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搜索结果：“gdc 0084”

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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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GDC-0152

Catalog No. A14135
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IAP 拮抗剂

GDC-0152是caspases（Smac）的第二个线粒体激活物，具有潜在的抗肿瘤活性。了解更多

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GDC-0032 (Taselisib)

Catalog No. A12831
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PI3K 抑制剂

GDC-0032 (Taselisib)是有效的下一代PI3抑制剂，靶向PI3α。了解更多

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GDC-0879

Catalog No. A10420
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B-Raf 抑制剂

GDC-0879是B-Raf激酶的特异性抑制剂，靶向B-Raf (V600E) (IC50: 0.13 nM)。了解更多

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GDC-0980 (Apitolisib, RG7422)

Catalog No. A11023
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mTOR/PI3K 抑制剂

GDC-0980 (Apitolisib,RG7422)是一种有效的，I型PI3激酶和mTOR激酶抑制剂（TORC1/2），对于p110α，β，δ和γ的体外IC50为5、27、7和14 nM。了解更多

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- Kasun Wanigasooriya, .et al. Patient Derived Organoids Confirm That PI3K/AKT Signalling Is an Escape Pathway for Radioresistance and a Target for Therapy in Rectal Cancer, Front Oncol, 2022, Jul 4;12:920444 PMID: 35860583
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GDC-0941 (Pictilisib)

Catalog No. A10421
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PI3K 抑制剂

GDC-0941 (Pictilisib)是一种强效、选择性、口服生物可利用的I类PI3激酶(PI3K)抑制剂，p110 α、β、δ和γ亚型、DNA-PK和mTOR的IC50值分别为3、33、3、75、1230和580 nM。了解更多

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- Li T, .et al. Bruton's tyrosine kinase potentiates ALK signaling and serves as a potential therapeutic target of neuroblastoma, Oncogene, 2018, Nov;37(47):6180-6194 PMID: 30013190
- Joo Sang Lee, .et al. Harnessing synthetic lethality to predict the response to cancer treatment, Nat Commun, 2018, 9: 2546 PMID: 29959327
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GDC-0068 (Ipatasertib, RG-7440)

Catalog No. A11246
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Akt 抑制剂

GDC-0068 (Ipatasertib,RG-7440)是一种选择性的，具有ATP竞争性的pan-Akt抑制剂，在无细胞试验中，其靶向Akt1、2和3的IC50值分别为5、18和8 nM。了解更多

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GDC-0449 (Vismodegib)

Catalog No. A10258
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Hedgehog 拮抗剂

GDC-0449 (Vismodegib)是一种新型有效的，特异性hedgehog抑制剂，IC50为3 nM。了解更多

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- Daniel Doheny, .et al. Combined inhibition of JAK2-STAT3 and SMO-GLI1/tGLI1 pathways suppresses breast cancer stem cells, tumor growth, and metastasis, Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
- Yi Yang, .et al. Tumidulin, a Lichen Secondary Metabolite, Decreases the Stemness Potential of Colorectal Cancer Cells, Molecules, 2018, Nov; 23(11): 2968 PMID: 30441806
- Olesen UH, .et al. Topical delivery of vismodegib using ablative fractional laser and micro-emulsion formulation in vitro, Lasers Surg Med, 2018, Aug 28 PMID: 30152536
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GDC-0973 (Cobimetinib)

Catalog No. A11441
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MEK1 抑制剂

GDC-0973 (Cobimetinib,RG7420)是一种有效且高度选择性的MEK1抑制剂，IC50为4.2 nM，对MEK1的选择性选择性是对MEK2的100倍以上，并且当针对一组超过100个丝氨酸的抑制剂进行测试时，没有显示出明显的抑制作用。了解更多

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- Yunping Hu, .et al. FGFR1/MAPK-directed brachyury activation drives PD-L1-mediated immune evasion to promote lung cancer progression, Cancer Lett, 2022, Oct 28;547:215867 PMID: 35985510
- Seidel D, .et al. A multidimensional impedance platform for the real-time analysis of single and combination drug pharmacology in patient-derived viable melanoma models, Biosens Bioelectron, 2019, Jan 1;123:185-194 PMID: 30201332
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GDC0994 (Ravoxertinib)

Catalog No. A13420
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ERK1/2 抑制剂

GDC-0994是一种强效选择性Erk1/2抑制剂。GDC-0994抑制ERK磷酸化和ERK介导的信号转导通路的激活。了解更多

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GF 109203X

Catalog No. A13197
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PKC 抑制剂

GF 109203X是一种有效且选择性的蛋白激酶C抑制剂，对α和β1亚型具有选择性（对于α，β1，δ，δ，ε和ζ亚型，IC50分别为0.0084、0.0180、0.210、0.132和5.8μM）。对MLCK，PKG和PKA具有选择性（IC50值分别为0.6、4.6和33μM）。5-HT3受体的强效拮抗剂（Ki = 29.5 nM）。= 29.5 nm)。了解更多

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ABT-199 (Venetoclax)

Catalog No. A12500
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Bcl-2 抑制剂

ABT-199 (Venetoclax) 是一种所谓的BH3类似药物，旨在阻断Bcl 2蛋白的功能。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
- Anna L Koessinger, .et al. Increased apoptotic sensitivity of glioblastoma enables therapeutic targeting by BH3-mimetics, Cell Death Differ, 2022, Apr 26 PMID: 35473984
- Florian J Bock, .et al. Apoptotic stress-induced FGF signalling promotes non-cell autonomous resistance to cell death, Nat Commun, 2021, Nov 12;12(1):6572 PMID: 34772930
- Chauhan D, .et al. BAX/BAK-Induced Apoptosis Results in Caspase-8-Dependent IL-1β Maturation in Macrophages, Cell Rep, 2018, Nov 27;25(9):2354-2368.e5 PMID: 30485805
- Martin Grundy, .et al. Predicting effective pro-apoptotic anti-leukaemic drug combinations using co-operative dynamic BH3 profiling, PLoS One, 2018, 13(1): e0190682 PMID: 29298347
- Joanne Dai, .et al. Intracellular BH3 profiling reveals shifts in anti-apoptotic dependency in B-cell maturation and activation, J Immunol, 2018, 200 (5) 1727-1736 PMID: 29358277
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Arbutin (Uva, p-Arbutin)

Catalog No. A10084
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Tyrosinase 抑制剂

Arbutin (Uva,p-Arbutin)是用于中药（TCM）的糖基化对苯二酚。熊果苷由于其酪氨酸酶抑制活性而抑制黑色素的形成。了解更多

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