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搜索结果：“raf”

“raf”的搜索结果

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PLX-4720

Catalog No. A10002
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Raf 抑制剂

PLX-4720是一种有效的，选择性的B-RafV600E抑制剂，无细胞试验中IC50为13 nM，同样有效地作用于c-Raf-1(Y340D和Y341D突变型)，作用于B-RafV600E比作用于野生型B-Raf选择性高10倍。了解更多

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Sorafenib Tosylate (Nexavar)

Catalog No. A10001
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Raf 抑制剂

Sorafenib Tosylate (Nexavar)是几种酪氨酸蛋白激酶(VEGFR和PDGFR)和RAF/MEK/ERK级联抑制剂的新型小分子抑制剂，Raf-1，wt BRAF和V599E突变型BRAF的IC50为6、22、38 nM。了解更多

Product Citations (12)

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- Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. Milciclib and sorafenib synergistically downregulate c-Myc to suppress tumor growth in an orthotopic murine model of human hepatocellular carcinoma, J Transl Sci, 2020, 7: 1-10
- Mariko Fujisawa, .et al. Involvement of the Interferon Signaling Pathways in Pancreatic Cancer Cells, Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
- Fangyuan Lai, .et al. Platelet-rich plasma enhances the proliferation of human adipose stem cells through multiple signaling pathways, Stem Cell Res Ther, 2018, 9: 107 PMID: 29661222
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Arum Park, .et al. Identification of Transcription Factor YY1 as a Regulator of a Prostate Cancer-Specific Pathway Using Proteomic Analysis, J Cancer, 2017, 8(12): 2303-2311 PMID: 28819434
- Cong Li, .et al. AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia., Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Zhihong Li, .et al. Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3, J Med Chem, 2014, Apr 24;57(8):3430-49 PMID: 24641103
- Hideki Yamaguchi, .et al. Saracatinib impairs the peritoneal dissemination of diffuse-type gastric carcinoma cells resistant to Met and fibroblast growth factor receptor inhibitors, Cancer Sci, 2014, 105(5): 528-536 PMID: 24612061
- Yaping Zhang, .et al. FLT3 and CDK4/6 inhibitors: Signaling mechanisms and tumor burden in subcutaneous and orthotopic mouse models of acute myeloid leukemia, J Pharmacokinet Pharmacodyn., 2014, 41(6): 675-691 PMID: 25326874
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Dabrafenib (GSK2118436A)

Catalog No. A11381
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Raf 抑制剂

Dabrafenib (GSK2118436A)是一种有效且选择性的B-RAF蛋白激酶抑制剂，具有V600E突变，目前正在临床试验中。了解更多

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- Yuki Shimizu, .et al. Acquired resistance to BRAF inhibitors is mediated by BRAF splicing variants in BRAF V600E mutation-positive colorectal neuroendocrine carcinoma, Cancer Lett, 2022, Sep 1;543 PMID: 35724767
- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Chenyang He, .et al. Detection of Dabrafenib using Optical Fibre Long Period Grating Sensor Modified with Surface Imprinted Polymers for Dose Detection and Prevention of Cancer Resistance, Clinical and Translational Biophotonics, 2020, TTh3B.2
- 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
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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ZM 336372

Catalog No. A11077
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C-Raf 抑制剂

ZM 336372是有效的ATP Raf-1体外竞争性抑制剂 (IC50 = 70 nM)。了解更多

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AZ628

Catalog No. A11063
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Raf 抑制剂

AZ628是一种RAF抑制剂，IC50值：BRAF V600E和野生型CRAF约为30 nM，野生型BRAF约为100 nM。了解更多

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PLX4032 (Vemurafenib)

Catalog No. A10739
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Raf 抑制剂

PLX4032(Vemurafenib)也称为RG7204，Vemurafenib，R7204，RO5185426。PLX4032是B-raf抑制剂，IC50为44 nM。了解更多

Product Citations (11)

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- Lee YJ, .et al. Overexpression of Dock180 and Elmo1 in melanoma is associated with cell survival and migration, Research Square, 2022, April 27th
- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Guixin Zhu, .et al. TRIM15 and CYLD regulate ERK activation via lysine-63-linked polyubiquitination, Nat Cell Biol, 2021, Sep;23(9):978-991 PMID: 34497368
- Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
- Kudo K, .et al. Cell surface CD63 increased by up-regulated polylactosamine modification sensitizes human melanoma cells to the BRAF inhibitor PLX4032, FASEB J, 2018, Dec 3:fj201800664RR PMID: 30508500
- Min Ho Choe, .et al. miR-550a-3-5p acts as a tumor suppressor and reverses BRAF inhibitor resistance through the direct targeting of YAP, Cell Death Dis, 2018, Jun; 9(6): 640 PMID: 29844307
- Jan Dorrie, .et al. BRAF and MEK Inhibitors Influence the Function of Reprogrammed T Cells: Consequences for Adoptive T-Cell Therapy, Int J Mol Sci, 2018, Jan; 19(1): 289 PMID: 29346301
- Aishwarya Kundu, .et al. Inhibition of Oncogenic BRAF Activity by Indole-3-Carbinol Disrupts Microphthalmia-Associated Transcription Factor Expression and Arrests Melanoma Cell Proliferation, Mol Carcinog, 2017, Jan; 56(1): 49-61 PMID: 26878440
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Toshinori Sueda, .et al. BRAFV600E inhibition stimulates AMP-activated protein kinase-mediated autophagy in colorectal cancer cells, Sci Rep, 2016, 6: 18949 PMID: 26750638
- Yanling Li, .et al. Tyrphostin AG1296, a platelet-derived growth factor receptor inhibitor, induces apoptosis, and reduces viability and migration of PLX4032-resistant melanoma cells, Onco Targets Ther, 2015, 8: 1043-1051 PMID: 25999739
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GW 5074

Catalog No. A11436
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Raf-1 抑制剂

GW 5074是一种强效、选择性和细胞渗透性的c-Raf1激酶抑制剂。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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Raf265 derivative

Catalog No. A10774
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RAF/VEGFR 抑制剂

Raf265 derivative是Raf265的衍生物，Raf265是一种口服，高度选择性的RAF和VEGFR激酶抑制剂，IC50为5至10μM。了解更多

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NVP-BHG712

Catalog No. A10661
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EphB4 抑制剂

NVP-BHG712是EphB4激酶的选择性抑制剂，在体外对EphB4的选择性超过40多种其他激酶（包括FGFR3）。了解更多

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- Y Kaibori, .et al. EphA2 phosphorylation at Ser897 by the Cdk1/MEK/ERK/RSK pathway regulates M-phase progression via maintenance of cortical rigidity, the FASEB Journal, 2019, Jan 22:fj201801519RR PMID: 30668924
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RAF265 (CHIR-265)

Catalog No. A10773
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RAF/VEGFR 抑制剂

RAF265 (CHIR-265)是一种口服，高度选择性的RAF和VEGFR激酶抑制剂，可控制或正常化VEGFR-2，同时抑制B-raf和c-Raf突变以预防癌症。了解更多

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TAK-733

Catalog No. A11040
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MEK 抑制剂

TAK-733是一种有效的，选择性的MEK变构抑制剂，作用于MEK1，IC50为3.2 nM，抑制Abl1，AKT3，c-RAF，CamK1，CDK2及c-Met等活性。了解更多

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Regorafenib (BAY 73-4506)

Catalog No. A10250
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VEGFR 抑制剂

Regorafenib (BAY 73-4506)是一种多激酶抑制剂，IC50为17、40和69 nM c-KIT，VEGFR2，B-Raf。Regorafenib（BAY 73-4506）是一种针对肿瘤及其脉管系统的口服生物利用型多激酶抑制剂。了解更多

Product Citations (9)

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- Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. Milciclib and sorafenib synergistically downregulate c-Myc to suppress tumor growth in an orthotopic murine model of human hepatocellular carcinoma, J Transl Sci, 2020, 7: 1-10
- Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
- Mariko Fujisawa, .et al. Involvement of the Interferon Signaling Pathways in Pancreatic Cancer Cells, Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
- Sunil Kumar Yadava, .et al. Low Temperature, Easy Scaling Up Method for Development of Smart Nanostructure Hybrid Lipid Capsules for Drug Delivery Application, Colloids Surf B Biointerfaces, 2020, Mar 2;190:110927 PMID: 32169777
- Takeshi Uenaka, .et al. In silico drug screening by using genome-wide association study data repurposed dabrafenib, an anti-melanoma drug, for Parkinson's disease, Hum Mol Genet, 2018, Nov 15; 27(22): 3974-3985 PMID: 30137437
- Yi Xu, .et al. Knockdown of delta-5-desaturase promotes the anti-cancer activity of dihomo-γ-linolenic acid and enhances the efficacy of chemotherapy in colon cancer cells expressing COX-2, Free Radic Biol Med, 2016, Jul; 96: 67-77 PMID: 27101738
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Hydrochlorothiazide

Catalog No. A10456
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Hydrochlorothiazide是噻嗪类的一线利尿剂化合物。了解更多

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Ciclopirox

Catalog No. A10213
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Ciclopirox是一种合成的抗真菌药物。它可以抑制酵母糠醛马拉丝霉的生长，并通过中断Na+K+ ATPase来抑制膜转移系统，从而发挥作用。了解更多

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- Katsuhisa Morita, .et al. Decomposition profile data analysis of multiple drug effects identifies endoplasmic reticulum stress-inducing ability as an unrecognized factor, Sci Rep, 2020, 10: 13139 PMID: 32753643
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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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SNS-314

Catalog No. A10851
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Aurora 抑制剂

SNS-314 Mesylate是Aurora A，Aurora B和Aurora C的有效和选择性抑制剂，IC50分别为9 nM，31 nM和3 nM。它对Trk A/B，Flt4，Fms，Axl，c-Raf和DDR2的效力较低。阶段1。了解更多

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OSI-930

Catalog No. A10679
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c-Kit/VEGFR 抑制剂

OSI-930是Kit，KDR，Flt，CSF-1R，c-Raf和Lck的有效抑制剂，IC50分别为80 nM，9 nM，8 nM，15 nM，41 nM和22 nM。了解更多

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