pi3kβ

Duvelisib (INK1197, IPI-145) is a selective inhibitor of phosphatidylinositol 3-kinase (PI3K) and p100δ, with effects on p110δ (IC50 value is 0.0025 μM), p110γ (IC50 value is 0.274 μM), p110β (IC50 value is 0.85 μM) and p110α (IC50 value is 1.602 μM).

Eganelisib (IPI-549) is an inhibitor of PI3Kγ (IC50 = 16, 3,200, 3,500, and >8,400 nM for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively)

AS-604850 is a specific and ATP-competitive PI3Kγ inhibitor (IC50: 250 nM), 18-fold more selective for PI3Kγ than PI3Kα, and over 80-fold selectivity for PI3Kγ than PI3Kδ β.

PF-04691502 is a potent and selective inhibitor of PI3K and mTOR kinases with antitumor activity.

AS-605240 is an effective and specific inhibitor of PI3Kγ (IC50 Ki: 87.8 nM).

CZC24832 is a selective inhibitor of PI 3-kinase γ.

Copanlisib (BAY 80-6946) is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. By inhibiting the PI3K signaling pathway, Copanlisib may impede tumor cell growth and survival in certain tumor populations. Dysregulated PI3K signaling, often linked to tumorigenesis, may also contribute to tumor resistance to various antineoplastic agents.

KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 values of 8.6 nM, 4 nM, 0.5 nM, and 0.1 nM respectively, and demonstrates less inhibition of PI3Kγ with an IC50 of 0.59 μM.

TG100-115 is a PI3Kγ δ inhibitor (IC50: 83 235 nM), with fewer effects on PI3Kα β.

AZD-8835 is a mixed inhibitor of PI3Kα δ (IC50: 6.2 5.7 nM), also with selectivity against PI3Kβ γ (IC50: 431 90 nM).

A66 is a specific and effective p110α inhibitor(IC50=32 nM).

AMG319 is a potent and selective PI3Kδ inhibitor with an IC50 of 18 nM and exhibits >47-fold selectivity over other PI3Ks. [Phase 2]

PIK-90, a DNA-PK and PI3K inhibitor, suppresses p110α( IC50=11 nM), p110γ(IC50=18 nM) and DNA-PK(IC50=13 nM) .

Voxtalisib (XL765) (SAR245409, XL765) is a dual inhibitor of mTOR PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1 2.

VS-5584 (SB2343) is a pan-PI3K mTOR kinase inhibitor.

Bimiralisib (PI3K-IN-2) is an orally bioavailable pan inhibitor of PI3K and inhibitor of the mTOR, with potential antineoplastic activity. PI3K-IN-2 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K mTOR. Activation of the PI3K mTOR pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy.

NVP-BAG956 (BAG956) is a potent PI3K PDK inhibitor that inhibits PI3Kδ, PI3Kα, PI3Kγ, and PI3Kβ, shows strong cytotoxicity against T-ALL cell lines, and can be used to study melanoma.

AZD 6482 (KIN-193) is a potent and selective inhibitor of p110β and PI3Kβ with IC50 values ​​of 0.69nM and 10nM, respectively. AZD 6482 is particularly effective in blocking AKT signaling and tumor growth dependent on p110β activation or PTEN loss.

GDC0084 (RG7666) is a PI3K inhibitor with potential antineoplastic activity. GDC0084 (RG7666) specifically inhibits PI3K in the PI3K AKT kinase (or protein kinase B) signaling pathway, thereby inhibiting the activation of the PI3K signaling pathway. This may result in the inhibition of both cell growth and survival in susceptible tumor cell populations.

GNE-490 is an effective inhibitor of pan-PI3K with IC50s of 3.5 nM, 25 nM, 5.2 nM, 15 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. GNE-490 has >200 fold selectivity for mTOR (IC50 = 750 nM).

Pilaralisib (XL-147) is an orally available small molecule that selectively inhibits the activity of phosphoinositide-3 kinase (PI3K). Pilaralisib has been used in trials studying the treatment of Cancer, Lymphoma, Solid Tumors, Glioblastoma, and Breast Cancer, among others.

Vps34-PIK-III (VPS34-IN2), a selective inhibitor of VPS34 enzymatic activity, inhibits autophagy and results in the stabilization of autophagy substrates.

IC-87114 is a specific PI3Kδ inhibitor(IC50=0.5 μM).

FD274 is a potent dual PI3K mTOR inhibitor with inhibitory effects on PI3Kα β γ δ and mTOR, with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM, respectively. FD274 showed significant antiproliferative activity in AML cell line antiproliferative assays. FD274 exhibited dose-dependent pit tumor growth activity in an HL-60 xenograft model. FD274 has potential for use in acute myeloid leukemia studies.