Duvelisib (IPI-145)

Biological Activity

Duvelisib (IPI-145) is a novel and selective PI3K δ/γ inhibitor with IC50 of 23 pM and 243 pM, respectively. 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. Duvelisib (IPI-145) suppresses murine/human B-cell proliferation with EC50 of 0.5 nM/0.5 nM and also inhibits human T-cell proliferation with EC50 of 9.5 nM. IPI-145 was well tolerated and clinically active in a broad range of malignancies, including iNHL. IPI-145 (10 mg/kg) demonstrates dose-dependent effect in rat collagen induced arthritis (CIA) model.

Customer Product Validations & Biological Datas

	Source	Blood (2014). Figure 1. IPI-145
	Method	immunoblotting
	Cell Lines	CLL cells
	Concentrations	0.01 to 1 μM
	Incubation Time	24 h
	Results	Cell viability was measured every 24 hours; 0.25 to 5 μM IPI-145 exhibited concentration and timedependent induction of cytotoxicity in CLL.

Chemical Information

Molecular Weight	416.86
Formula	C22H17ClN6O
CAS Number	1201438-56-3
Solubility (25°C)	DMSO 40 mg/mL
Storage	Powder          -20°C   3 years ;  4°C   2 years In solvent       -80°C   6 months ;  -20°C   1 month

References

[1] Anna Maria Frustaci, et al. Duvelisib for the treatment of chronic lymphocytic leukemia

[2] No authors listed. Duvelisib

[3] No authors listed. Duvelisib

[4] Ian W Flinn, et al. The phase 3 DUO trial: duvelisib vs ofatumumab in relapsed and refractory CLL/SLL

[5] Steven M Horwitz, et al. Activity of the PI3K-δ,γ inhibitor duvelisib in a phase 1 trial and preclinical models of T-cell lymphoma