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PI3K

PI3K

货号 产品名 CAS号 信息
CSN32908 Zandelisib 1401436-95-0 Zandelisib is a potent and selective inhibitor of phosphatidylinositol 3-kinase (PI3K) with IC50 of 3.5 nM for p110δ.
CSN12216 Wortmannin 19545-26-7 Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. It also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.
CSN21430 Vps34-IN-4 1383716-46-8 Vps34-IN1 is a potent inhibitor of the class III phosphoinositide 3-kinase (PI3K) vacuolar protein sorting 34 (Vsp34) with IC50 of 15 nM.
CSN18633 UNBS5162 956590-23-1 UNBS5162 is a naphthalimide and a hydrolysis product of UNBS3157 that decreases CXCL chemokine expression in experimental prostate cancers and the mean antiproliferative activity IC50 value is 17.9 μM for 9 cancer cell lines.
CSN51112 Umbralisib tosylate 1532533-72-4 Umbralisib tosylate is a novel phosphatidylinositol 3-kinase delta (PI3Kdelta) inhibitor under development at TG Therapeutics. In 2021, the product received accelerated approval in the U.S. for the oral, once-daily treatment of adult patients with relapsed or refractory marginal zone lymphoma (MZL) who have received at least one prior anti-CD20-based regimen and for the treatment of adult patients with relapsed or refractory follicular lymphoma (FL) who have received at least three prior lines of systemic therapy. Launch took place short after. In 2021, TG Therapeutics completed a rolling submission in the U.S in combination with ublituximab for the treatment of chronic lymphocytic leukemia (CLL). The product is in phase III clinical trials, as monotherapy or in combination with ublituximab, for the treatment of CLL. The product is also in phase II/III clinical trials, as monotherapy or in combination with ublituximab, for the treatment of relapsed or refractory small lymphocytic lymphoma and B-cell lymphomas, including MZL, FL, diffuse large B-cell lymphoma and mantle cell lymphoma. The company refers to the combination regimen of ublituximab and TGR-1202 as TG-1303. The drug is also in phase II clinical development for the treatment Waldenstrom macroglobulinemia. Phase I clinical trials are ongoing for the treatment of Hodgkin's lymphoma. Phase I clinical trials were completed for the treatment of patients with select relapsed or refractory solid tumors, such as adenocarcinoma of the pancreas, adenocarcinoma of the colon, rectum, gastric and GE junction cancer, and GI Stromal Tumor (GIST). In 2016, orphan drug designation was assigned to the compound in the U.S. for the treatment of CLL. In 2017, additional orphan drug designation was granted in the U.S. for the treatment of CLL and DLBCL, in combination with ublituximab. In January 2019, the FDA granted breakthrough therapy designation to the product for the treatment of adult patients with MZL who have received at least one prior anti-CD20 regimen. The compound was granted additional orphan drug designation in the U.S. for the treatment of treatment of nodal, extranodal, and splenic MZL in 2019, and for the treatment of FL in 2020. Originated by Rhizen Pharmaceuticals, the product was jointly developed by Rhizen Pharmaceuticals and TG Therapeutics since 2012. In 2014, exclusive global development and commercialization rights (excluding India) were licensed to TG Therapeutics. In 2020, the product received fast track designation in US by TG Therapeutics for the treatment of adult patients with CLL in combination with ublituximab.
CSN21129 Tenalisib 1639417-53-0 Tenalisib is a potent and selective dual PI3Kδ/γ inhibitor with IC50 of 24.5 nM and 33.2 nM for PI3Kδ and PI3Kγ, respectively. Its selectivity over α and β isoforms are more than 300-fold and 100-fold, respectively.
CSN23147 5-(4-(3-(4-Acetylpiperazine-1-carbonyl)phenyl)quinazolin-6-yl)-2-methoxynicotinonitrile 1431540-99-6 TC KHNS 11 is a potent and selective PI 3-kinase δ inhibitor that is orally bioavailable.
CSN33174 IPL-344 877120-59-7 Stressin-1 is a Phosphatidylinositol 3-Kinase (PI3K) activator.
CSN28425 SRX3207 2254693-15-5 SRX3207 is an orally active dual Syk/PI3K inhibitor with IC50 value of 30nM for Syk. It potently blocks phosphorylation of Syk at 348 site and Y525/526 site. SRX3207 reduced immunosuppressive macrophage polarization and increased infiltration and cytotoxicity of CD8+ T cells in LLC tumors and increased expression of Ifng and Gzmb in 3207 treated LLC tumors.
CSN17136 Sophocarpine monohydrate 145572-44-7 Sophocarpine, a natural product isolated and purified from the herb of Sophora alopecuroidos L., with anti-viral, anti-cachectic and anti-inflammatory effects, can alleviate liver fibrosis mainly by inhibiting the TLR4 pathway, it may be a potential chemotherapeutic agent for chronic liver diseases, ameliorate the ischemic injury induced by transient focal cerebral ischemia in rats and that this neuroprotective effect may be related to the anti-ASIC1 channel and anti-apoptotic action of sophocarpine, and also alleviate hepatocyte steatosis and the potential mechanism may be the activated signaling pathway of AMPK.
CSN23870 Sonolisib 502632-66-8 Sonolisib (PX-866), an improved Wortmannin analogue, is an oral, irreversible, and pan-isoform inhibitor of PI3K (IC50=0.1 nM (p110α), 1.0 nM (p120γ), 2.9 nM (p110δ)). Antitumor activity[1][2].
CSN20214 SN32976 1246202-11-8 SN32976 is a selective inhibitor of PI3K and mTOR with preferential activity to PI3Kα, in comparison to established pan PI3K inhibitors.
CSN22559 SF2523 1174428-47-7 SF2523 blocks BRD4 binding to MYCN promoter PS1/PS2.
CSN20521 Pichromene 883046-50-2 S14161 is a small molecule inhibitor of cyclins D1-D3 expression that inhibits phosphoinositide 3-kinase activity and arrests cells at the G0/G1 phase in a dose-dependent manner (concentrations tested from 5-10 μM).
CSN23791 PWT33597 mesylate 1246203-36-0 PWT33597 is a dual inhibitor of PI3K alpha and mTOR with selectivity for PI3K alpha (IC50 = 26 nM) over PI3K delta (IC50 = 291 nM) but also displaying activity against mTOR in biochemical assays (IC50 = 21 nM). It had good pharmacokinetic properties in multiple preclinical species.
CSN22202 PQR530 1927857-61-1 PQR530 is a potent, oral and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, exhibiting antitumor activity.
CSN27247 PIK-75   372196-67-3 PIK-75 is a selective p110α inhibitor with IC50 of 5.8 nM with 200-fold more potently than p110β, and also potently inhibits DNA-PK with IC50 of 2 nM.
CSN20258 PI3Kδ-IN-1 1911564-39-0 PI3Kδ inhibitor C52 is a potent, selective, and efficacious PI3Kδ inhibitor with improved Caco-2 permeability, reduced Caco-2 efflux, reduced hERG PC activity, and increased selectivity profile while maintaining potency in the CD69 hWB assay, and is very potent in PK/PD assays and highly efficacious in a mouse collagen-induced arthritis model.
CSN24179 PI3K/mTOR Inhibitor-2 1848242-58-9 PI3K/mTOR Inhibitor-2 is a dual pan-PI3K/mTOR inhibitor with IC50 values of 3.4/34/16/1nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ and 4.7 nM for mTOR, respectively.
CSN26739 PI3K-IN-2 1403458-28-5 PI3K-IN-2 (compound 10) is a potent and orally active PI3Kβ/δ (IC50=7.1/8.6 nM) inhibitor with excellent selectivity versus PI3Kσ and PI3Kγ (IC50=13/190 nM, respectively)[1].
CSN26213 PI-828 942289-87-4 PI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with IC50s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid kinase assay, respectively.
CSN12265 PI-103 371935-74-9 PI-103 is a potent inhibitor with low IC50 values against recombinant PI3K isoforms p110alpha (IC50= 2 nM), p110beta (IC50= 3 nM), p110delta (IC50= 3 nM), and p110gamma (IC50= 15 nM), less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. It blocks autophagic flux.
CSN22480 Parsaclisib 1426698-88-5 Parsaclisib is a potent and selective PI3Kδ inhibitor, with an IC50 of 1 nM at 1 mM ATP, and shows appr 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases.
CSN26226 MTX-211 1952236-05-3 MTX-211 is a dual inhibitor of EGFR and PI3K, used for the treatment of cancer and other diseases.
CSN16767 Hexadecyl (2-(trimethylammonio)ethyl) phosphate 58066-85-6 Miltefosine is a mult-target inhibitor which can inhibit Akt, PI3K and PKC.
CSN24176 P110δ-IN-1 1595129-71-7 ME-401 is a potent and selective P110δ inhibitor.
CSN11346 LY294002 154447-36-6 LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM in cell-free assays. It is an early-stage autophagy inhibitor and also inhibits CK2.
CSN22949 LTURM-36 1879887-94-1 LTURM 36 is a PI 3-kinase δ inhibitor with IC50 of 0.64 μM.
CSN11302 Buddleoside 480-36-4 Linarin, a natural product isolated and purified from the herb of Uncaria sinensis (Oliv.) Havil., prevents a beta-induced neurotoxicity through the activation of PI3K/Akt, which subsequently inhibits GSK-3b and up-regulates Bcl-2.
CSN20673 Leniolisib 1354690-24-6 Leniolisib is a potent and selective PI3Kδ inhibitor currently in used for the treatment of immunodeficiency disorders.
CSN26741 LAS191954 1403947-26-1 LAS191954 is a Potent, Selective, and Orally Available PI3Kδ Inhibitor for the Treatment of Inflammatory Diseases. LAS191954 showed PI3Kdelta IC50 = 2.6 nM; M-CSF p-Akt IC50 = 7.8 nM; % Metabolism (R/H) = 20/16; PK i.v. t1/2 (R/D) = 3.1 h/10.2h. LAS191954 showed efficacy at significantly lower doses than Idelalisib. LAS191954 showed a potency on the target of 2.6 nM, with the highest selectivity versus PI3Kα (8.2 μM) and the lowest versus PI3Kγ and PI3Kβ (72 and 94 nM, respectively).
CSN14616 Isoangustone A 129280-34-8 Isoangustone A, a natural product isolated and purified from the roots of Licorice with antitumor activity, induces G1 cycle arrest in DU145 human prostate and 4T1 murine mammary cancer cells, dampens mesangial sclerosis associated with inflammation in response to high glucose through hindering TGF-β and NF-κB signaling, inhibits cell proliferation by targeting PI3K, MKK4, and MKK7 in human melanoma and shows strong ferric reducing activities and effectively scavenged DPPH, ABTS(+), and singlet oxygen radicals.
CSN21128 IPI-3063 1425043-73-7 IPI-3063 is a potent and selective PI3K p110δ inhibitor with an IC50 of 2.5 ± 1.2 nM.
CSN22432 TNP 519178-28-0 IP3K Inhibitor is a IP3K inhibitor with an IC50 of 10.2 μM.
CSN14412 Hirsutenone 41137-87-5 Hirsutenone, a natural product isolated and purified from the eaves of Alnus nepalensis, exhibits anti-cancer effect against prostate cancer through a direct physical inhibition of Akt1/2, attenuates adipogenesis by directly targeting PI3K and ERK during MCE in 3T3-L1 preadipocytes, underscoring the potential therapeutic application of Hirsutenone in preventing obesity, and may exert a preventive effect against microbial endotoxin lipopolysaccharide-induced inflammatory skin diseases through inhibition of ERK pathway-mediated NF-kappaB activation. Hirsutenone showed potent PL(pro) inhibitory activity with IC50 value of 4.1µM.
CSN17198 Nemiralisib 1254036-71-9 GSK-2269557 has low oral bioavailability (F=2%) and in vivo clearance of 28 mL/min/kg but has a high volume of distribution of 6.3 L/kg.
CSN32481 Fimepinostat mesylate 1401998-36-4 Fimepinostat mesylate is a small molecule inhibitor of histone deacetylase and PI3 kinase.
CSN22813 ETP-45658 1198357-79-7 ETP 45658 is a PI 3-kinase inhibitor with IC50s of 22, 30, 129 and 710 nM for PI 3-Kα, PI 3-Kδ, PI 3-Kβ and PI 3-Kγ respectively,and also inhibits DNA-PK and mTOR with IC50s of 70.6 and 152 nM respectively.
CSN32444 Dezapelisib 1262440-25-4 Dezapelisib is an orally bioavailable, selective inhibitor of the delta isoform of the 110 kDa catalytic subunit of class I phosphoinositide-3 kinases (PI3K).
CSN26528 BGT226 915020-55-2 BGT226 is a phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. PI3K inhibitor BGT226 specifically inhibits PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway, which may trigger the translocation of cytosolic Bax to the mitochondrial outer membrane, increasing mitochondrial membrane permeability; apoptotic cell death may ensue. Bax is a member of the proapoptotic Bcl2 family of proteins.
CSN27186 BAY1082439 1375469-38-7 BAY-1082439 is a highly selective PI3K 110α/β inhibitor. Upon binding to P-gp and BCRP, BAY-1082439 enhanced the ATPase activity of both P-gp and BCRP, implying the potential of BAY-1082439 to increase drug accumulation by blocking the efflux activity of both P-gp and BCRP.
CSN27232 AMG 511   1253573-53-3 AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model .
CSN43214 SAR-260301 1260612-13-2
CSN51383 GSK251 2125968-05-8
CSN51408 PF-06843195 2067281-51-8
CSN106827 Nemiralisib hydrochloride 1254036-77-5
CSN106516 TGX-155 351071-90-4
CSN106514 TGX-115 351071-62-0
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