1. GPCR/G Protein
  2. Ras
  3. MRTX-1257

MRTX-1257 

目录号: HY-114436
产品使用指南

MRTX-1257 是选择性的、不可逆的、共价的并具有口服活性的 KRAS G12C 抑制剂,其在 H358 细胞中测得 KRAS 依赖 ERK 磷酸化的 IC50 值为 900 pM。

MCE 的所有产品仅用作科学研究,我们不为任何个人用途提供产品和服务

MRTX-1257 Chemical Structure

MRTX-1257 Chemical Structure

CAS No. : 2206736-04-9

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

Size Stock
250 mg Get quote
500 mg Get quote

* Please select Quantity before adding items.

Customer Review

Top Publications Citing Use of Products
  • 生物活性

  • 技术信息

  • 纯度 & 产品资料

  • 参考文献

Description

MRTX-1257 is a selective, irreversible, covalent and oral active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells[1].

IC50 & Target

IC50: 900 pM (KRAS dependent ERK phosphorylation in H358 cells)[1].

In Vivo

MRTX-1257 (1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg, orally, daily for 30 days) shows rapid tumor growth inhibition at all dose groups in MIA PaCa-2 G12C Xenograft model in mice[1].
MRTX-1257 shows sustained regression at 3,10, 30, and 100 mg/kg dose groups[1].
MRTX-1257 dosed of 100 mg/kg daily leads to complete responses that are maintained >70 days after cessation of treatment[1].

Animal Model: MIA PaCa-2 G12C Xenograft Model (mouse)[1].
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg.
Administration: Orally daily for 30 days.
Result: Showed rapid tumor growth inhibition at all dose groups.
Showed sustained regression at 3,10, 30, and 100 mg/kg dose groups.
100 mg/kg daily led to complete responses that are maintained >70 days after cessation of treatment.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Molecular Weight

565.71

Formula

C₃₃H₃₉N₇O₂

CAS No.

2206736-04-9

SMILES

N#CC[C@@H]1N(C(C=C)=O)CCN(C2=C3C(CN(C4=C5C(C)=CC=CC5=CC=C4)CC3)=NC(OC[C@H]6N(C)CCC6)=N2)C1

Shipping

Room temperature in continental US; may vary elsewhere

  • 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)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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:
MRTX-1257
目录号:
HY-114436
需求量:

MRTX-1257

Cat. No.: HY-114436