Raw Material Pharmaceutical Intermediate lbrutinib Powder lbrutinib
Product Description
Product Details
| Product Name |
lbrutinib |
| Apperance |
White to off-white powder |
| CAS |
936563-96-1 |
| MF |
C25H24N6O2 |
| MW |
440.507 |
Ibrutinib is the second new drug approved through the FDA's Breakthrough Drug Channel (the first being obinutuzumab), and it also enjoys two additional buff benefits from the FDA, as well as seven years of administrative protection after its launch.
ibrutinib is a targeted anti-cancer drug jointly developed by Johnson & Johnson and Pharmacyclics. It was approved for marketing by the US Food and Drug Administration (FDA) on November 13, 2013. The trade name is Imbruvica. This drug is used for the treatment of mantle cell lymphoma (MCL). In accordance with the on behalf of Chinese chemical name of lu: 1 - [3 (R) - (4 - amino - 3 - (4 - benzene oxygen phenyl) 1 h - pyrazole and [3, 4 - d] pyrimidine - 1 - base] piperidine - 1 - base] - 2 - acrylic - 1 - ketone; English chemical name: 1-[3 (R) -[4-amino-3- (4-phenoxyphenyl) -1H-pyrazolo [3, 4-D] pyrimidin-1-yl] piperidin-1-yl]-2-propen-1-one; Molecular formula: C25H24N6O2 Molecular weight: 440.50 CAS Registration Number: 936563-96-1.
Application&Function
Purpose
Ibrutinib (PCI-32765) is an irreversible selective Btk inhibitor with an IC50 value of 0.5 nM. Ibrutinib can be used as a Btk ligand for the synthesis of a series of PROTAC molecules, such as P13I. P13I acts on human Burkitt's lymphoma RAMOS cells at concentrations of 10 and 100? At nM, 73% and 89% of Btk were degraded respectively.
Bruton Tyrosine kinase (BTK) inhibitor
Ibrutinib is a Bruton tyrosine kinase (BTK) inhibitor, used for the treatment of chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL). Both MCL and CLL belong to B-cell non-Hodgkin's lymphomas, which are difficult to cure and prone to recurrence. The commonly used chemoimmunotherapy lacks targeting, and grade 3 or 4 adverse reactions often occur. Ibrutinib can target and bind to BTK, which is necessary for the formation, differentiation, information transmission and survival of B lymphocytes, irreversibly inhibit the activity of BTK, and effectively suppress the proliferation and survival of tumor cells. Moreover, it is rapidly absorbed after oral administration, reaching the maximum blood drug concentration within 1 to 2 hours. The adverse reactions are classified as grade 1 or 2, and it will become a new option for the treatment of CLL and MCL.
On November 13, 2013, the U.S. Food and Drug Administration (FDA) accelerated the approval of Imbruvica (generic name: Ibrutinib) by Pharmacyclics and Johnson & Johnson for the treatment of a rare aggressive blood cancer - mantle cell lymphoma (MCL). Ibrutinib is a first-in-class oral Bruton's tyrosine kinase (BTK) inhibitor. It was granted Breakthrough therapy designation by the FDA in February 2013 and was approved as a treatment for MCL and CLL on November 13, 2013 and February 12, 2014, respectively. This drug selectively covalently binds to the cystine residue (Cys-481) at the active site of the target protein Btk and irreversibly inhibits BTK, thereby effectively preventing tumors from migrating from B cells to lymphoid tissues adapted to the tumor growth environment.
Specification
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