5-fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)propyl]-3,4-dihydroquinazolin-4-one

Synonym
Product Category
Product Code
CAS Number
MDL Number
Pubchem CID
Reaxys RN
Idelalisib, CAL-101, GS-1101, IC489666, Zydelig
API & Intermediates
KAPI1F08
870281-82-6
MFCD19443647
11625818
25802168
image-155171-Trimethyl(trifluoromethyl)silane_reagent.png
Chemical Name
Molecular Formula
Molecular Weight
Assay
Appearance
Melting Point
Packaging
Storage
5-fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)propyl]-3,4-dihydroquinazolin-4-one
C22H18FN7O
415.43
≥99.8%(HPLC)
White to Slightly Pale Yellow Solid
250-252°C
500mg,1g,10g,25g,50g,100g and 500g
-20°C Freezer
Idelalisib (also known as CAL-101, GS-1101, IC489666, Zydelig) is a potent and selective inhibitor of highly specific small-molecule phosphatidylinositol-3-kinase (PI3Kδ), which mediates B-cell receptor (BCR) signaling and microenvironmental support signals that promote the growth and survival of malignant B lymphocytes. It has been reported that idelalisib induces apoptosis and inhibits proliferation in cell lines derived from malignant B lymphocytes and in primary tumor cells. Recently, idelalisib has been approved for the treatment of several hematological malignancies.
Exploiting the PI3K/AKT pathway for cancer drug discovery. [1]
Taming the PI3K team to hold inflammation and cancer at bay. [2]
CAL-101, a p110δ selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. [3]
The phosphoinositide 3'-kinase delta inhibitor, CAL-101, inhibits B-cell receptor signaling and chemokine networks in chronic lymphocytic leukemia. [4]
B-cell receptor signaling as a driver of lymphoma development and evolution. [5]
Haematological cancer: Idelalisib—targeting PI3Kδ in patients with B-cell malignancies. [6]
Idelalisib: First Global Approval. [7]
Structural, Biochemical, and Biophysical Characterization of Idelalisib Binding to Phosphoinositide 3-Kinase δ. [8]
References:
[1] B.T.Hennessy, et al, Nat. Rev. Drug Discov., 2005, 4(12), pp 988-1004.
[2] E.Hirsch, et al, Pharmacol. Ther., 2008, 118(2), pp 192-195.
[3] B.J.Lannutti, et al, Blood, 2011, 117(2), pp 591-594.
[4] J.Hoellenriegel, et al, Blood, 2011, 118(3), pp 3603-3612.
[5] C.U.Niemann, et al, Semin. Cancer Biol., 2013, 23(6), pp 410-421.
[6] J.A.Burger, et al, Nat. Rev. Clin. Oncol., 2014, 11, pp 184-186.
[7] A.Markham, Drugs, 2014, 74(14), pp 1701-1707.
[8] J.R.Somoza, et al, J. Biol. Chem., 2015, 290, pp 8439-8446.
Signal Word
Hazard Statements
Precautionary Statements
HS Code
RIDADR
Legal Information
Danger
H361,H372
P201,P202,P260,P264,P270,P280,P308+P313,P405,P501

Not regulated
Sales restrictions may apply.
1. Product Specification
2. Safety Data Sheet
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