What is the Ibrutinib?

Ibrutinib is , while it's Molecular Formula is C 25 H 24 N 6 O 2 . Ibrutinib is a highly selective Bruton’s tyrosine kinase (Btk) irreversible inhibitor.

What is the CAS number for Ibrutinib?

The CAS number of Ibrutinib is 936563-96-1.

What is Ibrutinib (936563-96-1) used for?

In November 2013, the US FDA approved ibrutinib (also referred to as PCI-32765), for the treatment of patients with mantle cell lymphoma (MCL) who had received at least one prior therapy. Ibrutinib is the second oral agent approved for the treatment of MCL. It works by irreversibly inhibiting Bruton’s tyrosine kinase (Btk) leading to the inhibition of B-cell receptor signaling and resulting in the reduction of malignant B-cell proliferation and induction of cell death. Btk plays an important role in the differentiation, development, proliferation, and survival of B cells via activation of cell-cycle regulators and regulating the expression of pro- and antiapoptotic proteins. Aberrant Btk activity results in a variety of B-cell malignancies including MCL. Ibrutinib inhibits Btk by irreversibly binding to cysteine-481 in the active site thereby inhibiting phosphorylation of tyrosine-223 and affecting downstream B-cell signaling pathways. Ibrutinib is a potent inhibitor of Btk (IC50=0.5 nM) and is efficacious in canine models of B-cell lymphoma. At dose ranges of 2.5–20 mg/kg, there was full occupancy of Btk in peripheral blood and tumor tissue for 24 h. A synthetic route to ibrutinib that employs Suzuki coupling of 3-iodo-1Hpyrazolo[3,4-d]pyrimidin-4-amine with (4-phenoxyphenyl)boronic acid followed by Mitsunobu reaction with N-Boc-3-hydroxypiperidine as key steps has been reported.

What is the Ibrutinib?

Ibrutinib is , while it's Molecular Formula is C 25 H 24 N 6 O 2 . Ibrutinib is a highly selective Bruton’s tyrosine kinase (Btk) irreversible inhibitor.

What is the CAS number for Ibrutinib?

The CAS number of Ibrutinib is 936563-96-1.

What is Ibrutinib (936563-96-1) used for?

In November 2013, the US FDA approved ibrutinib (also referred to as PCI-32765), for the treatment of patients with mantle cell lymphoma (MCL) who had received at least one prior therapy. Ibrutinib is the second oral agent approved for the treatment of MCL. It works by irreversibly inhibiting Bruton’s tyrosine kinase (Btk) leading to the inhibition of B-cell receptor signaling and resulting in the reduction of malignant B-cell proliferation and induction of cell death. Btk plays an important role in the differentiation, development, proliferation, and survival of B cells via activation of cell-cycle regulators and regulating the expression of pro- and antiapoptotic proteins. Aberrant Btk activity results in a variety of B-cell malignancies including MCL. Ibrutinib inhibits Btk by irreversibly binding to cysteine-481 in the active site thereby inhibiting phosphorylation of tyrosine-223 and affecting downstream B-cell signaling pathways. Ibrutinib is a potent inhibitor of Btk (IC50=0.5 nM) and is efficacious in canine models of B-cell lymphoma. At dose ranges of 2.5–20 mg/kg, there was full occupancy of Btk in peripheral blood and tumor tissue for 24 h. A synthetic route to ibrutinib that employs Suzuki coupling of 3-iodo-1Hpyrazolo[3,4-d]pyrimidin-4-amine with (4-phenoxyphenyl)boronic acid followed by Mitsunobu reaction with N-Boc-3-hydroxypiperidine as key steps has been reported.

Product Class

936563-96-1

Product Name：Ibrutinib
Molecular Formula：C₂₅H₂₄N₆O₂
Purity：99%
Molecular Weight：440.505

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Product Details:

CasNo： 936563-96-1

Molecular Formula： C₂₅H₂₄N₆O₂

Buy High Grade Ibrutinib,Hot Sale 936563-96-1 Low Price

Molecular Formula:C₂₅H₂₄N₆O₂
Molecular Weight:440.505
Boiling Point:715.0±60.0 °C at 760 mmHg
PKA:4.09±0.30(Predicted)
Flash Point:386.2±32.9 °C
PSA：99.16000
Density:1.3±0.1 g/cm³
LogP:4.73640

Ibrutinib(Cas 936563-96-1) Usage

Description

Ibrutinib, marketed under the brand name Imbruvica, is a potent kinase inhibitor medication used in the treatment of various blood cancers and complications of allogeneic stem cell transplants. It belongs to the class of medications known as kinase inhibitors, and specifically targets Bruton's tyrosine kinase (BTK), an enzyme crucial for the survival and proliferation of certain cancer cells.

Uses

Ibrutinib is primarily indicated for the treatment of blood cancers, including:

Chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma (SLL)
Mantle cell lymphoma (MCL)
Waldenstrom's Macroglobulinemia (WM)
Diffuse large B cell lymphoma (DLBCL)
Multiple myeloma (MM)
Follicular lymphoma (FL)

Regulatory Approval

Ibrutinib was approved by regulatory agencies such as the FDA and the European Commission for the treatment of various blood cancers, including MCL and CLL/SLL.

936563-96-1 Relevant articles

Toxicities and outcomes of 616 ibrutinib-treated patients in the United States: a real-world analysis

Anthony R. Mato,1 Chadhi Nabhan,2 Meghan C. Thompson,1 Nicole Lamanna,3 Danielle M. Brander,4 Brian Hill,5 Christina Howlett,6,7 Alan Skarbnik,7 Bruce D. Cheson,8 Clive Zent,9 Jeffrey Pu,10 Pavel Kiselev,11 Andre Goy,7 David Claxton,10 Krista Isaac,12 Kaitlin H. Kennard,1 Colleen Timlin,1 Daniel Landsburg,1 Allison Winter,5 Sunita D. Nasta,1 Spencer H. Bachow,3 Stephen J. Schuster,1 Colleen Dorsey,1 Jakub Svoboda,1 Paul Barr,13,* and Chaitra S. Ujjani8,*

, Haematologica. 2018 May; 103(5): 874–879.

Six hundred sixteen ibrutinib-treated patients were identified. A total of 546 (88%) patients were treated with the commercial drug. Clinical trial patients were younger (mean age 58 versus 61 years, P=0.01) and had a similar time from diagnosis to treatment with ibrutinib (mean 85 versus 87 months, P=0.8).

The Bruton's Tyrosine Kinase (BTK) Inhibitor, Ibrutinib (PCI-32765), Has Preferential Activity in the ABC Subtype of Relapsed/Refractory De Novo Diffuse Large B-Cell Lymphoma (DLBCL): Interim Results of a Multicenter, Open-Label, Phase 2 Study

Wyndham H. Wilson MD, PhD 1, John F. Gerecitano MD, PhD 2, Andre Goy MD 3, Sven de Vos MD, PhD 4, Vaishalee P. Kenkre MD 5, Paul M. Barr MD 6, Kristie A. Blum MD 7, Andrei R. Shustov MD * 8, Ranjana H. Advani MD 9, Jason Lih PhD * 10, Mickey Williams PhD * 10, Roland Schmitz PhD * 1, Yandan Yang PhD * 1, Stefania Pittaluga MD, PhD 1, George Wright PhD * 1, Lori A. Kunkel MD 11, Jesse McGreivy MD 11, Sriram Balasubramanian PhD 11, Mei Cheng PhD * 12, Davina Moussa * 11…Louis M. Staudt MD, PhD 13

blood, Volume 120, Issue 21, 16 November 2012, Page 686

Here, we present interim results of a phase 2 study in relapsed/refractory DLBCL of ibrutinib, a first in class inhibitor of BTK, a kinase in the BCR pathway. We tested the hypothesis that ibrutinib would be more active in ABC than GCB DLBCL due to their different addiction pathways, and we assessed the association of CD79B and MYD88 mutations with response.

936563-96-1 Upstream products

814-68-6
acryloyl chloride
936563-86-9
tert-butyl 3-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carboxylate
330792-69-3
2-[(4-phenoxy-phenyl)-methoxy-methylene]-malononitrile
330792-68-2
2-[hydroxy-(4-phenoxy-phenyl)-methylene]-malononitrile