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PI3K / Akt / mTOR

PI3K / Akt / mTOR

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CAL-130 Racemate

Catalog No. A20942
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PI3Kδ inhibitor

CAL-130 Racemate is the racemate of CAL-130. CAL-130 Racemate is a PI3Kδ inhibitor. 了解更多

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Alpelisib hydrochloride

Catalog No. A21794
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PI3Kα inhibitor

Alpelisib hydrochloride (BYL-719 hydrochloride) is a potent, orally active, and selective PI3Kα inhibitor with IC50s of 5 nM, 250 nM, 290 nM and 1200 nM for p110α, p110γ, p110δ, and p110β, respectively. 了解更多

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Umbralisib R-enantiomer

Catalog No. A21993
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PI3Kδ inhibitor

Umbralisib R-enantiomer (TGR-1202 R-enantiomer) is a PI3Kδ inhibitor, which is the less active enantiomer of TGR-1202. 了解更多

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GSK2292767

Catalog No. A16564
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PI3Kδ inhibitor

GSK2292767 is a potent and selective inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ; Ki = 79 pM). GSK2292767 is >100-fold selective for PI3Kδ over a panel of 250 kinases. 了解更多

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PQR-530

Catalog No. A19209
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dual pan-PI3K/mTORC1/2 inhibitor

PQR-530 is a potent, oral and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, exhibiting antitumor activity. 了解更多

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PI3Kdelta inhibitor 1

Catalog No. A19249
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PI3Kδ inhibitor

PI3Kdelta inhibitor 1 (Compound 5d) is a potent, selective and orally available PI3Kδ inhibitor with an IC50 of 1.3 nM. 了解更多

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GDC-0077

Catalog No. A19494
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PI3Kα inhibitor

GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC50=0.038 nM). 了解更多

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CHMFL-PI3KD-317

Catalog No. A19990
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PI3Kδ inhibitor

CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM. 了解更多

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NSC781406

Catalog No. A20402
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PI3K/mTOR inhibitor

NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα. 了解更多

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GDC-0326

Catalog No. A20437
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PI3Kα inhibitor

GDC-0326 is a potent and selective PI3Kα inhibitor with a Ki of 0.2 nM. 了解更多

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SF2523

Catalog No. A20557
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PI3K inhibitor

SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively. 了解更多

Product Citations (1)

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- Virender Kumar, .et al. Polymeric nanomedicine for overcoming resistance mechanisms in hedgehog and Myc-amplified medulloblastoma, Biomaterials, 2021, Nov;278:121138 PMID: 34634662
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PI3K-IN-6

Catalog No. A20687
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PI3K β/δ inhibitor

PI3K-IN-6 (compound 20a) is an oral active and highly selective phosphoinositide 3-kinase (PI3K) β/δ inhibitor, with IC50 values of 7.8 nM/5.3 nM for PI3K β/δ, respectively. 了解更多

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LAS191954

Catalog No. A20691
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PI3Kδ inhibitor

LAS191954 is a potent, selective and orally active PI3Kδ inhibitor for inflammatory diseases treatment, with an IC50 of 2.6 nM. 了解更多

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SRX3207

Catalog No. A22305
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Syk/PI3K inhibitor

SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor, with IC50 values of 10.7 nM and 861 nM for Syk and PI3Kα, respectively. SRX3207 relieves tumor immunosuppression. 了解更多

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Everolimus (RAD001)

Catalog No. A10374
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mTOR 抑制剂

Everolimus (RAD001)是西罗莫司的40-O-(2-羟乙基)衍生物，与西罗莫司作为mTOR抑制剂的作用相似。了解更多

Product Citations (9)

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- Ming-Chun Hung, .et al. AKT phosphorylation as a predictive biomarker for PI3K/mTOR dual inhibition-induced proteolytic cleavage of mTOR companion proteins in small cell lung cancer, Cell Biosci, 2022, 12: 122 PMID: 35918763
- Yusuke Murase, .et al. Antitumor activity of the dual PI3K/mTOR inhibitor gedatolisib and the involvement of ABCB1 in gedatolisib resistance in canine tumor cells, Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
- Gabriela Torres-Flores, .et al. Preparation and Characterization of Liposomal Everolimus by Thin-Film Hydration Technique, Adv Polym Technol, 2020, ID 5462949
- Takaaki Fujimura, .et al. Enhanced antitumor effect of alectinib in combination with cyclin-dependent kinase 4/6 inhibitor against RET-fusion-positive non-small cell lung cancer cells, Cancer Biol Ther, 2020, Sep 1;21(9):863-870 PMID: 32835580
- BD Henriksbo, .et al. Statins Activate the NLRP3 Inflammasome and Impair Insulin Signaling via p38 and mTOR, Am J Physiol Endocrinol Metab, 2020, Jul 1;319(1):E110-E116 PMID: 32421368
- Hiroshi Fukamachi, .et al. A subset of diffuse-type gastric cancer is susceptible to mTOR inhibitors and checkpoint inhibitors, J Exp Clin Cancer Res, 2019, 38:127 PMID: 30866995
- Nachi Namatame, .et al. Antitumor profile of the PI3K inhibitor ZSTK474 in human sarcoma cell lines, Oncotarget, 2018, Oct 12; 9(80): 35141-35161 PMID: 30416685
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Rieko Ohki, .et al. PHLDA3 is a novel tumor suppressor of pancreatic neuroendocrine tumors, Proc Natl Acad Sci U S A, 2014, 111(23): E2404-E2413 PMID: 24912192
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AZD8055

Catalog No. A10114
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mTOR 抑制剂

AZD8055是一种有效的，选择性的ATP竞争性mTOR激酶抑制剂，IC50为0.8 nM。了解更多

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- L. M. C. Koene, .et al. Effects of antiepileptic drugs in a new TSC/mTOR-dependent epilepsy mouse model, ACTN, 2019, June PMID: 31353861
- Helga Weber, .et al. Rapamycin and WYE-354 suppress human gallbladder cancer xenografts in mice, Oncotarget, 2015, Oct 13; 6(31): 31877–31888 PMID: 26397134
- Kentaro Hirose, .et al. Mechanistic target of rapamycin complex 1 signaling regulates cell proliferation, cell survival, and differentiation in regenerating zebrafish fins, BMC Dev Biol, 2014, 14: 42. PMID: 25480380
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Rapamycin (Sirolimus)

Catalog No. A10782
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mTOR 抑制剂

Rapamycin (Sirolimus)是通过抑制T细胞和B细胞对白介素2（IL-2）的反应来防止其活化。了解更多

Product Citations (9)

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- R Mahalakshmi, .et al. Hormetic effect of low doses of rapamycin triggers anti-aging cascades in WRL-68 cells by modulating an mTOR-mitochondria cross-talk, Mol Biol Rep, 2022, Jan;49(1):463-476 PMID: 34739690
- Yusuke Murase, .et al. Antitumor activity of the dual PI3K/mTOR inhibitor gedatolisib and the involvement of ABCB1 in gedatolisib resistance in canine tumor cells, Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
- Zhichao Wu, .et al. Prompt Graft Cooling Enhances Cardioprotection during Heart Transplantation Procedures through the Regulation of Mitophagy, Cells, 2021, Oct 27;10(11):2912 PMID: 34831135
- Matthew A Schaller, .et al. Ex vivo SARS-CoV-2 infection of human lung reveals heterogeneous host defense and therapeutic responses, JCI Insight, 2021, Sep 22;6(18):e148003 PMID: 34357881
- Matthew A. Schaller, .et al. In vitro infection of human lung tissue with SARS-CoV-2: Heterogeneity in host defense and therapeutic response, bioRxiv, 2021, January 21
- Ashley VanCleave, .et al. Development and characterization of the novel human osteosarcoma cell line COS-33 with sustained activation of the mTOR pathway, Oncotarget, 2020, Jul 7; 11(27): 2597-2610 PMID: 32676162
- Y Huang, .et al. STIM1 controls calcineurin/Akt/mTOR/NFATC2?mediated osteoclastogenesis induced by RANKL/M-CSF, Experimental and Therapeutic Medicine, 2020, 20(2), 736-747 PMID: 32742319
- Takuya Hirao, .et al. Altered intracellular signaling by imatinib increases the anti-cancer effects of tyrosine kinase inhibitors in chronic myelogenous leukemia cells, Cancer Sci, 2018, Jan; 109(1): 121-131 PMID: 29121435
- Ya-Hui Chen, .et al. The Different Effects of Atorvastatin and Pravastatin on Cell Death and PARP Activity in Pancreatic NIT-1 Cells, J Diabetes Res, 2016, 2016: 1828071 PMID: 28004006
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Torin 1

Catalog No. A11587
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mTOR 抑制剂

Torin1是mTOR的有效抑制剂，IC50为2-10 nM。了解更多

Product Citations (4)

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- Andromachi Lambrianidou, .et al. mTORC2 deploys the mRNA binding protein IGF2BP1 to regulate c-MYC expression and promote cell survival, Cell Signal, 2021, Apr;80:109912 PMID: 33388443
- Kowalsky AH, .et al. The GATOR2?CmTORC2 axis mediates Sestrin2-induced AKT Ser/Thr kinase activation, J Biol Chem, 2020, Feb 14;295(7):1769-1780 PMID: 31915252
- Ashyad Rayhan, .et al. Using genetic buffering relationships identified in fission yeast to reveal susceptibilities in cells lacking hamartin or tuberin function, Biol Open, 2018, Jan 15; 7(1): bio031302 PMID: 29343513
- Jin H. Song, .et al. Mechanisms Behind Resistance to PI3K Inhibitor Treatment Induced by the PIM Kinase, Mol Cancer Ther, 2018, Dec;17(12):2710-2721 PMID: 30190422
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PP242 (Torkinib)

Catalog No. A10746
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mTOR 抑制剂

PP242 (Torkinib)在mTORC1和mTORC2中都是有效的选择性mTOR抑制剂。了解更多

Product Citations (2)

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- Hiroshi Fukamachi, .et al. A subset of diffuse-type gastric cancer is susceptible to mTOR inhibitors and checkpoint inhibitors, J Exp Clin Cancer Res, 2019, 38:127
- Fuse MJ, .et al. Mechanisms of Resistance to NTRK Inhibitors and Therapeutic Strategies in NTRK1-Rearranged Cancers, Mol Cancer Ther, 2017, Oct;16(10):2130-2143 PMID: 28751539
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WYE-354

Catalog No. A10989
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mTOR 抑制剂

WYE-354是一种有效的mTOR细胞渗透抑制剂（IC50 = 4.3 nM），可阻断通过mTOR复合体1（mTORC1）和mTORC2的信号传导。它是PI3Kα（IC50 = 1026 nM）和其他激酶的弱得多的抑制剂。了解更多

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- H Weber ,etc. Rapamycin and WYE-354 suppress human gallbladder cancer xenografts in mice. Oncotarget, 2015, 6(31), 31877.
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FK-506 (Tacrolimus)

Catalog No. A10389
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mTOR 抑制剂

FK-506 (Tacrolimus)是一种免疫抑制药物，通过结合到抑免蛋白FKBP12 (FK506 结合蛋白)产生新的复合物，从而降低T细胞中肽酰脯氨酰异构酶活性。了解更多

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- Ogawa Y, .et al. Inhibition of astrocytic adenosine receptor A2A attenuates microglial activation in a mouse model of Sandhoff disease, Neurobiol Dis, 2018, Oct;118:142-154 PMID: 30026035
- Yuko Okamoto, .et al. In vivo drug delivery efficiency of albumin-encapsulated liposomes as hydrophobic drug carriers, J Drug Deliv Sci Technol, 2018, 47: 62-66
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AZD2014 (Vistusertib)

Catalog No. A11303
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mTORC1/2 抑制剂

Vistusertib (AZD2014)是一种新型mTOR抑制剂，无细胞试验中IC50为2.8 nM；对多种PI3K亚型(α/β/γ/δ)具有较高选择性。浓度为1 μM时，对大多数激酶无或有微弱结合力。了解更多

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- Shuhang Dai, .et al. Calcium/calmodulin-dependent protein kinase kinase 2 mediates pleiotropic effects of epidermal growth factor in cancer cells, Biochim Biophys Acta Mol Cell Res, 2022, Jul;1869(7):119252 PMID: 35271909
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mTOR inhibitor (mTOR-IN-1)

Catalog No. A15175
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mTOR 抑制剂

mTOR inhibitor (mTOR-IN-1)是mTOR的有效且选择性的ATP竞争性抑制剂，Ki为1.5 nM。了解更多

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MHY1485

Catalog No. A15508
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mTOR 抑制剂

MHY1485是mTOR激活剂；通过抑制自噬体和溶酶体之间的融合导致LC3II蛋白的积累和自噬体扩大，从而抑制自噬过程。了解更多

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QL-IX-55

Catalog No. A11537
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mTORC1/2 抑制剂

QL-IX-55是mTORC1/2的选择性ATP竞争性抑制剂，其IC50分别为50/50/10-50nM，用于人mTORC1/酵母mTORC1/酵母mTORC2。了解更多

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Temsirolimus (Torisel)

Catalog No. A10906
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mTOR 抑制剂

Temsirolimus (Torisel)是mTOR的特异性抑制剂，会干扰调节肿瘤细胞增殖，生长和存活的蛋白质的合成。了解更多

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KU-0063794

Catalog No. A10505
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mTOR 抑制剂

KU-0063794是哺乳动物雷帕霉素靶位的选择性抑制剂(分别为mTORC1和mTORC2，IC50 ~10 nM)。了解更多

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WYE-125132 (WYE-132)

Catalog No. A11038
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mTOR 抑制剂

WYE-125132 (WYE-132)是一种高度有效的，ATP竞争性的mTOR抑制剂，IC50为0.19 nM；作用于mTOR比作用于PI3Ks或PI3K相关激酶hSMG1和ATR选择性高。了解更多

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OSI-027

Catalog No. A11056
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mTOR 抑制剂

OSI-027是一种有效的，选择性的，可口服生物利用的mTOR激酶抑制剂，可抑制与mTOR的TORC1和TORC2复合物相关的激酶活性。了解更多

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WYE-687

Catalog No. A11187
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mTOR 抑制剂

WYE-687是雷帕霉素（mTOR）哺乳动物靶标的新型ATP竞争性和选择性抑制剂，IC50为7 nM；抑制mTORC1/pS6K(T389)和mTORC2/P-AKT(S473)，但不抑制P-AKT(T308)，作用于mTOR比作用于PI3Kα(>100倍)和PI3Kγ(>500倍)选择性高。了解更多

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WAY-600

Catalog No. A11188
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mTOR 抑制剂

WAY-600是一种有效的，ATP竞争性的，选择性的mTOR抑制剂，IC50为9 nM；抑制mTORC1/P-S6K(T389)和mTORC2/P-AKT(S473)，但不抑制P-AKT(T308)；作用于mTOR比作用于PI3Kα(>100倍)和PI3Kγ(>500倍)选择性高。了解更多

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Deforolimus (Ridaforolimus)

Catalog No. A10295
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mTOR 抑制剂

Deforolimus (Ridaforolimus)是mTOR蛋白的研究目标靶向小分子抑制剂。阻断mTOR通过干扰细胞生长，分裂，代谢和血管生成，在癌细胞中产生饥饿样的效应。了解更多

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INK 128 (MLN0128)

Catalog No. A11461
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mTOR 抑制剂

INK 128是TORC1/2抑制剂，也是具有潜在抗肿瘤活性的猛禽mTOR（TOR复合物1或TORC1）和raptor-mTOR（TOR复合物2或TORC2）的口服生物利用抑制剂。了解更多

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- Ashlyn Parkhurst, .et al. Dual mTORC1/2 inhibition compromises cell defenses against exogenous stress potentiating Obatoclax-induced cytotoxicity in atypical teratoid/rhabdoid tumors, Cell Death Dis, 2022, Apr 28;13(4):410 PMID: 35484114
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GDC-0349

Catalog No. A11443
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mTOR 抑制剂

GDC-0349是一种有效的，选择性的，ATP竞争性的mTOR抑制剂，Ki为3.8 nM，比作用于PI3Kα和其他266种激酶的抑制效果高790倍。了解更多

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Zotarolimus

Catalog No. A11950
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mTOR 抑制剂

Zotarolimus是一种免疫抑制剂，可以抑制FKBP-12结合的IC50为2.8nM。。它是雷帕霉素的半合成衍生物。它设计用于以磷酸胆碱为载体的支架。了解更多

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Torin 2

Catalog No. A11586
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mTOR 抑制剂

Torin 2 是有效的选择性mTOR抑制剂 (IC50 = 2.1 nM)。在PI3K上显示mTOR的800倍细胞选择性（mTOR和PI3K的细胞EC50值分别为0.25和200 nM）。了解更多

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- Diane Yang, .et al. Pancreatic Differentiation of Stem Cells Reveals Pathogenesis of a Syndrome of Ketosis-Prone Diabetes, Diabetes, 2021, Oct;70(10):2419-2429 PMID: 34344789
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XL388

Catalog No. A12395
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mTOR 抑制剂

XL388是哺乳动物雷帕霉素靶标(mTOR)的一类新型高效、选择性、ATP竞争性生物可利用抑制剂。了解更多

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AP1903

Catalog No. A13519
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AP1903是具有均二聚活性的脂质渗透性他克莫司类似物。二聚体药物AP1903将人类蛋白质FKBP12（Fv）的类似物同二聚化，该类似物包含单个酸取代（Phe36Val），因此AP1903以低1000倍的亲和力与野生型FKBP12结合。了解更多

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CC-115

Catalog No. A15779
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mTOR/DNA-PK 抑制剂

CC-115是mTOR/DNA-PK的抑制剂（IC50 = 21/13 nM）。了解更多

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CC-223

Catalog No. A13078
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mTOR 抑制剂

CC-223是一种有效的mTOR激酶抑制剂（IC50 = 16 nM），其敏感性是相关脂质激酶PI3K-alpha（IC50 = 4 uM）的> 150倍。了解更多

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CZ415

Catalog No. A16476
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mTOR inhibitor

CZ415 is a potent and highly selective mTOR inhibitor with a pIC50 of 8.07. CZ415 inhibits mTORC1 and mTORC2 protein complex. 了解更多

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mTOR inhibitor-2

Catalog No. A13035
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mTOR inhibitor

mTOR inhibitor-2 is a highlt potent, selective and oral mTOR inhibitor with an IC50 of 7 nM. mTOR inhibitor-2 inhibits cellular phosphorylation of mTORC1 (pS6 and p4E-BP1) and mTORC2 (pAKT (S473)) substrates. 了解更多

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HDACs/mTOR Inhibitor 1

Catalog No. A13462
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HDACs/mTOR Inhibitor 1

HDACs/mTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs) and mammalian target of Rapamycin (mTOR) target inhibitor for treating hematologic malignancies. 了解更多

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42-(2-Tetrazolyl)rapamycin

Catalog No. A21394
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mTOR inhibitor

42-(2-Tetrazolyl)rapamycin is a prodrug compound of a rapamycin analog extracted from patent US 20080171763 A1, Example 1. Rapamycin is a specific mTOR inhibitor. 了解更多

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BX-795

Catalog No. A11148
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PDK-1 抑制剂

BX-795是有效的PDK1抑制剂，可阻断肿瘤细胞中的PDK1/Akt信号传导并抑制培养物中多种肿瘤细胞系的锚定依赖性生长或诱导凋亡。了解更多

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- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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PDK1 inhibitor

Catalog No. A11528
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PDK1 抑制剂

PDK1 inhibitor是PDK1的有效和选择性抑制剂，具有作为抗癌剂的潜力。了解更多

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PDK1 inhibitor

Catalog No. A16185
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PDK1 抑制剂

PDK1 inhibitor，强效，ATP竞争性和选择性双重PI3K和PDPK1抑制剂（PDK1和p-T308-PKB抑制的IC50值分别为34 nM和94 nM。了解更多

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OSU-03012

Catalog No. A10681
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PDK-1 抑制剂

OSU-03012 (AR-12)是一种有效的重组PDK-1(phosphoinositide-dependent kinase 1)抑制剂。了解更多

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BX-912

Catalog No. A11149
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PDK1 抑制剂

BX-912是3-磷酸肌醇依赖性激酶1（PDK1）的抑制剂。了解更多

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GSK 2334470

Catalog No. A12767
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PDK1 抑制剂

GSK 2334470是一种有效的3-磷酸肌醇依赖性蛋白激酶（PDK1）抑制剂（IC50?10 nM）。了解更多

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We promise all products to perform as described.