IPI-145

IPI-145 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.

Product information

CAS Number: 1201438-56-3

Molecular Weight: 416.86

Formula: C22H17ClN6O

Synonym:

INK-1197

INK 1197

INK1197

IPI-145

IPI 145

IPI145

Duvelisib

Copiktra

IPI-145. INK1197

Chemical Name: (S)-3-(1-((9H-purin-6-yl)amino)ethyl)-8-chloro-2-phenylisoquinolin-1(2H)-one

Smiles: C[C@H](NC1N=CN=C2NC=NC=12)C1=CC2=CC=CC(Cl)=C2C(=O)N1C1C=CC=CC=1

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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

PI3Kδ and PI3Kγ inhibition with IPI-145 has anti-proliferative activity in primary AML cells by inhibiting the activity of AKT and MAPK. Pre-treatment of AML cells with IPI-145 inhibits both adhesion and migration of AML blasts to bone marrow stromal cells.

References:

1. LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548824/ PubMed PMID: 31644131.
2. Patel K, Danilov AV, Pagel JM. Duvelisib for CLL/SLL and follicular non-Hodgkin lymphoma. Blood. 2019 Nov 7;134(19):1573-1577. doi: 10.1182/blood.2019001795. PubMed PMID: 31554637.
3. Flinn IW, Cherry MA, Maris MB, Matous JV, Berdeja JG, Patel M. Combination trial of duvelisib (IPI-145) with rituximab or bendamustine/rituximab in patients with non-Hodgkin lymphoma or chronic lymphocytic leukemia. Am J Hematol. 2019 Dec;94(12):1325-1334. doi: 10.1002/ajh.25634. Epub 2019 Oct 4. PubMed PMID: 31490009.
4. Frustaci AM, Tedeschi A, Deodato M, Zamprogna G, Cairoli R, Montillo M. Duvelisib: a new phosphoinositide-3-kinase inhibitor in chronic lymphocytic leukemia. Future Oncol. 2019 Jul;15(19):2227-2239. doi: 10.2217/fon-2018-0881. Epub 2019 May 29. PubMed PMID: 31137964.
5. Rodrigues DA, Sagrillo FS, Fraga CAM. Duvelisib: A 2018 Novel FDA-Approved Small Molecule Inhibiting Phosphoinositide 3-Kinases. Pharmaceuticals (Basel). 2019 May 6;12(2). pii: E69. doi: 10.3390/ph12020069. PubMed PMID: 31064155; PubMed Central PMCID: PMC6631818.
6. Das M. Duvelisib in indolent non-Hodgkin lymphoma. Lancet Oncol. 2019 Mar;20(3):e138. doi: 10.1016/S1470-2045(19)30101-9. Epub 2019 Feb 21. PubMed PMID: 30799261.

Products are for research use only. Not for human use.