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Home > Inhibitors & Agonists > PI3K/Akt/mTOR > PI3K

PI3K

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Cat. No. Product Name Field of Application Chemical Structure
DC5072 Duvelisib (IPI-145, INK1197) Featured
Duvelisib (IPI-145) is a selective inhibitor of the p110δ isoform, exhibiting IC50 values of 2.5 nM, 27.4 nM, 85 nM, and 1602 nM for p110δ, p110γ, p110β, and p110α, respectively, highlighting its specificity and potency.
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DC46266 PI3K-IN-20 Featured
PI3K-IN-20 is a PI3k inhibitor extracted from WO2017101847 A1, compound 1.
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DC72848 Leniolisib phosphate Featured
Leniolisib (CDZ173) phosphate is a potent and selective PI3Kδ inhibitor. Leniolisib phosphate has the potential for immunodeficiency disorders treatment.
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DC12386 Leniolisib (CDZ173) Featured
Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor currently in phase II/III clinical trials for the treatment of immunodeficiency disorders.
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DC10193 Seletalisib Featured
Seletalisib (UCB5857) is potent and selective PI3Kδ inhibitor with an IC50 of 12 nM.
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DC9829 IPI-549 Featured
IPI-549 is an orally administered immuno-oncology development candidate that selectively inhibits PI3K-gamma.
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DC74260 cyclo-CRVLIR Featured
cyclo-CRVLIR is a cyclic peptide that binds selectively to p110α RAS binding domain (p110α-RBD) with ITC Kd of 3 uM, blocks p110α/RAS interaction in vitro and KRAS cancer cell lines.
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DC74269 TGX286
TGX286 is a potent, selective p110β inhibitor with IC50 of 7, 17 and 13 nM for p110β WT, p110β D862Q, and p110β E858H, respectively, >100-fold selectivity over p110α.
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DC74268 PITCOIN3
PITCOIN3 is a potent, highly selective, cell-permeable inhibitor of PI3KC2α catalytic activity with IC50 of 126 nM.
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DC74267 PITCOIN2
PITCOIN2 (LU-06-006) is a potent selective PI3KC2α inhibitor with IC50 of 126 nM, has selectivity against PI3KC2γ but shows micromolar activity on PI3KC2β.
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DC74266 PF-06862309
PF-06862309 (PF-06843195 phosphate ester prodrug) is the in vivo-active, phosphate ester prodrug of PF-06843195, a potent selective PI3Kα inhibitor with Kd of <18 pM.
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DC74265 LP-182
LP-182 (LP182) is a potent, selective and orally bioavailable multi-functional kinase inhibitor, specifically targets PI3K and MAPK signaling pathways.
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DC74264 LL-00084282
LL-00084282 is a potent, selective and efficacious dual PI3Kδγ inhibitor with IC50 of 16.26 and 17.45 nM for PI3Kδ and PI3Kγ, respectively.
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DC74263 LL-00071210
LL-00071210 is a potent, selective, orally bioavailable PI3Kδ inhibitor with IC50 values of 24.6 nM and 9.4 nM in biochemical and cellular assays, respectively.
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DC74262 I-229
I-229 is a potent and selective inhibitor of Vps34.
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DC74261 HM5023507
HM5023507 is a potemt, selective, orally active dual PI3Kδ/γ inhibitor with IC50 of 4 nM and 5 nM for p110γ and p110δ, respectively.
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DC7228 PF-04691502 Featured
PF-04691502 is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK.
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DC7538 A66 Featured
A66 is a potent and specific p110α inhibitor with IC50 of 32 nM, >100 fold selectivity for p110α over other class-I PI3K isoforms.
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DC5081 Apitolisib Featured
GDC-0980 (RG7422) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM, respectively. Also a mTOR inhibitor with Ki of 17 nM, and highly selective versus others PIKK family kinases.
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DC40777 MSC2360844(IOA-244 /roginolisib) Featured
MSC2360844 is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. MSC2360844 shows highly selective against a panel of 278 additional kinases.
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DC47383 GSK251 Featured
GSK251 is a highly potent, highly selective, orally bioavailable inhibitor of PI3Kδ with a novel binding mode.
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DC10754 LX2343 Featured
LX-2343 is a novel non-ATP competitive PI3K inhibitor, negatively regulating AKT/mTOR signaling, thus promoting autophagy, and increasing A-beta clearance.
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DC11906 Parsaclisib Featured
Parsaclisib (INCB050465) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib can be used for the research of relapsed or refractory B-cell malignancies.
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DC70705 PQR514 Featured
PQR514 is a potent selective pan-PI3K inhibitor with binding Ki of 2.2 and 33 nM for p110α and mTOR, repectively.PQR514 inhibits phosphorylated S6 ribosomal protein (pS6, Ser235/236) and phosphorylation PKB Ser473 in A2058 cells with IC50 of 17 and 68 nM, respectively.PQR514 displays negligible interference with protein kinase activities at 10 uM in a KINOMEScan panel.PQR514 exhibits growth inhibition in vitro across a panel of 66 tumor cells with GI50 of 0.25 uM.PQR514 demonstrates significant antitumor activity aginst OVCAR-3 human ovarian cancer xenograft model in BALB/c nude mice.
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DC42414 Zandelisib Featured
Zandelisib is a phosphatidylinositol 3-kinase (PI3K) extracted from patent WO2019183226 A1, Compound Example 1. Zandelisib selectively inhibits p110δ with an IC50 of 3.5 nM. Zandelisib functions as an antineoplastic.
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DC7628 PI-3065 Featured
PI-3065 is a novel potent and selective PI3K p110δ inhibitor with IC50 of 15 nM; exhibits > 100 fold selectivity against p110α, p110β, p110γ, DNA-PK and mTOR.
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DC44213 PF-06843195 Featured
PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy.
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DC71172 NVP-CLR457 Featured
NVP-CLR457 (compound 40) is an orally active, potent and balanced pan-class I PI3K inhibitor. NVP-CLR457 shows a clear dose-dependent PK/PD/efficacy relationship. NVP-CLR457 has antitumor activity.
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DC72739 FAP-PI3KI1
FAP-PI3KI1 is a fibroblast-activated protein (FAP)-targeted PI3K inhibitor that selectively targets FAP-expressing human idiopathic pulmonary fibrosis (IPF) cells and effectively inhibits collagen synthesis and reduces collagen deposition.
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DC1068 XL147 analogue(PI3K inhibitor X) Featured
XL147 analogue (SAR245408) is a selective and reversible class I PI3K inhibitor for wild type and mutant p110α with IC50 of 40 nM and 40 nM, respectively.
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