Raw Powder API Imatinib, a white powder, has the chemical formula: C29H31N7O, molecular weight: 493.60, melting point: 113℃, boiling point: 451℃, and density of 1.30 g/cm³. Imatinib is a tyrosine kinase inhibitor, a small molecule protein kinase inhibitor, which can block one or more protein kinases. It is clinically used to treat chronic myeloid leukemia and malignant gastrointestinal stromal tumors.
What is Imatinib?
Raw Powder API Imatinib is an oral drug used to treat adult patients with Philadelphia chromosome (Ber-Abl) positive chronic myelogenous leukemia (CML) in the acute phase, accelerated phase, and chronic phase after interferon treatment failure. CML is a hematopoietic stem cell disease caused by abnormal DNA of stem cells in the bone marrow. Abnormal DNA will produce abnormal protein, interfere with the normal process of leukocyte formation in bone marrow, and eventually lead to a sharp increase in leukocyte number. CML can be divided into three stages: chronic stage, accelerated stage, and crisis stage. The average survival time of patients in the crisis stage is only 2-3 months. Imatinib is also effective in the treatment of gastrointestinal stromal tumors, and the effective rate is about 50%.
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| Real shot pictures of Imatinib powder | Imatinib structure diagram |
The development history of Imatinib:
Protein kinase regulates almost all aspects of cell life, and the change in its expression or gene mutation will lead to cancer and other diseases. For example, the classic MAP kinase cascade mutation can lead to cancer. Since imatinib went on the market in 2001, kinase inhibitors have gone through 20 years. Whether protein kinase can be used as a drug target has been doubted by many pharmaceutical companies before. Until 1998, imatinib entered clinical trials, which changed people's view of protein kinase as a drug target. Since then, hundreds of protein kinase inhibitors have been developed and tested in humans, thus opening the era of targeted drug development.
In 2001, imatinib, the first kinase inhibitor, was approved by FDA.
How does Imatinib work?
Raw Powder API Imatinib, a derivative of Phenylpyrimidine, is a new tyrosine kinase inhibitor. About 95% of patients with chronic leukemia and CML have positive ph chromosome, that is, the proto-oncogene ABL on chromosome 9 is ectopic to the oncogene on chromosome 22 called breakthrough clustering region, BCR, and the two genes recombine together to produce the fusion protein p-210, which has higher tyrosine kinase activity than the normal C-ABL protein p-150. It can strongly inhibit the activity of ABL tyrosine kinase in vivo and in vitro, specifically inhibiting the expression of ABL and the proliferation of BCR-ABL cells, so it can be used to treat CML. In addition, it can also inhibit tyrosine kinases of platelet-derived growth factor, PDGF, stem cell factor, and SCF receptor, and inhibit biochemical reactions mediated by PDGF and SCF, but it does not affect the signal transduction of other stimulating factors.
What are the precautions for using Imatinib?
1. The liver function (including transaminase, serum bilirubin, and alkaline phosphatase) should be checked before treatment, and it can be rechecked once a month later.
2. The blood routine should be checked weekly in the first month of treatment and once every 2 weeks in the second month.
3. It is recommended to monitor weight regularly.
Who can't use Imatinib?
1. People who are allergic to this product are forbidden.
2. Use caution for patients with hepatic insufficiency.
3. Use caution in patients with severe heart failure.
4. Animal experiments show that this product is teratogenic, and there is still a lack of medication information for pregnant women, so pregnant women should use it with caution.
5. The distribution of human and animal milk that can be secreted in large quantities in human milk is not clear, so lactating women should use it with caution.
6. Use caution in patients with myelosuppression.
7. Use caution in patients with a viral or bacterial infection.
8. Use caution for patients with gastrointestinal dysfunction.
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Note: This compound should be used for research purposes only. These claims have not been evaluated by the Food and Drug Administration. Please consult your doctor and learn about available studies before using them. This product is not intended to diagnose, treat, cure or prevent any disease.
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