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Medical Research Areas
Angiogenesis
BTK
BTK
下级目录
GDC-0834
AVL-292
CNX-774
RN486
CTA056
QL47
Birabresib
CGI560
CGI1746
NameC
LFM-A13
目录项下的产品
1133432-46-8 / MFCD233432468
GDC-0834 is a potent and selective inhibitor of Bruton's tyrosine kinase (BTK), investigated as a potential treatment for rheumatoid arthritis. In vitro metabolite identification studies in hepatocytes revealed predominant formation of an inactive metabolite (M1) via amide hydrolysis in human. GDC-0834 was shown to be a potent reversible inhibitor of six known Aldehyde oxidase (AO) substrates with IC50 values ranging from 0.86 to 1.87 μM. Additionally, in silico modeling studies suggest that GDC-0834 is capable of binding in the active site of AO with the amide bond of GDC-0834 near the molybdenum cofactor (MoCo), orientated in such a way to enable potential nucleophilic attack on the carbonyl of the amide bond by the hydroxyl of MoCo. Together, the in vitro and in silico results suggest the involvement of AO in the amide hydrolysis of GDC-0834.
N-(3-(6-((4-(1,4-二甲基-3-氧代哌嗪-2-基)苯基)氨基)-4-甲基-5-氧代-4,5-二氢吡嗪-2-基)-2-甲基苯基)-4,5,6,7-四氢苯并[b]噻吩-2-甲酰胺
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1202757-89-8 / MFCD302757898
N-(3-((5-Fluoro-2-((4-(2-Methoxyethoxy)Phenyl)Amino)Pyrimidin-4-Yl)Amino)Phenyl)Acrylamide
N-(3-((5-氟-2-((4-(2-甲氧基乙氧基)苯基)氨基)嘧啶-4-基)氨基)苯基)丙烯酰胺
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1202759-32-7 / MFCD302759327
4-(4-((4-((3-Acrylamidophenyl)Amino)-5-Fluoropyrimidin-2-Yl)Amino)Phenoxy)-N-Methylpicolinamide
4-(4-((4-((3-丙烯酰胺苯基)氨基)-5-氟嘧啶-2-基)氨基)苯氧基)-N-甲基吡啶酰胺
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1242156-23-5 / MFCD342156235
6-Cyclopropyl-8-Fluoro-2-(2-(Hydroxymethyl)-3-(1-Methyl-5-((5-(4-Methylpiperazin-1-Yl)Pyridin-2-Yl)Amino)-6-Oxo-1,6-Dihydropyridin-3-Yl)Phenyl)Isoquinolin-1(2H)-One
6-环丙基-8-氟-2-(2-(羟甲基)-3-(1-甲基-5-((5-(4-甲基哌嗪-1-基)吡啶-2-基)氨基)-6-氧代-1,6-二氢吡啶-3-基)苯基)异喹啉-1(2H)-酮
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1265822-30-7 / MFCD365822307
CTA056 is a potent and selective ITK inhibitor (interleukin-2-inducible T-cell kinase inhibitor). ITK is a member of the Btk (Bruton's tyrosine kinase) family of tyrosine kinases, plays an important role in normal T-cell functions and in the pathophysiology of both autoimmune diseases and T-cell malignancies. CTA056 exhibits the highest inhibitory effects toward Itk, followed by Btk and endothelial and epithelial tyrosine kinase. Among the 41 cancer cell lines analyzed, CTA056 selectively targets acute lymphoblastic T-cell leukemia and cutaneous T-cell lymphoma. CTA056 may be potential therapeutic agent for the treatment of T-cell leukemia and lymphoma.
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1469988-75-7 / MFCD569988757
QL47, also known as QL-XII-47, is a potent and selective BTK inhibitor, which covalently modifies Cys481. QL47 inhibits BTK kinase activity with an IC50 of 7 nM, inhibits autophosphorylation of BTK on Tyr223 in cells with an EC50 of 475 nM and inhibits phosphorylation of a downstream effector PLCγ2 (Tyr759) with an EC50 of 318 nM. In Ramos cells QL47 induces a G1 cell cycle arrest which is associated with pronounced degradation of BTK protein. QL47 inhibits the proliferation of B-cell lymphoma cancer cell lines at submicromolar concentrations.
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202590-98-5 / MFCD02590985
OTX-015
OTX-015
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中华人民共和国
√
845269-74-1 / MFCD45269741
CGI560 is a potent BTK inhibitor with IC50 = 400 nM for BTK.
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910232-84-7 / MFCD010232847
4-(Tert-Butyl)-N-(2-Methyl-3-(4-Methyl-6-((4-(Morpholine-4-Carbonyl)Phenyl)Amino)-5-Oxo-4,5-Dihydropyrazin-2-Yl)Phenyl)Benzamide
4-(叔丁基)-N-(2-甲基-3-(4-甲基-6-((4-(吗啉-4-羰基)苯基)氨基)-5-氧代-4,5-二氢吡嗪-2-基)苯基)苯甲酰胺
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936563-96-1 / MFCD036563961
Ibrutinib
伊布鲁替尼
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广州市
中华人民共和国
上海市
北京市
244240-24-2 / MFCD09878279
(2Z)-2-Cyano-N-(2,5-Dibromophenyl)-3-Hydroxy-2-Butenamide
(2Z)-2-氰基-N-(2,5-二溴苯基)-3-羟基-2-丁烯酰胺
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