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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ALK 抑制剂
PF-06463922是一种有效的双重ALK/ROS1抑制剂，对ROS1，ALK（WT）和ALK（L1196M）的Ki分别为<0.02 nM，<0.07 nM和0.7 nM。
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NUAK kinase 抑制剂
WZ4003是一种高度特异性的NUAK激酶抑制剂，对于NUAK1和NUAK2的IC50为20 nM和100 nM。
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ALK5 抑制剂
A 77-01是有效的TGF-βI型受体超家族激活素样激酶ALK5抑制剂，IC50为25 nM。
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ALK 抑制剂
LDK378 (Ceritinib) dihydrochloride是有效的抗ALK抑制剂，IC50为0.2 nM，对IGF-1R和InsR的选择性分别为40倍和35倍。
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ALK 抑制剂
ALK inhibitor 1 是ALK激酶的新型选择性抑制剂。
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ALK 抑制剂
ALK inhibitor 2 是ALK激酶的新型选择性抑制剂。
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FAK/ALK 抑制剂
CEP-37440是一种新型的高效选择性FAK/ALK双重抑制剂，IC50为2.3 nM（FAK）和120 nM（ALK细胞在50％人血浆中的IC50。
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ACK1/ALK 抑制剂
KRCA-0008是一种有效的选择性ALK/Ack1抑制剂，对ALK和Ack1的IC50分别为12 nM/4 nM。表现出类似药物的性质而无hERG责任。
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TRK, ROS1, ALK 抑制剂
Entrectinib，也称为RXDX-101和NMS-E628，是TrkA，TrkB和TrkC以及ROS1和ALK的小分子抑制剂，具有很高的效力和选择性。
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ALK 抑制剂
Brigatinib (AP26113)是一种有效的选择性ALK（IC50，0.6 nM）和ROS1（IC50，0.9 nM）抑制剂。它还以较低的效力抑制ROS1，FLT3和FLT3（D835Y）和EGFR的突变体。
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ALK2 抑制剂
LDN-214117是一种选择性有效的ALK2抑制剂。LDN-214117对ALK2的抑制最大，生化IC50为24 nM。
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ALK5 抑制剂
R-268712是一种有效且选择性的ALK5抑制剂，IC50为2.5 nM。
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ALK 抑制剂
HG-14-10-04是一种有效的特异性ALK抑制剂，IC50为20 nM。
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ALK/ ROS1 dual inhibitor
WY-135 is an ALK (IC50=1.4 nM) and ROS1 (IC50=1.1 nM) dual inhibitor.
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DNA alkylating agent
Duocarmycin GA is an antibody drug conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin GA can be used against multi-drug resistant cell lines.
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Alk2 inhibitor
ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, and over 700-fold selectivity against ALK3.
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ALK inhibitor
Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively.
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ALK/TRKA/TRKB/TRKC inhibitor
Belizatinib is an oral, dual, potent inhibitor of ALK and TRKA, TRKB, and TRKC, with IC50 of 0.7?nM for wild-type recombinant ALK kinase.
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ALK/MET inhibitor
Ensartinib hydrochloride (X-396 hydrochloride) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.
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ALK tyrosine kinase inhibitor
X-376 is a potent and highly specific ALK tyrosine kinase inhibitor (TKI) (IC50=0.61 nM). X-376 is a less potent inhibitor of MET (IC50=0.69 nM). X-376 displays potent anti-tumor activity.
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IGF-1R 抑制剂
GSK1838705A是一种小分子激酶抑制剂，其抑制IGF-IR和胰岛素受体的IC50分别为2.0和1.6 nmol/L。
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- Watanabe S, .et al. Insulin augments serotonin-induced contraction via activation of the IR/PI3K/PDK1 pathway in the rat carotid artery, Pflugers Arch, 2016, Apr;468(4):667-77 PMID: 26577585
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ALK2 抑制剂
DMH-1是骨形态发生蛋白（BMP）ALK2受体的选择性抑制剂（IC50 = 108 nM）。
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- Teresa Rayon, .et al. Species-specific pace of development is associated with differences in protein stability, Science, 2020, Sep 18;369(6510):eaba7667 PMID: 32943498
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c-Met/NPM-ALK 抑制剂
Crizotinib hydrochloride是c-Met激酶和NPM-ALK的抑制剂。
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- 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
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ALK 抑制剂
TAE684是ALK的抑制剂，也是LRRK2激酶活性的有效抑制剂（针对野生型LRRK2的IC（50）为7.8nM，针对G2019S突变体的为6.1nM）。
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- 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
- 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
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ALK 抑制剂
LDN193189是一种高效的小分子BMP抑制剂，可抑制BMP I型受体ALK2（IC50=5 nM），ALK3（IC50=30 nM）和ALK6（TGFβ1/BMP信号转导）以及随后的SMAD磷酸化。
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- Trang Thi Huyen Dang, .et al. BMP10 positively regulates myogenic differentiation in C2C12 myoblasts via the Smad 1/5/8 signaling pathway, Mol Cell Biochem, 2021, May;476(5):2085-2097 PMID: 33517521
- Shizu Aikawa, .et al. Autotaxin-lysophosphatidic acid-LPA 3 signaling at the embryo?\epithelial boundary controls decidualization pathways, EMBO J, 2017, Jul 14; 36(14): 2146-2160 PMID: 28588064
- HIROTAKA SOMEYA, .et al. Thymosin beta 4 is associated with RUNX2 expression through the Smad and Akt signaling pathways in mouse dental epithelial cells, Int J Mol Med, 2015, May; 35(5): 1169-1178 PMID: 25739055
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ALK4/ALK5 抑制剂
EW-7197是一种高效，选择性可生物利用的TGF-βI受体ALK4/ALK5抑制剂，IC50分别为13 nM和11 nM。
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- Bordignon P, .et al. Dualism of FGF and TGF-β Signaling in Heterogeneous Cancer-Associated Fibroblast Activation with ETV1 as a Critical Determinant, Cell Rep, 2019, Aug 27;28(9):2358-2372 PMID: 31461652
- Morita T, .et al. Tumor Progression Is Mediated by Thymosin-β4 through a TGFβ/MRTF Signaling Axis, Mol Cancer Res, 2018, May;16(5):880-893 PMID: 29330296
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ALK/ c-Met 抑制剂
PF-2341066 (Crizotinib)是c-Met激酶和NPM-ALK的抑制剂。PF-2341066抑制ALK阳性ALCL细胞中的细胞增殖（IC50 = 30 nM）。
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- 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
- Yu B, .et al. Pharmacokinetics and metabolism of ulixertinib in rat by liquid chromatography combined with electrospray ionization tandem mass spectrometry, J Sep Sci, 2020, Jan 22 PMID: 31970927
- 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
- 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
- Saki Omote, .et al. Effect of tyrosine kinase inhibitors on renal handling of creatinine by MATE1, Sci Rep, 2018, 8: 9237 PMID: 29915248
- Arakawa H, .et al. Inhibitory Effect of Crizotinib on Creatinine Uptake by Renal Secretory Transporter OCT2, J Pharm Sci, 2017, Sep;106(9):2899-2903 PMID: 28336299
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TGF-β/ALK5 抑制剂
A 83-01是转化生长因子βI型受体ALK5、淋巴结受体ALK4和淋巴结受体ALK7的选择性抑制剂。
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- Dan Zhao, .et al. From crypts to enteroids: establishment and characterization of avian intestinal organoids, Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
- Anna Nakanishi, .et al. Effects of human induced pluripotent stem cell-derived intestinal organoids on colitis-model mice, Regen Ther, 2022, Sep 9;21:351-361 PMID: 36161099
- Amira Abugomaa, .et al. Establishment of a direct 2.5D organoid culture model using companion animal cancer tissues, Biomed Pharmacother, 2022, Oct;154:113597 PMID: 36030590
- Isamu Ogawa, .et al. Suspension culture of human induced pluripotent stem cell-derived intestinal organoids using natural polysaccharides, Biomaterials, 2022, Sep;288:121696 PMID: 36038421
- Mohamed Elbadawy, .et al. Anti-tumor effect of trametinib in bladder cancer organoid and the underlying mechanism, Authorea, 2020, October 20
- Daichi Onozato, .et al. Application of Human Induced Pluripotent Stem Cell-Derived Intestinal Organoids as a Model of Epithelial Damage and Fibrosis in Inflammatory Bowel Disease, Biol Pharm Bull, 2020, 43(7), 1088-1095
- Amira Abugomaa, .et al. Establishment of 2.5D Organoid Culture Model Using 3D Bladder Cancer Organoid Culture, Sci Rep, 2020, Jun 10;10(1):9393 PMID: 32523078
- Jing-Yu Lin, .et al. In vitro expansion of pancreatic islet clusters facilitated by hormones and chemicals, Cell Discov, 2020, 6: 20 PMID: 32284878
- Kondo S, .et al. Establishment of a novel culture method for maintaining intestinal stem cells derived from human induced pluripotent stem cells, Biol Open, 2020, Jan 9;9(1) PMID: 31919043
- Onozato D, .et al. Generation of Intestinal Organoids Suitable for Pharmacokinetic Studies from Human Induced Pluripotent Stem Cells, Drug Metab Dispos, 2018, Nov;46(11):1572-1580 PMID: 29615438
- Usui T, .et al. Preparation of Human Primary Colon Tissue-Derived Organoid Using Air Liquid Interface Culture, Curr Protoc Toxicol, 2018, Feb 21;75:22.6.1-22.6.7 PMID: 29512123
- Kondo S, .et al. Using human iPS cell-derived enterocytes as novel in vitro model for the evaluation of human intestinal mucosal damage, Inflamm Res, 2018, Dec;67(11-12):975-984 PMID: 30317465
- Onozato D, .et al. Efficient Generation of Cynomolgus Monkey Induced Pluripotent Stem Cell-Derived Intestinal Organoids with Pharmacokinetic Functions, Stem Cells Dev, 2018, Aug 1;27(15):1033-1045 PMID: 29742964
- Tatsuya Usui, .et al. Hedgehog Signals Mediate Anti-Cancer Drug Resistance in Three-Dimensional Primary Colorectal Cancer Organoid Culture, Int J Mol Sci, 2018, Apr; 19(4): 1098 PMID: 29642386
- Tatsuya Usui, .et al. Establishment of a dog primary prostate cancer organoid using the urine cancer stem cells, Cancer Sci, 2017, Dec; 108(12): 2383-2392 PMID: 29024204
- Tatsuya Usui, .et al. Establishment of a novel three-dimensional primary culture model for hippocampal neurogenesis, Physiol Rep, 2017, Jun; 5(12): e13318 PMID: 28642339
- Tatsuya Usui, .et al. Establishment of a Novel Model for Anticancer Drug Resistance in Three-Dimensional Primary Culture of Tumor Microenvironment, Stem Cells Int, 2016, 2016: 7053872 PMID: 28119740
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Syk 抑制剂
R406 (Tamatinib)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。
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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。
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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。
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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。
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FLT3 inhibitor
BSc5371 is a potent and irreversible FLT3 inhibitor, with Kds of 1.3, 0.83, 1.5, 5.8 and 2.3 nM for mutant FLT3(D835H), FLT3(ITD, D835V), FLT3(ITD, F691L), FLT3-ITD and wild type FLT3wt, respectively.
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FLT-3 ITD degrader
PROTAC FLT-3 degrader 1 is an FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction.
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FLT3 inhibitor
FLT3-IN-4 is a potent and orally effective Fms-like tyrosine receptor kinase 3 (FLT3; IC50=7 nM) inhibitor for treating acute myelogenous leukemia.
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FLT3/CDK inhibitor
FN-1501 is a potent inhibitor of FLT3 and CDK, with IC50s of 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively. FN-1501 has anticancer activity.
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FLT3/AXL inhibitor
Gilteritinib hemifumarate is a potent FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively.
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dual FLT3/Aurora kinase inhibitor
CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor.
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FLT3 inhibitor
FLT3-IN-3 is a potent FLT3 inhibitor with IC50s of 13 and 8 nM for FLT3 WT and FLT3 D835Y, respectively.
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SYK/FLT3 inhibitor
TAK-659 is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively.
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FLT3 inhibitor
5'-Fluoroindirubinoxime (5??-FIO, compound 13), an Indirubin (HY-N0117) derivative, is a potent FLT3 inhibitor, with an IC50 of 15 nM.
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FLT3 inhibitor
HM-43239 is a Novel Potent Small Molecule FLT3 Inhibitor, in Acute Myeloid Leukemia (AML) with FMS-like Tyrosine Kinase 3 (FLT3) Mutations
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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。
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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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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。
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JAK2 抑制剂
TG101209是一种新型的JAK2抑制剂，无细胞试验中IC50为6 nM，对Flt3和RET作用效果稍弱，IC50分别为25 nM和17 nM，作用于JAK2比作用于JAK3选择性高30倍左右，对JAK2V617F和MPLW515L/K突变型敏感。在多发性骨髓瘤中具有显着的体外活性，并且对CD45+骨髓瘤细胞显示出优先的细胞毒性。
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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。
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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。
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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。
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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。
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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。
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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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