847925-91-1

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RO4929097

847925-91-1

Cat.No.ABP000966 Chemical NameRO4929097 MDL: MFCD18384976 MolFormulaC22H20F5N3O3 MolWeight469.408 Purity >99%

Chemical Name : RO4929097

CAS : 847925-91-1

Synonyms: N1-[(7S)-6,7-Dihydro-6-oxo-5h-dibenz[b,d]azepin-7-yl]-2,2-dimethyl-n3-(2,2,3,3,3-pentafluoropropyl)-propanediamide

Storage:at -20℃ 2 years

Biologieal

PCI-32765 is a high potent irreversible BTK inhibitor with an IC50 of 0.46 nM for the purified Btk.[1]PCI-32765 is highly active and well tolerated in CLL/SLL pts irrespective of high risk genomic abnormalities. Although follow-up is short, the high response rate and very low progression rate suggests that PCI-32765 may be an important new targeted treatment approach for CLL pts. In ex vivo assays with whole bold, PCI-32765 prevents the activation of human BCR with an IC50 of about 0.2 μM, while not influencing the activation of T cell. Treatment of CD40 or BCR activated CLL cells with PCI-32765 results in inhibition of BTK tyrosine phosphorylation and also effectively abrogates downstream survival pathways activated by this kinase including ERK1/2, PI3K, and NF-κB. In addition, PCI-32765 prevents activation-induced proliferation of CLL cells in vitro, and effectively inhibits survival signals provided externally to CLL cells from the microenvironment including soluble factors (CD40L, BAFF, IL-6, IL-4, and TNF-α), fibronectin engagement, and stromal cell contact.[2] PCI-32765 is originally developed by Pharmacyclics. And participants is been invited for the phase I clinical trials.

Reference

[1] Chang BY et al. Arthritis Res Ther. 2011 Jul 13;13(4):R115.

[2] Herman SE et al. Blood. 2011 Jun 9;117(23):6287-96.

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