5-iodo-1H-pyrazolo[3,4-b]pyrazin-3-amine cas 1392149-77-7 support customized synthesis

This is a very important molecule in the field of pharmaceutical research. Its generic name is Sotorasib, and its trade names are Lumakras (in the United States) or Lumykras (in the European Union).
Here is the detailed introduction about it:
1. Basic Information
· CAS Number: 1392149-77-7
· Generic Name: Sotorasib (Sotoralisib)
· Trade Name: Lumakras / Lumykras
· Chemical Name: (R)-1-(4-(2-(2-chloro-3-fluorobenzyl)-7-fluoro-4-oxo-3,4-dihydroquinazoline-6-yl) piperazine-1-yl)-2-hydroxyprop-2-yl-1-propenamide
· Development Code: AMG 510
2. Drug Categories and Mechanisms of Action
· Category: Small molecule targeted anti-cancer drugs
· Target: KRAS G12C
· Mechanism of action:
· The KRAS gene is one of the most common oncogenes in human cancers and has long been regarded as an "impossible-to-target" target.
· Approximately 13% of patients with non-small cell lung cancer, as well as some patients with colorectal cancer, pancreatic cancer, etc., carry the KRAS G12C mutation (i.e., a mutation where glycine at the 12th codon of the KRAS gene is replaced by cysteine).
· Sotorasib is a covalent irreversible inhibitor. It can specifically bind to the mutated cysteine residue, locking the KRAS G12C protein in an inactive GDP-bound state, thereby blocking the downstream signaling pathways that promote cell proliferation and survival, and inducing cancer cell death.
3. Indications
Sotorasib is mainly used to treat adult patients with locally advanced or metastatic non-small cell lung cancer who carry the KRAS G12C mutation and have received at least one systemic treatment previously.
4. Research and Development Milestones and Significance
· Breakthrough significance: Sotorasib is the world's first KRAS G12C inhibitor approved for market by the FDA. Its success marks a historic breakthrough in the fight against the "undruggable" target KRAS, bringing new hope to numerous cancer patients carrying this mutation.
· Approval time:
· US FDA: May 2021
· China NMPA: May 202
5. Key clinical data
In the crucial Phase II clinical trial, Sotorasib demonstrated the following in patients with advanced NSCLC who had previously received treatment and had KRAS G12C mutations:
· Objective response rate: Approximately 37.1% (i.e., the proportion of patients whose tumors shrank to a certain standard)
· Median progression-free survival: Approximately 6.8 months
· Disease control rate: Approximately 80.6%
These data demonstrate the effectiveness and controllable safety of this treatment after standard therapy failure.
6. Common Adverse Reactions
Like other anti-cancer drugs, Sotorasib can also cause side effects. The common adverse reactions include:
· Diarrhea
· Muscle and bone pain
· Nausea
· Abnormal liver function (such as elevated transaminase levels)
· Fatigue
· Cough
Most of the adverse reactions are grade 1-2 and can usually be managed through symptomatic treatment or dose adjustment.
Summary

CAS 1392149-77-7 (Sotorasib / AMG 510) is not merely a chemical substance; it represents a landmark achievement in the field of cancer targeted therapy. As the first drug to successfully target the KRAS G12C mutation, it has opened up a new therapeutic area, providing efficient and precise treatment options for cancer patients with specific genetic profiles.