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Submit ReviewMRTX 849
说明： Mutation-selective inhibitor of KRASG12C
别名： Adagrasib
化学名： 4-[7-(8-Chloro-1-naphthalenyl)-5,6,7,8-tetrahydro-2-[[(2S)-1-methyl-2-pyrrolidinyl]methoxy]pyrido[3,4-d]pyrimidin-4-yl]-1-(2-fluoro-1-oxo-2-propen-1-yl)-(2S)-2-piperazineacetonitrile
纯度： ≥98% (HPLC)
生物活性 for MRTX 849
MRTX 849 is a mutant-selective inhibitor of KRASG12C (IC50 = 142 nM). MRTX 849 covalently binds to KRASG12C at the cysteine 12 residue and inhibits KRAS-dependent signal transduction by locking the protein in its inactive GDP-bound state. MRTX 849 induces pronounced tumor regression in 17 of 26 (65%) KRASG12C -positive cell lines and patient-derived xenograft models from multiple tumor types. It is orally bioavailable.
技术数据 for MRTX 849
| 分子量 | 604.13 |
| 公式 | C32H35ClFN7O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2326521-71-3 |
| PubChem ID | 138611145 |
| InChI Key | PEMUGDMSUDYLHU-ZEQRLZLVSA-N |
| Smiles | O(C[C@@H]1CCCN1C)C2=NC(=C3C(CN(CC3)C=4C5=C(C=CC4)C=CC=C5Cl)=N2)N6C[C@H](CC#N)N(C(C(=C)F)=O)CC6 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for MRTX 849
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 60.41 | 100 | |
| ethanol | 60.41 | 100 |
制备储备液 for MRTX 849
以下数据基于产品分子量 604.13。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.66 mL | 8.28 mL | 16.55 mL |
| 5 mM | 0.33 mL | 1.66 mL | 3.31 mL |
| 10 mM | 0.17 mL | 0.83 mL | 1.66 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.33 mL |
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产品说明书 for MRTX 849
参考文献 for MRTX 849
参考文献是支持产品生物活性的出版物。
Hallin et al (2020) The KRAS G12C inhibitor MRTX849 provides insight toward therapeutic susceptibility of KRAS-mutant cancers in mouse models and patients. Cancer Discov. 10 54 PMID: 31658955
Fell et al (2020) Identification of the clinical development candidate MRTX849, a covalent KRASG12C inhibitor for the treatment of cancer. J.Med.Chem. 63 6679 PMID: 32250617
If you know of a relevant reference for MRTX 849, please let us know.
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关键词: MRTX 849, MRTX 849 supplier, MRTX, 849, potent, mutation, selective, inhibitors, inhibits, KRASG12C, KRAS, G12C, Adagrasib, Ras, GTPases, 7488, Tocris Bioscience
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Cancer Metabolism Research Product Guide
This product guide reviews some of the main areas in cancer metabolism research and lists around 150 products that can be used to investigate metabolic pathways in cancer including:
- Glycolysis
- Tricarboxylic Acid Cycle
- Lipidogenesis
- 1C Metabolism and Nucleic Acid Synthesis
- Drivers of Metabolic Reprogramming
- pH and Redox Balance
RAS Oncoproteins Scientific Review
Written by Kirsten L. Bryant, Adrienne D. Cox and Channing J. Der, this review provides a comprehensive overview of RAS protein function and RAS mutations in cancer. Key signaling pathways are highlighted and therapeutic vulnerabilities are explored. This review also includes a detailed section on RAS drug discovery and targeting synthetic lethal interactors of mutant RAS. Compounds available from Tocris are listed.
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.
Epigenetics in Cancer Poster
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Pathways for MRTX 849
Akt Signaling Pathway
The Akt signaling pathway plays a key role in the mediation of protein synthesis, metabolism, proliferation and cell cycle progression. It may be referred to as a 'prosurvival' pathway.