BLU-667 (Pralsetinib) CAS No.:2097132-94-8

Introduction

BLU-667 (Pralsetinib) CAS No.:2097132-94-8 is a novel small-molecule inhibitor of RET kinase, which has been shown to be effective against a range of cancers. It is manufactured in China and is available for wholesale to merchants in countries outside of China. This product introduction will provide an overview of the key features and benefits of BLU-667 that make it an attractive option for merchants looking to expand their product line.

Key Features

1. Highly Specific Inhibition of RET Kinase

BLU-667 is a highly selective and potent inhibitor of RET kinase, a tyrosine kinase that is overexpressed in many cancers. Unlike other RET inhibitors, BLU-667 has been designed to target the mutant forms of RET more selectively, reducing toxicity and making it more effective against tumors.

2. Excellent Cellular Penetration

BLU-667 has excellent cellular penetration, allowing it to reach its target more effectively. This is particularly important for the treatment of solid tumors, which can be difficult to penetrate with other drugs.

3. Favorable Pharmacokinetics

BLU-667 has favorable pharmacokinetics, with a long half-life and low clearance rates. This means that it can be dosed less frequently and has a lower risk of toxic accumulation.

4. Broad Range of Anti-Tumor Activity

BLU-667 has shown activity against a range of tumors, including non-small cell lung cancer, colorectal cancer, and medullary thyroid cancer. This broad range of activity makes it an attractive option for merchants looking to cater to a diverse range of patients.

Benefits

1. Improved Treatment Outcomes

The primary benefit of BLU-667 is improved treatment outcomes for patients with RET-positive cancers. Clinical trials have shown that BLU-667 is effective in shrinking tumors and prolonging progression-free survival in patients with non-small cell lung cancer, colorectal cancer, and medullary thyroid cancer.

2. Reduced Toxicity

BLU-667 has been designed to be more selective in its inhibition of RET kinase, reducing the risk of toxicity compared to other RET inhibitors. This allows for higher doses and longer treatment durations, improving outcomes for patients.

3. Improved Compliance

The favorable pharmacokinetics of BLU-667 mean that it can be dosed less frequently, improving compliance and reducing the burden on patients.

4. Diverse Range of Applications

The broad range of anti-tumor activity exhibited by BLU-667 means that it has a diverse range of applications, making it an attractive option for merchants catering to different patient populations.

Conclusion

BLU-667 (Pralsetinib) CAS No.:2097132-94-8 is a highly selective and potent inhibitor of RET kinase with excellent pharmacokinetics and a broad range of anti-tumor activity. It offers improved treatment outcomes and reduced toxicity for patients with RET-positive cancers and has a diverse range of applications. Merchants looking to expand their product line should consider BLU-667 as an attractive option for meeting the needs of a diverse patient population.

Chemical Structure : BLU-667

CAS No.: 2097132-94-8

 

BLU-667 (Pralsetinib;BLU667)

Catalog No.: URK-V764 Only Used For Lab.

BLU-667 (Pralsetinib, BLU667) is a highly potent, selective, next generation RET inhibitor with IC50 of 0.3-0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion.

Biological Activity

BLU-667 (Pralsetinib, BLU667) is a highly potent, selective, next generation RET inhibitor with IC50 of 0.3-0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion.
BLU-667 displays 8- to 28-fold more potent against WT RET than cabozantinib, vandetanib, and RXDX-105; shows 88-fold selectivity over VEGFR-2, >100-fold more selective for RET over 96% of kinases in a panel of 371 kinases.
BLU-667 inhibits RET autophosphorylation with cellular IC50 of 5 nM, at least 10 times more potently than cabozantinib, vandetanib, and RXDX-105. BLU-667 inhibits phosphorylation of RET, SHC, and ERK1/2 in a panel of RET-driven cell lines at <10 nM, suppresses proliferation of KIF5B-RET Ba/F3 cells harboring V804L, V804M, or V804E variants as potently as WT RET.
BLU-667 demonstrates antitumor activity on diverse RET-driven in vivo models.

Physicochemical Properties

References

1. Subbiah V, et al. Cancer Discov. 2018 Apr 15. pii: CD-18-0338.

2. Piotrowska Z, et al. Cancer Discov. 2018 Dec;8(12):1529-1539.

URK-V764_COA

URK-V764_SDS

URK-V764_TDS

 

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