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HY-10997

CAS:936563-96-1

 (Synonyms  Ibrutinib;PCI32765;PCI 32765)
936563-96-1  Technical Data: Price and Availability of  Cas No:936563-96-1

Cas : 936563-96-1 M.Wt: 440.5
Cas : 936563-96-1 Formula: C25H24N6O2
Cas : 936563-96-1 Purity: >98 %
Cas : 936563-96-1 Storage: at 20℃ 2 years
Cas : 936563-96-1 Solubility: DMSO: ≥ 52 mg/mL
Cas : 936563-96-1 Name: PCI-32765
USD
1g/$540 In-stock
5mg/$50 In-stock
10mg/$65 In-stock
50mg/$120 In-stock
100mg/$150 In-stock
200mg/$240 In-stock
500mg/$440 In-stock
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>10g Get quote
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936563-96-1  Data Sheet:
 
Introduction of 936563-96-1 :
PCI-32765(Ibrutinib) is a potent and highly selective Btk inhibitor with IC50 of 0.5 nM, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc. IC50 value: 0.3 nM Target: Btk in vitro: Ibrutinib shows the potent and irreversible inhibitory effect and selectivity for Btk enzymatic activity. In BCR pathway-activated DOHH2 cell line, Ibrutinib inhibits autophosphorylation of Btk, phosphorylation of Btk's physiological substrate PLCγ, and phosphorylation of further downstream kinase, ERK with IC50 of 11 nM, 29 nM and 13 nM, respectively [1]. Ibrutinib exhibits a significant dose-dependent and time-dependent induction of cytotoxicity in chronic lymphocytic leukemia (CLL) cells. In addition, Ibrutinib induces cell death depending on caspase pathway activation and antagonizes the ability of CLL cells to proliferate after TLR signaling [2]. A recent study shows that Ibrutinib inhibits BCR-activated primary B cell proliferation with IC50 of 8 nM and results in inhibition of TNFα, IL-1β and IL-6 production in primary monocytes with IC50 of 2.6 nM, 0.5 nM and 3.9 nM, respectively [3]. in vivo: In a collagen-induced arthritis model, Ibrutinib significantly reduces clinical arthritis scores reflecting paw swelling and joint inflammation by inhibiting B-cell activation. In a MRL-Fas(lpr) lupus model, Ibrutinib reduces renal disease and autoantibody production [1]. In an adoptive transfer TCL1 mouse model of CLL, Ibrutinib (25 mg/kg/day) causes a transient early lymphocytosis, and delays CLL disease progression [4].
 
References on 936563-96-1 :
 

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