Duvelisib - CAS 1201438-56-3
Catalog number: B0084-462545
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C22H17ClN6O
Molecular Weight:
416.869
COA:
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Targets:
PI3K
Description:
Duvelisib, also known as IPI-145 and INK-1197, is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities. Upon administration, PI3K delta/gamma inhibitor IPI 145 prevents the activation of the PI3K delta/gamma-mediated signaling pathways which may lead to a reduction in cellular proliferation in PI3K delta/gamma-expressing tumor cells. Unlike other isoforms of PI3K, the delta and gamma isoforms are overexpressed primarily in hematologic malignancies and inflammatory and autoimmune diseases. By selectively targeting these PI3K isoforms, PI3K signaling in normal, non-neoplastic cells is minimally or not affected which would result in a more favorable side effect profile.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-462545 100 mg $228 In stock
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Appearance:
white solid powder
Synonyms:
IPI145; IPI 145; IPI-145. INK-1197; INK 1197; INK1197; Duvelisib.
MSDS:
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Application:
For research used only
InChIKey:
SJVQHLPISAIATJ-ZDUSSCGKSA-N
InChI:
InChI=1S/C22H17ClN6O/c1-13(28-21-19-20(25-11-24-19)26-12-27-21)17-10-14-6-5-9-16(23)18(14)22(30)29(17)15-7-3-2-4-8-15/h2-13H,1H3,(H2,24,25,26,27,28)/t13-/m0/s1
Canonical SMILES:
CC(C1=CC2=C(C(=CC=C2)Cl)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5
Current Developer:
Infinity Pharmaceuticals, Inc. and Intellikine
1.The phosphoinositide-3-kinase (PI3K)-delta and gamma inhibitor, IPI-145 (Duvelisib), overcomes signals from the PI3K/AKT/S6 pathway and promotes apoptosis in CLL.
Balakrishnan K1,2, Peluso M3, Fu M2, Rosin NY2, Burger JA2, Wierda WG2, Keating MJ2, Faia K3, O'Brien S2, Kutok JL3, Gandhi V1,2. Leukemia. 2015 Sep;29(9):1811-22. doi: 10.1038/leu.2015.105. Epub 2015 Apr 28.
The functional relevance of the B-cell receptor (BCR) and the evolution of protein kinases as therapeutic targets have recently shifted the paradigm for treatment of B-cell malignancies. Inhibition of p110δ with idelalisib has shown clinical activity in chronic lymphocytic leukemia (CLL). The dynamic interplay of isoforms p110δ and p110γ in leukocytes support the hypothesis that dual blockade may provide a therapeutic benefit. IPI-145, an oral inhibitor of p110δ and p110γ isoforms, sensitizes BCR-stimulated and/or stromal co-cultured primary CLL cells to apoptosis (median 20%, n=57; P<0.0001) including samples with poor prognostic markers, unmutated IgVH (n=28) and prior treatment (n=15; P<0.0001). IPI-145 potently inhibits the CD40L/IL-2/IL-10 induced proliferation of CLL cells with an IC50 in sub-nanomolar range. A corresponding dose-responsive inhibition of pAKT(Ser473) is observed with an IC50 of 0.36 nM. IPI-145 diminishes the BCR-induced chemokines CCL3 and CCL4 secretion to 17% and 37%, respectively.
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CAS 1201438-56-3 Duvelisib

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