BLU285 CAS No.:1703793-34-3

BLU285 – High-Quality Inhibitor for Gastrointestinal Stromal Tumors (GIST)

Introduction

Gastrointestinal Stromal Tumors (GIST) is a rare tumor that occurs in the gastrointestinal tract, presenting a range of symptoms such as abdominal pain, bleeding, and nausea. Although the exact cause of GIST remains unknown, it is believed to be caused by changes in the DNA of cells that make up the gastrointestinal tract. Currently, treatments for GIST include surgery, chemotherapy, radiation therapy, or targeted therapy. Targeted therapy specifically inhibits the activity of specific molecules responsible for cancer growth and development. BLU285 is a high-quality targeted inhibitor that has been proven to be a promising treatment for GIST.

What is BLU285 (CAS No.: 1703793-34-3)?

BLU285 is a small molecule inhibitor that was designed to specifically target KIT and PDGFRA mutated gastrointestinal stromal tumors (GISTs). It is a potent and selective inhibitor of KIT and PDGFRA kinases, and it binds to the ATP-binding pocket of these kinases to block their kinase activity. The drug has been demonstrated to be highly effective in preclinical models, and it has shown potent activity against a wide range of GIST mutations, including those that are resistant to currently available therapies.

Key Features of BLU285

Highly Selective

BLU285 is highly selective for KIT and PDGFRα kinase inhibition, which reduces the potential of off-target toxicity. It is a highly potent inhibitor of KIT and PDGFRα enzymatic activity, which are two of the most commonly mutated genes in gastrointestinal stromal tumors.

Limited Side Effects

Unlike other treatments for GIST, BLU285 has limited side effects. It does not affect cells and tissues that do not express KIT and PDGFRA, which means that it is less likely to cause off-target toxicity compared to other kinase inhibitors.

Efficient Administration

BLU285 is an oral drug that is administered in the form of a capsule or tablet. This makes the treatment highly convenient for patients, as they can take the medication at home rather than requiring hospitalization.

Proven Efficacy

BLU285 has shown highly promising results in numerous preclinical studies, with studies showing that the drug inhibits GIST cell lines in vitro and in vivo. The drug has also been shown to have activity against GIST metastases in mouse models.

Clinical Trial Data

In a phase 1 trial, BLU285 showed rapid and potent inhibition of KIT and PDGFRA kinases. The drug also demonstrated durable disease control in patients with advanced, treatment-resistant GIST. The trial showed a 40% response rate in patients with KIT exon 11 mutations, making BLU285 one of the most effective treatments currently available for this patient population.

Conclusion

BLU285 is a highly selective, potent, and promising targeted therapy for KIT and PDGFRA mutated gastrointestinal stromal tumors. It has been demonstrated to be highly effective in preclinical models and has shown promising results in clinical trials. The drug is associated with limited side effects and is administered orally, making it a highly convenient treatment option for patients. As such, BLU285 is a highly competitive drug that is likely to attract significant interest from merchants and distributors worldwide. If you are interested in our product please don't hesitate to contact us.

Chemical Structure : Avapritinib

CAS No.: 1703793-34-3

 

Avapritinib (BLU-285;BLU285)

Catalog No.: URK-V697 Only Used For Lab.

Avapritinib (BLU-285) is a potent and highly selective inhibitor of mutant KIT and PDGFRα with IC50 of 0.6, 0.27 and 0.24 nM for KIT del557-558, KIT D816V and PDGFRA D842V, respectively.

Biological Activity

Avapritinib (BLU-285) is a potent and highly selective inhibitor of mutant KIT and PDGFRα with IC50 of 0.6, 0.27 and 0.24 nM for KIT del557-558, KIT D816V and PDGFRA D842V, respectively; displays weak inhibition against WT KIT with IC50 of 73 nM, >150-fold more potent on KIT D816V than several important kinase antitargets such as VEGFR2, SRC and FLT3; inhibits other well-characterized disease-driving KIT mutants both in vitro and in vivo in preclinical models, demonstrates marked activity in patients with diseases associated with KIT and PDGFRA (GIST) activation loop mutations.
Gastric Cancer
Phase 1 Clinical

Physicochemical Properties

References

1. Cancer Discov. 2017 Dec 12. doi: 10.1158/2159-8290.

2. Evans EK, et al. Sci Transl Med. 2017 Nov 1;9(414). pii: eaao1690.

3. Cancer Discov. 2018 Jan;8(1):OF20. doi: 10.1158/2159-8290.

URK-V697_COA

URK-V697_SDS

URK-V697_TDS

 

Note: All products of Ureiko are only used for scientific research or drug certificate declaration, and we do not provide products and services for any personal use!

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