RN 486
|
|
|
- CAS号:
- 1242156-23-5
- 英文名:
- RN486
- 英文别名:
- RN486;RN468;CS-689;RN486/RN-486;RN486
LM-2078;RN486 TFA Salt;RN486; RN-486; RN 486;6-Cyclopropyl-8-fluoro-2-(2-(hydroxymethyl)-3-(1-methyl-5-(5-(4-methylpiperazin-1-yl)pyridin-2;6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[1-methyl-5-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]isoquinolin-1-one;6-cyclopropyl-8-fluoro-2-(2-(hydroxyMethyl)-3-(1-Methyl-5-(5-(4-Methylpiperazin-1-yl)pyridin-2-ylaMino)-6-oxo-1,6-dihydropyridin-3-yl)phenyl)isoquinolin-1(2H)-one
- 中文名:
- RN 486
- 中文别名:
- 化合物DBEQ;化合物RN486;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
- CBNumber:
- CB02650908
- 分子式:
- C35H35FN6O3
- 分子量:
- 606.69
- MOL File:
- 1242156-23-5.mol
|
|
|
RN 486化学性质
-
沸点:
-
868.6±65.0 °C(Predicted)
-
|
-
密度:
-
1.378±0.06 g/cm3(Predicted)
-
|
-
储存条件:
-
Store at -20°C
-
|
-
溶解度:
-
≥30.35 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH
-
|
-
形态:
-
solid
-
|
-
酸度系数(pKa):
-
13.95±0.10(Predicted)
-
|
-
颜色:
-
Off-white to light yellow
-
|
-
CAS 数据库:
-
1242156-23-5
-
|
RN 486性质、用途与生产工艺
RN486是一种有效的选择性BTK 抑制剂，IC50为4 nM。
RN486 not only potently and selectively inhibits the Btk enzyme, but also displays functional activities in human cell-based assays in multiple cell types, blocking Fcε receptor cross-linking-induced degranulation in mast cells (IC50 = 2.9 nM), Fcγ receptor engagement-mediated tumor necrosis factor α production in monocytes (IC50 = 7.0 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC50 = 21.0 nM). RN486 is able to block the signaling of BCR as demonstrated by a marked inhibition of phosphorylation of both Btk and PLCγ2 in B cells. RN486 displays a selective B cell inhibitory profile in BioMAP Systems.
RN486 displays similar functional activities in rodent models, effectively preventing type I and type III hypersensitivity responses. More importantly, RN486 produces robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 inhibits both joint and systemic inflammation either alone or in combination with methotrexate, reducing both paw swelling and inflammatory markers in the blood.
RN 486
上下游产品信息
上游原料
下游产品
1242156-23-5, RN 486 相关搜索:
- Inhibitors
- 合成有机化合物配体
- 小分子抑制剂，天然产物
- 小分子抑制剂
- C35H35FN6O3
- 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
- 化合物DBEQ
- 化合物RN486
- 1242156-23-5
- 1(2H)-Isoquinolinone, 6-cyclopropyl-2-[3-[1,6-dihydro-1-methyl-5-[[5-(4-methyl-1-piperazinyl)-2-pyridinyl]amino]-6-oxo-3-pyridinyl]-2-(hydroxymethyl)phenyl]-8-fluoro-
- 2-(3-(5-(5-(4-methylpiperazin-1-yl)pyridin-2-ylamino)-1,6-dihydro-1-methyl-6-oxopyridin-3-yl)-2-(hydroxymethyl)phenyl)-6-cyclopropyl-8-fluoroisoquinolin-1(2H)-one
- 6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[1-methyl-5-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]isoquinolin-1-one
- 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)-on
- RN486; RN-486; RN 486
- CS-689
- 6-Cyclopropyl-8-fluoro-2-(2-(hydroxymethyl)-3-(1-methyl-5-(5-(4-methylpiperazin-1-yl)pyridin-2
- RN486 TFA Salt
- RN486
LM-2078
- 6-Cyclopropyl-2-[3-[1,6-dihydro-1-methyl-5-[[5-(4-methyl-1-piperazinyl)-2-pyridinyl]amino]-6-oxo-3-pyridinyl]-2-(hydroxymethyl)phenyl]-8-fluoro-1(2H)-isoquinolinone
- RN468
- RN486/RN-486
- 6-cyclopropyl-8-fluoro-2-(2-(hydroxyMethyl)-3-(1-Methyl-5-(5-(4-Methylpiperazin-1-yl)pyridin-2-ylaMino)-6-oxo-1,6-dihydropyridin-3-yl)phenyl)isoquinolin-1(2H)-one
- 6-cyclopropyl-8-fluoro-2-(2-(hydroxyMethyl)-3-(1-Methyl-5-((5-(4-Methylpiperazin-1-yl)pyridin-2-yl)aMiNA)-6-oxo-1,6-dihydropyridin-3-yl)phenyl)isoquiNAlin-1(2H)-one
- RN486