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.
-
FLT3 抑制剂
AC220 (Quizartinib)是一种有效的选择性FLT3抑制剂，对于MC4-11和A375，IC50分别为0.56±0.3 nM和> 10 mM。
了解更多
- 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
- 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
- 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
-
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
- 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
-
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
- 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
-
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
- 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
-
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
-
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。
了解更多
-
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
-
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
-
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
-
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
-
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
- 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
-
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
-
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
-
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
-
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
-
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
-
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
-
FLT3 抑制剂
FLT3-IN-2是有效的FLT3抑制剂。
了解更多
-
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。
了解更多
-
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
-
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
-
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
-
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.
了解更多
-
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.
了解更多
-
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.
了解更多
-
FLT3/AXL inhibitor
Gilteritinib hemifumarate is a potent FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively.
了解更多
-
dual FLT3/Aurora kinase inhibitor
CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor.
了解更多
-
FLT3 inhibitor
FLT3-IN-3 is a potent FLT3 inhibitor with IC50s of 13 and 8 nM for FLT3 WT and FLT3 D835Y, respectively.
了解更多
-
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.
了解更多
-
FLT3 inhibitor
5'-Fluoroindirubinoxime (5??-FIO, compound 13), an Indirubin (HY-N0117) derivative, is a potent FLT3 inhibitor, with an IC50 of 15 nM.
了解更多
-
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
了解更多
-
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。
了解更多
- 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
-
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）。
了解更多
- 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
-
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。
了解更多
- 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
-
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）。
了解更多
- 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
-
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。
了解更多
- 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
-
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。
了解更多
- 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
-
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）。
了解更多
- 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
-
c-Met/NPM-ALK 抑制剂
Crizotinib hydrochloride是c-Met激酶和NPM-ALK的抑制剂。
了解更多
- 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
-
ALK5 抑制剂
SB-505124是转化生长因子-βI型受体（ALK5），ALK4和ALK7的选择性抑制剂（ALK5和ALK4的IC50值分别为47和129 nM）。
了解更多
-
ALK 抑制剂
SB525334是转化生长因子-β受体I（ALK5，TGF-βRI）的选择性抑制剂 (IC50 = 14.3 nM)。抑制TGF-β1诱导的smad2/3核定位和TGF-βRI诱导的肾细胞mRNA表达。
了解更多
-
ALK 抑制剂
CH5424802是一种有效的，选择性的，口服的ALK抑制剂，具有独特的化学支架，对具有ALK基因改变的癌症表现出优先的抗肿瘤活性。
了解更多
-
ALK 抑制剂
ASP3026是ALK激酶的新型选择性抑制剂。ASP3026在Tyr激酶组中有效抑制ALK激酶活性，并且比克唑替尼更具选择性。
了解更多
-
ALK 抑制剂
AP26113是一种有效的，选择性的ALK抑制剂，对野生型的功效为0.62 nM，对包括crizotinib耐药的L1196M系在内的多种突变体的活性也很强。在一组EML4-ALK或NPM-ALK阳性细胞系中，AP26113的IC50值为4-31 nM。
了解更多
-
ALK 抑制剂
LDK-378是ALK(间变性淋巴瘤激酶)的高度选择性、生物利用度和AT竞争性小分子抑制剂，ALK是一种受体酪氨酸激酶，被认为是肺癌的重要药物靶点。
了解更多
-
ALK/IGF1R 抑制剂
AZD3463是ALK/IGF1R抑制剂。
了解更多
-
ALK 抑制剂
CEP-28122是在人类癌症的实验模型中具有抗肿瘤活性的间变性淋巴瘤激酶的高效，选择性口服活性抑制剂。
了解更多
-
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。
了解更多
-
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。
了解更多
-
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。
了解更多
微信关注
China
United States