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Your Position: Home > Insights > KRAS-Targeted Therapy Fighting Uphill
KRAS-Targeted Therapy Fighting Uphill
Release time: 2022-07-14 Source: ACROBiosystems Read: 1966

Kirsten Rat Sarcoma Viral Oncogene Homolog (KRAS) is the most frequently mutated oncogene, driving in numerous cancer types including non-small-cell lung cancer (NSCLC). KRAS is considered a undruggable target due to lack of classic drug binding sites. Over the last few years, great efforts have been made to explore routes for indirect targeting of KRAS mutant cancers. Scientists has found ways to drug KRAS-mutated cancers. FDA has approved an allele-specific covalent inhibitor of KRAS (G12C), AMG510 (sotorasib) from Amgen, which was a giant step for oncology.

ACROBiosystems has developed a series of KRAS proteins, which can be used for screening and validation of small-molecule inhibitors and PROTACs in vitro, and accelerating related drug development.

Structures of KRAS surfaces targeted by KRAS mutant inhibitors

Product features

Homogeneous structure and high purity (>90%) verified by MALS

High enzymatic activity

Mutant KRAS proteins with common mutation hotspots(G12C/G12D)

Product list

MoleculeCat. No.Product Description
KRS-H5547HumanHuman KRAS Protein, His Tag
KRS-H51H3HumanHuman KRAS (2-185,G12C) Protein, His Tag (active enzyme)
KRS-H51H4HumanHuman KRAS (2-185,G12D) Protein, His Tag (active enzyme, MALS verified)

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Other related products of small-molecule PROTACs

MoleculeCat. No.Product Description
JAK1JA1-H5547Human JAK1 Protein, His Tag
Akt1AK1-H5283Human Akt1 Protein, His,Strep II Tag
Elongin B & Elongin C & VHLELL-H5595Human Elongin B&Elongin C&VHL Heterotrimer Protein, Strep II Tag&Strep II Tag&His Tag (MALS & SPR verified) 

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Assay Data

Homogeneous structure and high purity (>90%) verified by MALS
Homogeneous structure and high purity (>90%) verified by MALS

The purity of Human KRAS (2-185,G12D), His Tag (Cat. No. KRS-H51H4) is more than 90% and the molecular weight of this protein is around 24-34 kDa verified by SEC-MALS.

High enzyme activity

GTPase-Glo test Human KRAS (2-185,G12C) Protein, His Tag (active enzyme)(Cat. No. KRS-H51H3)activity, the GTP is ≤85%

GTPase-Glo test Human KRAS (2-185,G12D) Protein, His Tag (active enzyme, MALS verified)(Cat. No. KRS-H51H4)activity, the GTP is ≤95%

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