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搜索结果：“abl”

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Tianeptine sodium

Catalog No. A10931
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5-HT Receptor 激动剂

Tianeptine钠是体内和体外的选择性5-羟色胺再摄取促进剂（SSRE）。了解更多

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TSU-68 (Orantinib, SU6668)

Catalog No. A10953
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PDFGRβ 抑制剂

TSU-68 (Orantinib,SU6668)在无细胞试验中具有8 nM的Ki对PDGFR自磷酸化的最大效力，但也强烈抑制Flk-1和FGFR1反磷酸化，对IGF-1R，Met，Src， Lck，Zap70，Abl和CDK2；不抑制EGFR。了解更多

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- Aaron Y. Lai, .et al. Venular degeneration leads to vascular dysfunction in a transgenic model of Alzheimer's disease., Brain, 2015, Apr;138(Pt 4):1046-58 PMID: 25688079
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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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OSI-906

Catalog No. A11053
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IGF-1R 抑制剂

OSI-906是一种选择性IGF-1R抑制剂，在无细胞试验中IC50为35 nM；对InsR抑制作用适中，IC50为75 nM，对Abl，ALK，BTK，EGFR， FGFR1/2，PKA等没有抑制活性。了解更多

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- Masao Kakoki, .et al. Cyanocobalamin prevents cardiomyopathy in type 1 diabetes by modulating oxidative stress and DNMT-SOCS1/3-IGF-1 signaling, Communications Biology, 2021, 4:775
- Nakamura T, .et al. Naturally Occurring Hair Growth Peptide: Water-Soluble Chicken Egg Yolk Peptides Stimulate Hair Growth Through Induction of Vascular Endothelial Growth Factor Production, J Med Food, 2018, Jul;21(7):701-708 PMID: 29583066
- Tzeng SF, .et al. O-Glycosylation-mediated signaling circuit drives metastatic castration-resistant prostate cancer, FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- Takata N, .et al. IGF-2/IGF-1R signaling has distinct effects on Sox1, Irx3, and Six3 expressions during ES cell derived-neuroectoderm development in vitro, In Vitro Cell Dev Biol Anim., 2016, May;52(5):607-15 PMID: 26956358
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TAK-901

Catalog No. A11067
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Aurora Kinase A/B 抑制剂

TAK-901是一种新型Aurora A/B抑制剂，IC50为21 nM/15 nM。它不是细胞JAK2，c-Src或Abl的有效抑制剂。了解更多

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PP121

Catalog No. A11207
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PI3K 抑制剂

PP121是一种作用于PDGFR，Hck，mTOR，VEGFR2，Src和Abl的多靶点抑制剂，IC50分别为2 nM，8 nM，10 nM，12 nM，14 nM和18 nM，也抑制DNA-PK，IC50为60 nM。了解更多

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Saracatinib (AZD0530)

Catalog No. A10108
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Src/Abl 抑制剂

Saracatinib (AZD0530)是一种高选择性，双特异性Src/Abl激酶抑制剂，对c-Src和Abl激酶的IC50分别为2.7和30 nM。了解更多

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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
- Chisato Naito, .et al. Facilitatory effects of fetuin-A on atherosclerosis, Atherosclerosis, 2016, Mar;246:344-51 PMID: 26828753
- Kenta Maruyama, .et al. 5-Azacytidine-induced Protein 2 (AZI2) Regulates Bone Mass by Fine-tuning Osteoclast Survival, J Biol Chem, 2015, Apr 10; 290(15): 9377-9386 PMID: 25691576
- Amanda L Jackson, .et al. Emerging therapies: angiogenesis inhibitors for ovarian cancer, Expert Opin Emerg Drugs, 2015, Jun;20(2):331-46 PMID: 26001052
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WP1130 (Degrasyn)

Catalog No. A10988
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DUB/Bcr/ABL 抑制剂

WP1130 (Degrasyn)是一种新型的选择性小分子去泛素酶抑制剂和Bcr/Abl破坏途径激活剂，可特异性和快速下调野生型和突变型Bcr/Abl蛋白，而不会影响慢性粒细胞性白血病（CML）中的bcr/abl基因表达细胞。了解更多

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Danusertib (PHA-739358)

Catalog No. A10715
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Aurora 抑制剂

Danusertib (PHA-739358)是Aurora A/B/C的Aurora激酶抑制剂，在无细胞分析中的IC50为13 nM/79nM/61 nM，对Abl，TrkA，c-RET和FGFR1以及更低的浓度具有中等效力对Lck，VEGFR2/3，c-Kit，CDK2等有效。了解更多

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- Samuel Q. Li, etc. Targeting Wild-Type and Mutationally Activated FGFR4 in Rhabdomyosarcoma with the Inhibitor Ponatinib (AP24534). PLoS One. 2013; 8(10): e76551.
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Imatinib Mesylate

Catalog No. A10468
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Bcr-Abl 抑制剂

Imatinib mesylate是一种选择性酪氨酸激酶抑制剂，通过抑制KIT信号转导途径，在治疗胃肠间质瘤中诱导了持续的客观反应。了解更多

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- Inge Govaerts, .et al. PSEN1-selective gamma-secretase inhibition in combination with kinase or XPO-1 inhibitors effectively targets T cell acute lymphoblastic leukemia, J Hematol Oncol, 2021, 14: 97 PMID: 34167562
- Genevra Kuziel, .et al. Stromal CCL2 Signaling Promotes Mammary Tumor Fibrosis through Recruitment of Myeloid-Lineage Cells, Cancers (Basel), 2020, Jul 28;12(8):E2083 PMID: 32731354
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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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DCC-2036 (Rebastinib)

Catalog No. A11200
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Bcr-Abl 抑制剂

DCC-2036 (Rebastinib)是一种Bcr-Abl抑制剂，作用于Abl1(WT)和Abl1(T315I)，IC50分别为0.8 nM和4 nM，也抑制SRC， LYN， FGR， HCK， KDR， FLT3，和Tie-2，对c-Kit具有低的抑制活性。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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Nilotinib (AMN-107)

Catalog No. A10644
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Bcr-Abl 抑制剂

Nilotinib (AMN-107)是一种Bcr-Abl抑制剂，IC50小于30 nM。了解更多

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- Rami Shinnawi, .et al. Monitoring Human-Induced Pluripotent Stem Cell-Derived Cardiomyocytes with Genetically Encoded Calcium and Voltage Fluorescent Reporters, Stem Cell Reports, 2015, Oct 13; 5(4): 582-596 PMID: 26372632
- Tetsuya Saita, .et al. Preparation of Antibodies and Development of an Enzyme-Linked Immunosorbent Assay for the Tyrosine Kinase Inhibitors Lapatinib and Nilotinib., Biol Pharm Bull. , 2015, 38(10):1652-7 PMID: 26424026
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GNF 2

Catalog No. A11439
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Bcr-Abl 抑制剂

GNF 2是一种Bcr-abl抑制剂，在表达Bcr-abl的细胞中抑制增殖并诱导凋亡。了解更多

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AP24534 (Ponatinib)

Catalog No. A10080
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BCR-ABL 抑制剂

AP24534 (Ponatinib)是有效的多激酶和pan-BCR-ABL抑制剂。了解更多

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- 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
- Yamamoto Y, .et al. Development of a sandwich enzyme-linked immunosorbent assay for the quantification of ponatinib in serum, Anal Biochem, 2019, Feb 13. pii: S0003-2697(18)31083-2 PMID: 30771339
- N Naganna, .et al. Amino alkynylisoquinoline and alkynylnaphthyridine compounds potently inhibit acute myeloid leukemia proliferation in mice, EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
- 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
- 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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Bafetinib (INNO-406)

Catalog No. A10119
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Bcr-Abl 抑制剂

Bafetinib (INNO-406)是一种双重Bcr-Abl/Lyn酪氨酸激酶抑制剂。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
- S. Dallari, .et al. Src family kinases Fyn and Lyn are constitutively activated and mediate plasmacytoid dendritic cell responses, Nat Commun, 2017, 8: 14830 PMID: 28368000
- Andrea Haerzschel, .et al. BCR and chemokine responses upon anti-IgM and anti-IgD stimulation in chronic lymphocytic leukaemia, Ann Hematol, 2016, 95(12): 1979-1988 PMID: 27542958
- Magdalena Winiarska, .et al. Inhibitors of SRC kinases impair antitumor activity of anti-CD20 monoclonal antibodies, MAbs., 2014, 6(5): 1300-1313. PMID: 25517315
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Dasatinib (BMS-354825)

Catalog No. A10290
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Abl-Src 抑制剂

Dasatinib (BMS-354825)是一种口服多BCR/ABL和Src家族酪氨酸激酶抑制剂。Dasatinib (BMS-354825)的主要靶标是BCR/ABL，Src，c-Kit，ephrin受体和其他几种酪氨酸激酶，但不是erbB激酶，例如EGFR或Her2。了解更多

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- Chihiro Motozono, .et al. The SARS-CoV-2 Omicron BA.1 spike G446S mutation potentiates antiviral T-cell recognition, Nat Commun, 2022, Sep 21;13(1):5440 PMID: 36130929
- 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
- David E J Klawon, .et al. Altered selection on a single self-ligand promotes susceptibility to organ-specific T cell infiltration, J Exp Med, 2021, Jun 7;218(6) PMID: 33914024
- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Sano T, .et al. Gliding Basal Cell Migration of the Urothelium during Wound Healing, Am J Pathol, 2018, Nov;188(11):2564-2573 PMID: 30121259
- Ines Peschel, .et al. FLT3 and FLT3-ITD phosphorylate and inactivate the cyclin-dependent kinase inhibitor p27Kip1 in acute myeloid leukemia, Haematologica, 2017, Aug; 102(8): 1378-1389 PMID: 28522571
- 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
- John D. Leonard, .et al. Identification of natural regulatory T cell epitopes reveals convergence on a dominant autoantigen, Immunity, 2017, Jul 18; 47(1): 107-117.e8 PMID: 28709804
- 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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KW-2449

Catalog No. A10508
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FLT3/FGFR/Bcr-Abl/Aurora 抑制剂

KW-2449是FLT3、ABl、ABl-T315I和Aurora激酶的多激酶抑制剂。了解更多

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