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Angiogenesis

Angiogenesis

Angiogenesis is the formation and remodelling of new blood vessels and capillaries from growth of pre-existing blood vessels. It normally occurs during wound healing and embryonic development, but is also required for tumour growth and metastasis in cancer.

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PF-03814735

Catalog No. A11171
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Aurora A/B Kinase 抑制剂

PF-03814735是一种新颖，有效且可逆的Aurora A/B抑制剂，IC50为0.8 nM/5 nM，对Flt3，FAK，TrkA的效力较低，对Met和FGFR1的活性最低。了解更多

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MRX-2843

Catalog No. A16958
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MERTK and FLT3 抑制剂

MRX-2843是MERTK和FLT3的口服小分子抑制剂。了解更多

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TG-101348 (Fedratinib, SAR302503)

Catalog No. A11082
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JAK2/FLT3 抑制剂

TG-101348 (Fedratinib,SAR302503)是Janus相关激酶2的口服生物利用型，ATP竞争性和选择性抑制剂，在无细胞试验中IC50为3 nM，作用于JAK2比作用于JAK1和JAK3选择性高35和334倍,具有潜在的抗肿瘤活性。了解更多

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SB1317 (TG02)

Catalog No. A13454
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CDK/JAK2/FLT3 抑制剂

SB1317是细胞周期蛋白依赖性激酶（CDKs）、类FMS酪氨酸激酶-3（FLT3）和Janus激酶2（JAK2）的有效抑制剂，CDK2、JAK2和FLT3的IC50值分别为13nM、56nM和73nM。了解更多

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TG-02 (SB1317)

Catalog No. A11962
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FLT3 抑制剂

TG-02 (SB1317)是一种新型的小分子有效CDK/JAK2/FLT3抑制剂。了解更多

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R406 besylate

Catalog No. A10769
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Syk 抑制剂

R406 besylate是一种口服酪氨酸激酶抑制剂，IC50为41 nM。对Syk抑制作用强，但是不抑制Lyn，对Flt3的作用比对Syk低5倍。了解更多

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- Gabriella Leung, .et al. ARPC1B binds WASP to control actin polymerization and curtail tonic signaling in B cells, JCI insight, 2021, Dec 8;6(23):e149376 PMID: 34673575
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TCS 359

Catalog No. A12427
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FLT3 抑制剂

TCS 359是一种有效的FLT3受体酪氨酸激酶抑制剂（IC50 = 42 nM），对多种其他激酶具有选择性。了解更多

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AMG-925

Catalog No. A14025
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Dual FLT3/CDK4 抑制剂

AMG-925是一种有效，选择性和生物利用性的FLT3/细胞周期蛋白依赖性激酶4（CDK4）双激酶抑制剂。了解更多

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FLT3-IN-2

Catalog No. A16250
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FLT3 抑制剂

FLT3-IN-2是有效的FLT3抑制剂。了解更多

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G-749

Catalog No. A14214
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FLT3 抑制剂

G-749是一种新型有效的FLT3抑制剂，对于FLT3（WT），FLT3（D835Y）的IC50为0.4 nM，0.6 nM和1 nM。了解更多

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SU5614

Catalog No. A15548
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FLT3 抑制剂

SU5614是有效的选择性FLT3抑制剂。SU5614恢复了FL依赖性细胞中FLT3配体（FL）的抗凋亡和增殖活性。了解更多

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BPR1J-097

Catalog No. A16248
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FLT3 抑制剂

BPR1J-097是一种新颖的小分子FLT-3抑制剂，具有良好的体内抗肿瘤活性。了解更多

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AST 487

Catalog No. A15003
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RET kinase 抑制剂

AST487是Ret激酶抑制剂/FLT3抑制剂，对Ret的IC50为0.88 uM。了解更多

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Go 6976

Catalog No. A12419
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PKC 抑制剂

Go6976是一种有效的PKC抑制剂，对PKC（大鼠脑），PKCα和PKCβ1的IC50分别为7.9 nM，2.3 nM和6.2 nM。也是JAK2和Flt3的有效抑制剂。了解更多

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Gilteritinib (ASP2215)

Catalog No. A14411
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FLT3/Axl 抑制剂

Gilteritinib (ASP2215)是一种有效的FLT3/AXL抑制剂，对具有AML突变或FLT3-ITD和FLT3-D835的AML具有有效的抗白血病活性。了解更多

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- Mohammad Azhar, .et al. Rational polypharmacological targeting of FLT3, JAK2, ABL, and ERK1 suppresses the adaptive resistance to FLT3 inhibitors in AML, Blood Adv, 2022, Aug 31 PMID: 36044389
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UNC-2025

Catalog No. A15904
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Dual MER/FLT3 抑制剂

UNC-2025是一种有效的且可生物利用的双重MER/FLT3抑制剂，IC50分别为0.74 nM和0.8 nM，选择性是Axl和Tyro3的20倍。了解更多

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FLT3-IN-1

Catalog No. A16249
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FLT3 抑制剂

FLT3-IN-1是一种新型的有效选择性Flt3抑制剂，IC50为10 nM。抗表达FLT3-ITD的MV4-11细胞，IC50为6 nM。了解更多

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Tandutinib (MLN518)

Catalog No. A10887
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FLT3 抑制剂

Tandutinib (MLN518)是一种有效的FLT3抑制剂，c-KIT和PDGF受体酪氨酸激酶的自磷酸化，从而抑制细胞增殖并诱导细胞凋亡。了解更多

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Pexidartinib (PLX3397)

Catalog No. A15520
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CSF1/Kit/FLT3 抑制剂

Pexidartinib (PLX3397)是KIT，CSF1R和FLT3的小分子酪氨酸激酶（RTK）抑制剂，具有潜在的抗肿瘤活性。了解更多

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- Lu Luo, .et al. Intermittent theta-burst stimulation improves motor function by inhibiting neuronal pyroptosis and regulating microglial polarization via TLR4/NF κB/NLRP3 signaling pathway in cerebral ischemic mice, J Neuroinflammation, 2022, Jun 11;19(1):141 PMID: 35690810
- Sarah R Anderson,, .et al. Neuronal apoptosis drives remodeling states of microglia and shifts in survival pathway dependence, bioRxiv, 2022, 01.05.475126
- Hannah D Mason, .et al. Glia limitans superficialis oxidation and breakdown promotes cortical cell death after repeat head injury, JCI Insight, 2021, Oct 8;6(19):e149229 PMID: 34428178
- Chritica Lodder, .et al. CSF1R inhibition rescues tau pathology and neurodegeneration in an A/T/N model with combined AD pathologies, while preserving plaque associated microglia, Acta Neuropathol Commun, 2021, Jun 8;9(1):108 PMID: 34103079
- Anderson SR, .et al. Developmental Apoptosis Promotes a Disease-Related Gene Signature and Independence from CSF1R Signaling in Retinal Microglia, Cell Rep, 2019, May 14;27(7):2002-2013.e5 PMID: 31091440
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Pacritinib (SB1518)

Catalog No. A12694
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JAK2/FLT3 抑制剂

Pacritinib (SB1518)是Janus激酶2（JAK2）和JAK2突变体JAK2V617F的口服生物利用抑制剂，无细胞试验中IC50分别为23和22 nM，具有潜在的抗肿瘤活性。Pacritinib与JAK2竞争ATP结合，这可能导致抑制JAK2活化，抑制JAK-STAT信号传导途径以及半胱天冬酶依赖性凋亡。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
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ENMD-2076

Catalog No. A10352
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Aurora A / FLT3 抑制剂

ENMD-2076具有针对Aurora A和Flt3的选择性活性，IC50为14 nM和1.86 nM，对Aurora A的选择性是Aurora B的25倍，对VEGFR2/KDR和VEGFR3，FGFR1和FGFR2和PDGFRα的作用较小。阶段2。了解更多

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AC710

Catalog No. A15933
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FLT3/KIT/PDGFRα/PDGFRβ 抑制剂

AC710是一种有效的，具有活性的，选择性血小板衍生的生长因子受体家族激酶抑制剂，具有潜在的抗癌活性。了解更多

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AC710 Mesylate

Catalog No. A16246
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FLT3/KIT/PDGFRα/PDGFRβ 抑制剂

AC710 Mesylate是一种有效的选择性PDGFR家族激酶抑制剂，对于FLT3/KIT/PDGFRα/PDGFRβ的Kd值分别为0.6 nM/1.0 nM/1.3 nM/1.0 nM。了解更多

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Crenolanib (CP-868596)

Catalog No. A11052
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PDGFR/FLT3 抑制剂

Crenolanib (CP-868596)是口服生物可用的PDGFR酪氨酸激酶的选择性小分子抑制剂，在皮摩尔浓度下抑制PDGFRA和PDGFRB。了解更多

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- 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
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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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Dovitinib Dilactic acid (TKI258 Dilactic acid)

Catalog No. A10198
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RTK 抑制剂

Dovitinib是一种小分子多靶点酪氨酸激酶抑制剂，可抑制通过ZNF198-FGFR1或BCR-FGFR1转化为IL3独立性的Ba / F3细胞，IC50值分别为150 nM和90 nM。了解更多

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Dovitinib (TKI-258)

Catalog No. A11411
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RTK 抑制剂

Dovitinib是一种小分子多靶点酪氨酸激酶抑制剂，可抑制通过ZNF198-FGFR1或BCR-FGFR1转化为IL3独立性的Ba / F3细胞，IC50值分别为150 nM和90 nM。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
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Nintedanib esylate

Catalog No. A16197
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RTK 抑制剂

Nintedanib esylate是多种受体酪氨酸激酶（RTK）和非受体酪氨酸激酶（nRTK）的有效抑制剂。了解更多

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- Thibaut Fourniols, .et al. Inhibition of Colorectal Cancer-Associated Fibroblasts by Lipid Nanocapsules Loaded With Acriflavine or Paclitaxel, Int J Pharm, 2020, Jun 30;584:119337 PMID: 32371002
- 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

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