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Segnalazione PI3K/Akt/mTOR

Segnalazione PI3K/Akt/mTOR

Gli inibitori della segnalazione PI3K/Akt/mTOR sono composti che bersagliano le vie della fosfoinositide 3-chinasi (PI3K), della chinasi Akt e del bersaglio della rapamicina nei mammiferi (mTOR). Queste vie sono regolatori critici della crescita cellulare, della sopravvivenza, del metabolismo e dell'autofagia, rendendole bersagli chiave nella ricerca sul cancro e nei disturbi metabolici. Inibendo queste vie è possibile aiutare a controllare la crescita e la proliferazione tumorale, offrendo potenziali strategie terapeutiche per vari tipi di cancro e altre malattie caratterizzate da una segnalazione cellulare disfunzionale. Presso CymitQuimica, offriamo una vasta selezione di inibitori PI3K/Akt/mTOR di alta qualità per supportare la tua ricerca in oncologia, segnalazione cellulare e malattie metaboliche.

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  • PI3kδ inhibitor 1

    CAS:
    <p>PI3kδ inhibitor 1 is a selective inhibitor of PI3Kδ (IC50 of 3.8 nM).</p>
    Formula:C28H33FN6O2
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:504.60
  • GSK3-IN-9

    CAS:
    <p>GSK3-IN-9 (0713) is a selective inhibitor of glycogen synthase kinase 3 (GSK3). It holds potential for research into fragile X syndrome, attention deficit hyperactivity disorder (ADHD), childhood epilepsy, intellectual disabilities, diabetes, acute myeloid leukemia (AML), autism, and mental disorders.</p>
    Formula:C18H20N4O
    Colore e forma:Solid
    Peso molecolare:308.378
  • Lys(CO-C3-p-I-Ph)-O-tBu

    CAS:
    <p>Lys(CO-C3-p-I-Ph)-O-tBu, a pharmacokinetic modifier (PK modifier), enhances the pharmacokinetic properties of PSMA ligand molecules by increasing their residence time in plasma through improved binding to albumin and reducing absorption by the salivary glands, potentially extending the active compound's half-life. Moreover, Ac-PSMA-trillium is an effective PSMA-targeting compound for various biological applications when modified with different radioactive isotopes. When labeled with 111 In, it serves as a DOTA chelating agent and imaging agent. Alternatively, when labeled with 225 Ac, it acts as a Macropa chelator for targeted radionuclide therapy (TRT) in researching metastatic castration-resistant prostate cancer (mCRPC) [1] [2].</p>
    Formula:C20H31IN2O3
    Colore e forma:Solid
    Peso molecolare:474.38
  • GSK3β-IN-1

    CAS:
    <p>GSK3β-IN-1 (compound 1) is an inhibitor of glycogen synthase kinase-3β (GSK-3β) with an IC50 value of 65 nM, and it is utilized in Alzheimer's disease research.</p>
    Formula:C17H13FN2O4S
    Colore e forma:Solid
    Peso molecolare:360.36
  • SIK2/3-IN-1

    CAS:
    <p>SIK2/3-IN-1 (Compound 7S) is an orally active and selective inhibitor of SIK2/3. It significantly inhibits tumor growth without causing weight loss in the MV4-11 AML mouse CDX model. SIK2/3-IN-1 is applicable for research in MEF2C-dependent acute myeloid leukemia.</p>
    Formula:C20H19F3N6O2
    Colore e forma:Solid
    Peso molecolare:432.399
  • EGFR/HER2-IN-5


    <p>EGFR/HER2-IN-5: Irreversible, oral dual EGFR inhibitor, IC50 0.6 nM, targets L858R/T790M mutations, anti-tumor in vivo for lung cancer study.</p>
    Colore e forma:Solid
  • DNA-PK-IN-9


    <p>DNA-PK-IN-9 (YK6) is a potent DNA-PK inhibitor with an IC50 of 10.47 nM, important in cancer research.</p>
    Formula:C21H21N5O2
    Colore e forma:Solid
    Peso molecolare:375.42
  • Vulolisib

    CAS:
    <p>Vulolisib inhibits PI3K (α: IC50 0.2nM, β: 168nM, γ: 90nM, δ: 49nM), taken orally with anti-cancer properties.</p>
    Formula:C18H19F2N5O3S
    Colore e forma:Solid
    Peso molecolare:423.44
  • PI4KIII β inhibitor 5

    CAS:
    <p>PI4KIII beta inhibitor 5 (Compound 43) is an inhibitor of PI4KIIIβ with an IC50 of 19 nM. By inhibiting the PI3K/AKT pathway, it induces apoptosis in cancer cells, causes cell cycle arrest at the G2/M phase, and promotes autophagy. Additionally, PI4KIII beta inhibitor 5 demonstrates significant anti-tumor activity in the H446 small cell lung cancer xenograft model. This compound is applicable in cancer research studies.</p>
    Formula:C24H27F2N3O4S2
    Colore e forma:Solid
    Peso molecolare:523.616
  • HER2-IN-21

    CAS:
    <p>HER2-IN-21 (compound 657994) is an inhibitor of the human epidermal growth factor receptor 2 (HER2) with an IC50 value of 3.85 μM.</p>
    Formula:C20H18N4O3S
    Colore e forma:Solid
    Peso molecolare:394.447
  • HER2-IN-8

    CAS:
    <p>HER2-IN-8 is an inhibitor of HER-2 that can be used in the study of cancer and inflammation-related diseases.</p>
    Formula:C26H25F2N9O3
    Colore e forma:Solid
    Peso molecolare:549.53
  • HER2-IN-7

    CAS:
    <p>HER2-IN-7 is a potent HER2 inhibitor with potential for researching ErbB-related diseases, especially cancer.</p>
    Formula:C28H26F3N7O3
    Colore e forma:Solid
    Peso molecolare:565.55
  • Sacibertinib

    CAS:
    <p>Sacibertinib inhibits Trk, targeting EGFR-TK (EC50 110 nM) &amp; HER2 (EC50 244 nM), with anticancer properties.</p>
    Formula:C32H31ClN6O4
    Colore e forma:Solid
    Peso molecolare:599.08
  • ETP-47037

    CAS:
    <p>ETP-47037: strong PI3Kα inhibitor (IC50: 0.99 nM), also targets PI3Kβ, δ, γ; may protect telomeres.</p>
    Formula:C20H27N9O3S
    Colore e forma:Solid
    Peso molecolare:473.55
  • EGFR-IN-132

    CAS:
    <p>EGFR-IN-132 (Compound 23) is an EGFR inhibitor effective against various EGFR mutations including the wild-type, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S with IC50 values of 1.6, 0.025, 0.019, 0.022, and 0.029 nM, respectively. This compound demonstrates favorable pharmacokinetics with high oral bioavailability.</p>
    Formula:C27H31N7O3
    Colore e forma:Solid
    Peso molecolare:501.58
  • NSC381467

    CAS:
    <p>NSC381467: Potent, oral EGFR-TK inhibitor with strong antiproliferative effects, promising for cancer research.</p>
    Formula:C20H16O7
    Colore e forma:Solid
    Peso molecolare:368.34
  • GSK-3β inhibitor 25

    CAS:
    <p>GSK-3β inhibitor25 (Compound 6h) exhibits weak inhibitory activity against GSK-3β with an IC50 greater than 100 μM.</p>
    Formula:C16H15NOS
    Colore e forma:Solid
    Peso molecolare:269.361
  • Tesevatinib tosylate

    CAS:
    <p>Tesevatinib tosylate (XL-647 tosylate) is an orally administered epidermal growth factor receptor (EGFR) inhibitor that can cross the blood-brain barrier. It significantly reduces cell viability with IC50 values of 11 nM and 102 nM in GBM12 and GBM6, respectively. Additionally, Tesevatinib tosylate inhibits HER2 (IC50=16.1 nM), VEGFR2 (IC50=1.5 nM), and Src (IC50=10.3 nM), demonstrating antitumor activity by inhibiting tumor proliferation.</p>
    Formula:C31H33Cl2FN4O5S
    Colore e forma:Solid
    Peso molecolare:663.59
  • EGFR/BRAF-IN-1


    <p>EGFR/BRAF-IN-1 inhibits EGFR/BRAF (BRAFV600E IC50: 45 nM, GI50: 35 nM) and has antioxidant properties.</p>
    Formula:C26H28ClN3O4
    Colore e forma:Solid
    Peso molecolare:481.97
  • PI3K-IN-37

    CAS:
    <p>PI3K-IN-37 inhibits PI3K α/β/δ (IC50: 6/8/4 nM) and mTOR (IC50: 4 nM).</p>
    Formula:C25H26N6O2
    Colore e forma:Solid
    Peso molecolare:442.51
  • Andamertinib

    CAS:
    <p>Andamertinib is an EGFR inhibitor with antitumor activity.</p>
    Formula:C31H36N8O3
    Colore e forma:Solid
    Peso molecolare:568.669
  • EGFR-IN-135


    <p>EGFR-IN-135 (compound 3d) is an EGFR inhibitor with an IC50 value of 0.086 µM. It inhibits cell growth and arrests the cell cycle in the S phase in breast cancer cell lines.</p>
    Formula:C12H14N4OS2
    Colore e forma:Solid
    Peso molecolare:294.4
  • NU5455

    CAS:
    <p>NU5455 is a potent DNA-PKcs inhibitor, oral, boosts doxorubicin in liver tumors, amplifies topoisomerase inhibitors, no adverse effects.</p>
    Formula:C34H33N3O5S
    Colore e forma:Solid
    Peso molecolare:595.71
  • EGFR-IN-17


    <p>EGFR-IN-17: potent, selective EGFR inhibitor, IC50 of 0.2 nM, overcomes C797S drug resistance.</p>
    Formula:C27H31ClN7O3P
    Colore e forma:Solid
    Peso molecolare:568.01
  • EGFR-IN-125

    CAS:
    <p>EGFR-IN-125 (example 37) is a potent EGFR inhibitor with IC50 values of &lt;0.3 nM for EGFR(d746-750/T790M/C797S), 0.52 nM for EGFR(L858R/T790M/C797S), 0.5 nM for EGFR(d746-750/C797S), 0.69 nM for EGFR(L858R/C797S), and 0.92 nM for EGFR (wild type).</p>
    Formula:C30H26N8O
    Colore e forma:Solid
    Peso molecolare:514.58
  • EGFR-IN-18


    <p>EGFR-IN-18 strongly inhibits L858R/T790M/C797S mutant EGFR (4.9 nM) and also targets wild-type EGFR (47 nM).</p>
    Formula:C33H28N6O3S
    Colore e forma:Solid
    Peso molecolare:588.68
  • EGFR/VEGFR2-IN-2


    <p>EGFR/VEGFR2-IN-2 (compound 4b) serves as a dual inhibitor of VEGFR-2 and EGFR.</p>
    Formula:C24H15FO3
    Colore e forma:Solid
    Peso molecolare:370.37
  • EGFR-IN-147

    CAS:
    <p>EGFR-IN-147 (compound ID-5841161) is a potent EGFR inhibitor, demonstrating a 14% inhibition rate at a concentration of 1μM. It holds promise for cancer research applications.</p>
    Formula:C13H13N5O
    Colore e forma:Solid
    Peso molecolare:255.275
  • GSK-3β inhibitor 7


    <p>GSK-3β inhibitor 7 is a GSK-3β inhibitor (IC50: 5.25 μM).</p>
    Formula:C27H23BrN4O2S
    Colore e forma:Solid
    Peso molecolare:547.47
  • EGFR-IN-159

    CAS:
    <p>EGFR-IN-159 (compound 12) is a dihydropyrimidine and a potent EGFR inhibitor with an IC50 of 29.00 nM. It exhibits dose-dependent inhibition of EGFR and HER2. The compound shows cytotoxicity against MCF-7 breast cancer cells and Vero cells with IC50 values of 16.07 μg/mL and 35.98 μg/mL, respectively. EGFR-IN-159 does not cross the blood-brain barrier (BBB) and demonstrates significant anticancer activity.</p>
    Formula:C21H23N3O5
    Colore e forma:Solid
    Peso molecolare:397.424
  • JBJ-02-112-05

    CAS:
    <p>JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active inhibitor of EGFR with an IC 50 of 15 nM for EGFR L858R/T790M [1].</p>
    Formula:C27H20N4O2S
    Purezza:98%
    Colore e forma:Solid
    Peso molecolare:464.54
  • GSK-3β inhibitor 26

    CAS:
    <p>GSK-3β inhibitor26 (Compound D14) is a GSK-3β inhibitor with an IC50 of 18.23 μM. This compound is applicable in research related to cancer, inflammation, and neurodegenerative diseases.</p>
    Formula:C15H11N3O3
    Colore e forma:Solid
    Peso molecolare:281.266
  • BML-265

    CAS:
    <p>BML-265 is a potent inhibitor of EGFR tyrosine kinase (EGFR tyrosine kinase). It disrupts Golgi apparatus integrity in human cells and hinders the transport of secretory proteins across various substances. In contrast, BML-265 does not affect the integrity and transport of the Golgi apparatus in rodent cells.</p>
    Formula:C18H15N3O2
    Colore e forma:Solid
    Peso molecolare:305.331
  • HER2-IN-6

    CAS:
    <p>HER2-IN-6, a potent HER2 inhibitor, may target wild/mutant EGFR and HER2-mediated tumors. (Patent WO2021164697A1, compound 11)</p>
    Formula:C26H32N8O3
    Colore e forma:Solid
    Peso molecolare:504.58
  • JBJ-09-063

    CAS:
    <p>JBJ-09-063: EGFR inhibitor, IC50s 0.147-0.396 nM for various mutants; hinders EGFR/Akt/ERK1/2 phosphorylation; targets TKI-sensitive/resistant lung cancer.</p>
    Formula:C31H29FN4O3S
    Colore e forma:Solid
    Peso molecolare:556.65
  • EGFR/HER2-IN-7


    <p>EGFR/HER2-IN-7: Potent, selective dual inhibitor for MCF-7 cancer; IC50: EGFR 0.18μM, HER2 0.146μM, DHFR 0.907μM.</p>
    Formula:C19H21N3O2S
    Colore e forma:Solid
    Peso molecolare:355.45
  • SST0116CL1

    CAS:
    <p>SST0116CL1 is an HSP90 inhibitor (IC50: 0.21 μM) that targets the ATP-binding pocket of Hsp90, disrupting its chaperone function and leading to the degradation of client proteins (EGFR, CDK4, and AKT). It induces the degradation of Her2 in BT-474 cells (IC50: 0.2 μM) and exhibits antiproliferative activity, inhibiting tumor growth.</p>
    Formula:C22H31ClN4O6
    Colore e forma:Solid
    Peso molecolare:482.96
  • EGFR-IN-24


    <p>EGFR-IN-24 is a potent inhibitor of EGFR and inhibits EGFR (del19/T790M/C797S) and EGFR (L858R/T790M/C797S).</p>
    Formula:C30H35FN6O3
    Colore e forma:Solid
    Peso molecolare:546.64
  • Neptinib

    CAS:
    <p>Neptinib (NEP010), a derivative of Afatinib, exhibits enhanced antitumor properties and improved pharmacokinetics when administered orally. It demonstrates a notable suppression of tumor expansion in mouse models of non-small cell lung cancer harboring various EGFR mutations. Furthermore, Neptinib effectively inhibits the EGFR kinase family, exhibiting IC 50 values of 0.24 nM for EGFR wt, 7.25 nM for EGFR L858R/T790M, 0.46 nM for EGFR L858R, and 1.79 nM for EGFR T790M.</p>
    Formula:C22H23ClFN5O2
    Colore e forma:Solid
    Peso molecolare:443.90
  • 4-FPBUA

    CAS:
    <p>4-FPBUA, a semi-synthetic analog of lichen acid, enhances the functionality of cell-based blood-brain barriers (BBB) and increases the transport of β-amyloid (Aβ) in monolayer cells. Additionally, it acts as an inhibitor of mTOR, enhancing cellular autophagy (Autophagy) which can reverse BBB disruption in vivo, making it relevant for research in Alzheimer's disease.</p>
    Formula:C31H23FO7
    Colore e forma:Solid
    Peso molecolare:526.51
  • PI3Kβ-IN-1

    CAS:
    <p>PI3Kβ-IN-1 is a selective, orally active PI3Kβ inhibitor (IC50: 2 nM).</p>
    Formula:C25H14F2N8
    Colore e forma:Solid
    Peso molecolare:464.43
  • GSK-3β inhibitor 20

    CAS:
    <p>GSK-3β inhibitor20 (compound 3A) is an effective inhibitor of GSK-3β, exhibiting an IC50 value of 74.4 nM.</p>
    Formula:C22H21N5O2S
    Colore e forma:Solid
    Peso molecolare:419.50
  • PI3K-IN-27

    CAS:
    <p>PI3K-IN-27 is a potent PI3K inhibitor, relevant for cancer and immune disease research. See patent WO2021233227A1.</p>
    Formula:C30H26F2N6O2S
    Colore e forma:Solid
    Peso molecolare:572.63
  • EGFR-IN-133

    CAS:
    <p>EGFR-IN-133 (Compound 24) serves as an inhibitor targeting various mutations of the EGFR, including the wild type, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S with respective IC50 values of 0.1, 0.044, 0.036, 0.04, and 0.054 nM. The compound exhibits favorable pharmacokinetic properties and high oral bioavailability.</p>
    Formula:C27H29F2N7O3
    Colore e forma:Solid
    Peso molecolare:537.56
  • LAS195319

    CAS:
    <p>LAS195319 is a potent and selective inhaled PI3Kδ Inhibitor (IC50 = 0.5 nM) for the Treatment of Respiratory Diseases.</p>
    Formula:C29H26N10O3S
    Colore e forma:Solid
    Peso molecolare:594.65
  • EGFR-IN-23

    CAS:
    <p>EGFR-IN-23, identified as compound 8 in WO2021244502A1, is a potent EGFR tyrosine kinase inhibitor (TKI) demonstrating an inhibitory concentration (IC50) of 8.</p>
    Formula:C36H44BrN10O3P
    Colore e forma:Solid
    Peso molecolare:775.68
  • NS-062

    CAS:
    <p>NS-062 is an orally effective, irreversible covalent inhibitor targeting EGFR, demonstrating antiproliferative activity in the resistant double mutant H1975 cells with an IC50 of 0.19 μM. It also exhibits antitumor activity in a murine H1975 xenograft model.</p>
    Formula:C28H30Cl2F2N6O4
    Colore e forma:Solid
    Peso molecolare:623.48
  • DNA-PK-IN-15

    CAS:
    DNA-PK-IN-15 (compound 6) acts as an inhibitor of DNA-PK, exhibiting an IC50 value of 0.08 nM.
    Formula:C23H23N9O
    Colore e forma:Solid
    Peso molecolare:441.49
  • DNA-PK-IN-2

    CAS:
    <p>DNA-PK-IN-2 is an inhibitor of the DNA-PK enzyme complex, useful in cancer research.</p>
    Formula:C20H23N5O3
    Colore e forma:Solid
    Peso molecolare:381.43
  • EGFR-IN-58


    <p>EGFR-IN-58 is a potent, selective, ATP-competitive inhibitor of EGFR. EGFR-IN-58 exhibits significant cytotoxicity against melanoma, colon and blood cancers.</p>
    Formula:C31H30FN7O
    Colore e forma:Solid
    Peso molecolare:535.61