboring KRAS G12D mutant assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
Antiproliferative activity against human AGS cells harboring KRAS G12D mutant assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
[PMID: 38197882]
ASPC1 IC50
231.2 nM
Compound: 8o
Antiproliferative activity against human ASPC1 cells assessed as inhibition of cell viability incubated for 6 hrs followed by compound washout measured after 114 hrs by Cell Titer Glo assay
Antiproliferative activity against human ASPC1 cells assessed as inhibition of cell viability incubated for 6 hrs followed by compound washout measured after 114 hrs by Cell Titer Glo assay
[PMID: 38197882]
ASPC1 IC50
59.97 nM
Compound: 8o
Antiproliferative activity against human ASPC1 cells harboring KRAS G12D mutant assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
Antiproliferative activity against human ASPC1 cells harboring KRAS G12D mutant assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
[PMID: 38197882]
ASPC1 IC50
61.14 nM
Compound: 8o
Antiproliferative activity against human ASPC1 cells assessed as inhibition of cell viability incubated for 120 hrs of continuous treatment by Cell Titer Glo assay
Antiproliferative activity against human ASPC1 cells assessed as inhibition of cell viability incubated for 120 hrs of continuous treatment by Cell Titer Glo assay
[PMID: 38197882]
HPAF-II IC50
45.22 nM
Compound: 8o
Antiproliferative activity against human HPAF-II cells harboring KRAS G12D mutant assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
Antiproliferative activity against human HPAF-II cells harboring KRAS G12D mutant assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
[PMID: 38197882]
NCI-H1975 IC50
> 10000 nM
Compound: 8o
Antiproliferative activity against human NCI-H1975 cells harboring wild-type KRAS assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
Antiproliferative activity against human NCI-H1975 cells harboring wild-type KRAS assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
[PMID: 38197882]
NCI-H358 IC50
> 9000 nM
Compound: 8o
Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
[PMID: 38197882]
SNU1 IC50
43.51 nM
Compound: 8o
Antiproliferative activity against human SNU1 cells harboring KRAS G12D mutant assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
Antiproliferative activity against human SNU1 cells harboring KRAS G12D mutant assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
[PMID: 38197882]
体外研究
(In Vitro)

PROTAC KRAS G12D degrader 1 (Compound 8o) (24 h) 在 SNU-1、HPAF-II、AGS 和 PANC 04.03 细胞 (均为杂合型 KRASG12D) 中可剂量依赖性地降解 KRASG12D，其 DC50 值分别为 19.77 nM、52.96 nM、7.49 nM 和 87.8 nM[1]。
PROTAC KRAS G12D degrader 1 (1 μM, 1-24 h) 可显著降低 AsPC-1 细胞中的 KRASG12D 蛋白水平[1]。
PROTAC KRAS G12D degrader 1 (15 days) 可抑制 KRASG12D 突变细胞的增殖，包括 AsPC-1、SNU-1、HPAF-II、AGS 和 PANC 04.03，其 IC50 值分别为 59.97 nM、43.51 nM、31.36 nM、51.53 nM 和 >10000 nM[1]。
PROTAC KRAS G12D degrader 1 (1 μM, 6 h) 可在 AsPC-1 细胞中持续诱导 KRASG12D 降解，并抑制 pERK[1]。

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

PROTAC KRAS G12D degrader 1 相关抗体:
体内研究
(In Vivo)

PROTAC KRAS G12D degrader 1 (Compound 8o) (50 mg/kg，皮下注射，每日一次或每三日一次，连续 22 天) 可抑制携带 AsPC-1 移植瘤的 BALB/c 裸鼠的肿瘤生长[1]。

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

Animal Model: AsPC-1 cells (5 × 106 in 100 µL) were subcutaneously implanted into the flanks of 8-9-week-old BALB/c nude mice[1]
Dosage: 50 mg/kg
Administration: s.c., once daily or every three days, 22 days
Result: Achieved tumor growth inhibition.
Reduced KRASG12D protein level and the phosphorylation level of ERK in AsPC-1 xenograft tumor tissues.
Downregulated the mRNA level of DUSP4.
Showed no significant changes in body weight.
分子量

1103.33

Formula

C59H72F2N10O7S
CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 10 mg/mL (9.06 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.9063 mL 4.5317 mL 9.0635 mL
5 mM 0.1813 mL 0.9063 mL 1.8127 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 98.32%

COA (286 KB) HNMR (335 KB) RP-HPLC (169 KB) LCMS (234 KB)

产品使用指南 (1538 KB)
参考文献

PROTAC KRAS G12D degrader 1 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9063 mL 4.5317 mL 9.0635 mL 22.6587 mL
5 mM 0.1813 mL 0.9063 mL 1.8127 mL 4.5317 mL
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:

PROTAC KRAS G12D degrader 13033583-54-6PROTACsRasERKExtracellular signal regulated kinasesPROTACAsPC-1HPAF-IIPANCInhibitorinhibitorinhibit

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：
PROTAC KRAS G12D degrader 1
目录号：
HY-161176
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