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HTRF KRAS G12C / GTP Binding Kit, 500 Assay Points

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HTRF KRAS G12C / GTP Binding Kit, 500 Assay Points
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The KRAS G12C GTP binding kit is designed to identify KRAS G12C / GTP inhibitors.

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MARCH10
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Feature Specification
Application Protein-Protein Interaction
Sample Volume 2 µL
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The KRAS G12C GTP binding kit is designed to identify KRAS G12C / GTP inhibitors.

Click to copy promo code to clipboard.
March lab savings - buy on Revvity.com or Revvity punchout to SAVE 10% with promo code!
MARCH10
Sale ends 3/24. Terms and conditions apply.
View product information
Product Variants
Unit Size: 500 assay points
Part #:
64BDKRASGPEG
List Price
USD 1,306.67
Your online price:
Unit Size: 10,000 assay points
Part #:
64BDKRASGPEH
List Price
USD 15,640.42
Your online price:
For research use only. Not for use in diagnostic procedures. All products to be used in accordance with applicable laws and regulations including without limitation, consumption, and disposal requirements under European REACH regulations (EC 1907/2006).
Total list price:
USD 1,306.67
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Picture of HTRF g12c gtp binding kit
Picture of HTRF g12c gtp binding kit
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HTRF KRAS G12C / GTP Binding Kit, 500 Assay Points
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Picture of HTRF g12c gtp binding kit
Picture of HTRF g12c gtp binding kit
HTRF KRAS G12C / GTP Binding Kit, 500 Assay Points
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Product information

Overview

A fast and easy way to identify new KRAS G12C/GTP competitors.KRAS is a small GTPase implicated ous biological processes, such as cell proliferation, cell survival, and cell metabolism. This proto-oncogene is well known to be mutated in many cancer subtypes, inducing an uncontrolled proliferation and cell metabolism modifications. It thereby contributes to the Warburg effect in cancer cells. Like the majority of small GTPases, KRAS binds to GDP in its inactive form or binds to GTP to switch into active form. KRAS G12C is one of the most commonly present mutant forms in cancer which leads to a permanently active state of KRAS. ying new KRAS/ GTP competitors efore a relevant strategy rol biological processes involved in cancer growth, by reducing the KRAS activity as well as the associated pathways.

Specifications

Application
Protein-Protein Interaction
Brand
HTRF
Detection Modality
HTRF
Product Group
Kit
Sample Volume
2 µL
Shipping Conditions
Shipped in Dry Ice
Target Class
Binding Assay
Technology
TR-FRET
Therapeutic Area
Oncology & Inflammation
Unit Size
500 assay points

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HTRF KRAS G12C / GTP Binding Kit, 500 Assay Points
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HTRF KRAS G12C / GTP Binding Kit, 500 Assay Points
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How it works

Assay principle

The HTRF KRAS GTP binding assay is in a competitive assay format which uses a GTP-Red reagent as KRAS G12C ligand, a 6His tagged human KRAS G12C protein, and an anti 6His Cryptate-labeled antibody. The compound being tested competes with the GTP Red reagent, and thereby prevents FRET from occurring.

1ppi-how-it-works-assay-principle-kras-g12c-gtp-binding.svg

 

Assay protocol

The Human KRAS G12C binding assay can be run in a 96- or 384-well low volume white plate (20 µL final). As described here, samples or standards are dispensed directly into the assay plate. The human His-tagged KRAS G12C protein is then adde,d followed by the dispensing of the HTRF reagents: The anti 6His antibody labeled with Europium cryptate and the GTP-Red reagent. The reagents labelled with HTRF fluorophores may be pre-mixed and added in a single dispensing step. No washing steps are needed. The protocol can be further miniaturized or upscaled by simply resizing each addition volume proportionally.

2ppi-how-it-works-assay-protocol-htrf-kras-g12c-gtp-binding.svg

 

Assay details

 

GTP-Red reagent Kd

70nM

 

GTP-Red reagent concentration

50nM

 

KRAS GTP binding Standard (GDP) IC50

34nM

 

KRAS GTP binding Standard Ki

 

19.8nM

 

 

Assay validation

Screening of GTP competitors with human KRAS G12C protein

Various nucleotides known to be GTP competitors were added to the assay. GDP (assay standard), GTPyS, and GTP displayed the right potency, in good correlation with the literature. ATP, a non-specific nucleotide, and BAY-293, a KRAS/SOS1 inhibitor, had no effect on the assay, confirming the specificity of the kit.

3assay-validation-human-kras-g12c-gtp-binding-1.svg
4assay-validation-human-kras-g12c-gtp-binding-2.svg

 

Resources

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Application Note
KRAS GTP competitors and KRAS/SOS1 inhibitors screening with new HTRF biochemical-based assays

Screening for KRAS competitors and inhibitors with HTRF™ technology

KRAS is a proto-oncogene known to be mutated in many cancer...

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Application Note Icon
Application Note
KRAS GTP competitors and KRAS/SOS1 inhibitors screening with new HTRF biochemical-based assays

Screening for KRAS competitors and inhibitors with HTRF™ technology

KRAS is a proto-oncogene known to be mutated in many cancer...

Learn More

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