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RAS Inhibitor Screening 서비스 | Oncology 분석서비스 이미지

RAS Inhibitor Screening 서비스 | Oncology 분석서비스

암에서 가장 흔하게 변이되는 종양유전자인 RAS를 표적으로 하는 Inhibitor의 효과를 스크리닝해 드립니다.

특징  

 

  • RAS는 암에서 가장 흔하게 변이되는 종양유전자이며, isoform인 KRAS, NRAS, HRAS중에서 KRAS가 돌연변이 발생의 80% 이상을 관여합니다. KRAS G12D가 가장 우세하며, G12V와 G12C가 그 뒤를 따릅니다. 췌장암, 폐암, 대장암은 KRAS G12 mutation에 의해 유발되는 경우가 많고, 흑색종은 NRAS Q61 돌연변이와 관련이 높습니다. 
  • 최근 undruggable KRAS G12C를 druggable 표적으로 전환하는 획기적인 발전을 통해 다른 RAS 변종도 암을 치료할 수 있는 높은 치료 잠재력을 보유하고 있습니다.
  • KRAS, NRAS, HRAS 스크리닝 서비스 및 RAS Human Variant LeadHunter Panel을 제공합니다. 
  • RAS Human Variant LeadHunter Panel은 직접 및 간접 RAS inhibitor를 신속하게 식별할 수 있습니다. 



Figure 1. Demonstrative results by NEA-based RAS variant assays. A. KRAS G12D inhibitor MRTX-1133 showed > 100-fold stronger potency than BI-2865, a pan-KRAS inhibitor, in the KRAS G12D assay. B. Similar potencies were obtained between the above-mentioned two RAS inhibitors in the KRAS G12V assay. C. MRTX-1133 showed slightly left-shifted potency compared to BI-2865 in the KRAS G12R assay. AMG-510, a selective KRAS G12C inhibitor, exhibited no inhibition against these three KRAS G12 mutations. N.D.: Not detected.



Table 1. The selectivity and potency of reported KRAS and SOS1 inhibitors were successfully determined. AMG-510 and MRTX-1133 displayed selective and strong inhibition against KRAS G12C and KRAS G12D, respectively. BI-2865 displayed high potent activity across all KRAS variants compared to NRAS and HRAS. BI-3406, a SOS1 inhibitor, showed moderate inhibition against most RAS mutations. ND: Not detected at 100 μM.



Figure 2. OncoPanel RAS mutant cancer cell lines. A. Number of cancer cell lines bearing KRAS (40+), NRAS (18+), and HRAS (7+) mutations. B. Number of cancer cell lines bearing KRAS mutations including G12D (9+), G12V (10+), G12C (4+), and G13D (4+). The cell proliferation assays can be performed in 2D and 3D formats with flexible treatment designs (3-, 5-, 10-day) and multiple readouts (HCA and CTG).


분석 서비스 종류  

 

분석 종류 분석 넘버
KRAS (G12C) Human GTPase SWITCH-II Pocket ELECT Binding LeadHunter Assay - US 88-3005-1002
KRAS (G12C) Human GTPase SWITCH-II Pocket KdELECT Binding LeadHunter Assay - US 88-3007-1002
KRAS (G12D) Human GTPase SWITCH-II Pocket ELECT Binding LeadHunter Assay - US 88-3005-1003
KRAS (G12D) Human GTPase SWITCH-II Pocket KdELECT Binding LeadHunter Assay - US 88-3007-1003
KRAS (G12V) Human GTPase SWITCH-II Pocket ELECT Binding LeadHunter Assay - US 88-3005-1004
KRAS (G12V) Human GTPase SWITCH-II Pocket KdELECT Binding LeadHunter Assay - US 88-3007-1004
KRAS Human GTPase SWITCH-II Pocket KdELECT Binding LeadHunter Assay - US 88-3007-1001
KRAS G12A Human Nucleotide Exchange Assay LeadHunter Assay - TW 125965
KRAS G12C Human Nucleotide Exchange Assay LeadHunter Assay - TW 125960
KRAS G12C/SOS1 Human Protein-Protein Interaction LeadHunter Assay - TW 125940
KRAS G12D Human Nucleotide Exchange Assay LeadHunter Assay - TW 125950
KRAS G12R Human Nucleotide Exchange Assay LeadHunter Assay - TW 125946
KRAS G12S Human Nucleotide Exchange Assay LeadHunter Assay - TW 125945
KRAS G12V Human Nucleotide Exchange Assay LeadHunter Assay - TW 125944
KRAS G13C Human Nucleotide Exchange Assay LeadHunter Assay - TW 125943
KRAS G13D Human Nucleotide Exchange Assay LeadHunter Assay - TW 125942
KRAS Q61H Human Nucleotide Exchange Assay LeadHunter Assay - TW 125941
KRAS WT Human Nucleotide Exchange Assay LeadHunter Assay - TW 125970
KRAS WT/SOS1 Human Protein-Protein Interaction LeadHunter Assay - TW 125930
HRAS WT Human Nucleotide Exchange Assay LeadHunter Assay - TW 125720
NRAS WT Human Nucleotide Exchange Assay LeadHunter Assay - TW 144030
RAS Human Variant LeadHunter Panel - TW PP320

 

 

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RAS Inhibitor Screening 서비스 . . EUROFINS DISCOVERY
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EUROFINS DISCOVERY
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Product
RAS Inhibitor Screening 서비스
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0.5 ml Elite Pre-stained Protein Ladder (2 x 0.25 ml) PAL-EPL-500 0.5ml 500
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