5-Bromo-1H-pyrazolo[3,4-b]pyridin-3-amine cas 405224-24-0 support customized

1. Basic Information
· CAS Number: 405224-24-0
· Generic Name: Palbociclib (Pabociclib)
· Trade Name: Ibrance (Ibrance)
· Chemical Name: 6-Acetyl-8-cyclopentyl-5-methyl-2-([5-(1-piperazinyl)-2-pyridyl]amino)pyridin-2-ylidenepyrrolo[2,3-d]pyrimidine-7(8H)-one
· Development Code: PD-0332991
2. Drug Categories and Mechanisms of Action
· Category: Small molecule targeted anti-cancer drugs
· Target: Cyclin-dependent kinase 4 and 6
· Mechanism of action:
· During the cell division cycle, CDK4/6 are key positive regulators. They bind to cyclin D and promote the cell to move from the G1 phase to the S phase, thereby initiating cell division.
· In many cancers, especially hormone receptor-positive breast cancer, the activity of CDK4/6 is abnormally excessive, leading to unlimited proliferation of cancer cells.
· Palbociclib is a highly selective CDK4/6 inhibitor. It inhibits the activity of CDK4/6, blocks the phosphorylation of RB protein, causes the cell cycle to stall at the G1 phase, and thereby inhibits the DNA synthesis and proliferation of cancer cells.
3. Indications
Pabossine is mainly used for the treatment of locally advanced or metastatic breast cancer with hormone receptor positivity and HER2 negativity.
· When used in combination with endocrine therapy:
· In combination with aromatase inhibitors, as the initial endocrine treatment for postmenopausal women.
· In combination with fulvestrant, for patients whose condition progresses despite endocrine treatment.
4. Research and Development Milestones and Significance
· Breakthrough significance: Pabossine is the world's first CDK4/6 inhibitor approved by the FDA. Its emergence has significantly transformed the treatment landscape for HR+/HER2- advanced breast cancer, shifting the treatment model from simple endocrine therapy to the era of "endocrine therapy + CDK4/6 inhibitor" combination therapy, and significantly prolonging the progression-free survival of patients.
· Approval time:
· US FDA: February 2015 (approved through accelerated approval process, then converted to full approval)
· China NMPA: July 2018
5. Key clinical data
In the key clinical trial named PALOMA series, the combination of palbociclib and letrozole/fulvestrant demonstrated remarkable efficacy compared to the use of endocrine therapy alone:
· Progression-free survival doubled: Significantly reduced the risk of disease progression or death by approximately 50%. The median progression-free survival was extended from approximately 14 months to over 24 months (specific data varies depending on the number of clinical trial lines).
· High objective response rate: Significantly increased the rate of tumor shrinkage.
6. Common Adverse Reactions
The most common adverse reaction of Pabossine is closely related to its mechanism of action (inhibiting the cell cycle), and it mainly manifests as bone marrow suppression:
· Neutropenia: This is the most common and serious adverse reaction, and regular monitoring of blood counts is necessary.
· Leukopenia
· Fatigue
· Nausea
· Hair loss
· Diarrhea
· Oral inflammation
It should be noted that neutropenia is usually manageable and can recover after suspending the medication or reducing the dosage. The incidence of febrile neutropenia is relatively low.
Summary

CAS 405224-24-0 (Palbociclib / Palbociclib) is a benchmark drug in the field of tumor-targeted therapy. As the pioneering product of CDK4/6 inhibitors, it successfully transformed the basic scientific understanding of the cell cycle into an efficient cancer treatment, providing more effective and innovative treatment options for countless patients with hormone receptor-positive breast cancer.
Important Note: The above information is provided for general knowledge only and should not replace professional medical advice. Any decisions regarding disease diagnosis and treatment plans must be made in consultation with qualified doctors.