Tamatinib - Names and Identifiers
Name | R406
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Synonyms | R406 CS-735 Tamatinib R406 tosilate R406(benzenesulfonate) 6-[[5-Fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-2H-pyrido[3,2 6-(5-fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dimethyl-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one benzenesulfonate 6-[[5-Fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-2H-pyrido[3,2-b]-1,4-oxazin-3(4H)-one benzenesulfonate
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CAS | 841290-81-1
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Tamatinib - Physico-chemical Properties
Molecular Formula | C28H29FN6O8S
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Molar Mass | 628.6286632 |
In vitro study | R406 strongly inhibits Immunoglobulin E (IgE) and IgG-regulated receptor signaling activity. R406 inhibits IgE antibody-induced production and release of LTC4, cytokines, and chemokines, including TNFα, IL-8, and GM-CSF. R406 inhibits activation of T-cell Syk substrate linker protein in mast cells and phosphorylation of B- cell linker protein/SLP65 in B- cells. R406 binds to the ATP-binding pocket of Syk, which is a competitive inhibitor of ATP, and inhibits the kinase activity of Syk, with K I of 30 nM. R406 blocks Syk-dependent FcR regulatory activity in monocytes/macrophages and neutrophils and BCR regulatory activity in B lymphocytes. 406 significantly induced apoptosis of chronic lymphocytic leukemia (CCL) cells, and blocked the secretion of CCL3 and ccl4. R406 effectively inhibits platelet signaling and inhibits the function of plasma formed by Fc gamma RIIA cross-binding in patients using specific antibodies or HIT. |
In vivo study | In mice that had been prophylactically treated, a positive Arthus reaction was performed, and 5 mg/kg R406 induced 86% of the murine skin lesions. R406 acts on the antibody-induced arthritis mouse model and also effectively inhibits inflammation. During the autoimmune reaction, R406 did not affect the function of macrophages and neutrophils, and the immunotoxicity was the lowest. |
Tamatinib - Introduction
R406, also known as PFI-2, is a chemical. The following is a description of its nature, use, preparation and safety information:
Nature:
The chemical formula of PFI-2 is C31H30F3N7O7S, and its appearance is a white solid. It is a potent and highly selective inhibitor that inhibits the catalytic activity of the enzyme body development-related protein CBP/P300.
Use:
PFI-2 are mainly used in research fields, especially in cancer treatment and tumor research. As an inhibitor, it can be used to study the function of CBP/p300 enzyme development-related proteins and the treatment mechanism of related diseases.
Preparation Method:
The production method of the PFI-2 is not disclosed, so the specific production method cannot be understood for the time being.
Safety Information:
Regarding PFI-2 safety information, due to its use in the research field, no relevant safety data exists. During operation and use, the laboratory's safe operating procedures should be followed and appropriate protective equipment should be worn. For further safety information on the substance, it is recommended to refer to the relevant safety data sheet.
Last Update:2024-04-10 22:29:15