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SB525334

SB525334用途

SB 525334是一种有效,选择性的转化生长因子β1受体 (ALK5) 抑制剂,IC50 为 14.3 nM。

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SB525334名称

[ CAS 号 ]:
356559-20-1

[ 中文名 ]:
6-[2-叔丁基-5-(6-甲基-吡啶-2-基)-1H-咪唑-4-基]-喹噁啉

[ 英文名 ]:
SB525334

[中文别名 ]:

[英文别名 ]:

SB 525334
S1476_Selleck
SB525334

SB525334生物活性

[ 描述 ]:

SB 525334是一种有效,选择性的转化生长因子β1受体 (ALK5) 抑制剂,IC50 为 14.3 nM。

[ 相关类别 ]:

信号通路 >> TGF-beta/Smad 信号通路 >> TGF-β受体

研究领域 >> 癌症

[参考文献]

[1]. Grygielko ET, et al. Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-beta type I receptor kinase in puromycin-induced nephritis. J Pharmacol Exp Ther, 2005, 313(3), 943-951.

[2]. Thomas M, et al. Activin-like kinase 5 (ALK5) mediates abnormal proliferation of vascular smooth muscle cells from patients with familial pulmonary arterial hypertension and is involved in the progression of experimental pulmonary arterial hypertension induced by monocrotaline. Am J Pathol, 2009, 174(2), 380-389.

[3]. Laping NJ, et al. Tumor-specific efficacy of transforming growth factor-beta RI inhibition in Eker rats. Clin Cancer Res, 2007, 13(10), 3087-3899.

[相关活性小分子]

SB431542 | Galunisertib (LY2157299) | 3-(6-甲基-2-吡啶基)-N-苯基-4-(4-喹啉基)-1H-吡唑-1-硫代甲酰胺 | 4-[5,6-二氢-2-(2-吡啶)-4H-吡咯并[1,2-b]吡唑-3-基]-7-[2-(4-吗啉)乙氧基]喹啉 | LDN193189 | 2-(3-(6-甲基吡啶-2-基)-1H-吡唑-4-基)-1,5-萘啶 | EW-7197 | 4-[6-[4-异丙氧基苯基]吡唑并[1,5-a]嘧啶-3-基]喹啉 | 4-[4-[3-(吡啶-2-基)-1H-吡唑-4-基]吡啶-2-基]-N-(四氢吡喃-4-基)苯甲酰胺 | LY-364947 | SB-505124 | LY3200882 | LSKL, 血小板反应蛋白抑制剂 (TSP-1) | 4-[1,1'-联苯]-4-基-1,4,5,6,7,8-六氢-2,7,7-三甲基-5-氧代-3-喹啉羧酸乙酯 | K02288

SB525334物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
540.5±45.0 °C at 760 mmHg

[ 熔点 ]:
159 °C

[ 分子式 ]:
C₂₁H₂₁N₅

[ 分子量 ]:
343.425

[ 闪点 ]:
238.6±21.7 °C

[ 精确质量 ]:
343.179688

[ PSA ]:
67.35000

[ LogP ]:
4.05

[ 外观性状 ]:
yellow

[ 蒸汽压 ]:
0.0±1.4 mmHg at 25°C

[ 折射率 ]:
1.636

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
DMSO: ≥20mg/mL

SB525334MSDS

详细MSDS(安全技术说明书)

SB525334安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H315-H319-H335-H413

[ 警示性声明 ]:
P261-P301 + P310-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22-36/37/38

[ 安全声明 (欧洲) ]:
26

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

[ 危险类别 ]:
6.1

[ 海关编码 ]:
2934999090

SB525334海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

SB525334文献

Mesenchymal activin-A overcomes defective human trisomy 21 trophoblast fusion.

Endocrinology 152 , 5017-28, (2011)

Placental development is markedly abnormal in trisomy 21 (T21) pregnancies. We hypothesized that abnormal paracrine cross talk between the fetal mesenchymal core and the trophoblast might be involved ...

Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-beta type I receptor kinase in puromycin-induced nephritis.

J. Pharmacol. Exp. Ther. 313 , 943-951, (2005)

SB-525334 (6-[2-tert-butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl]-quinoxaline) has been characterized as a potent and selective inhibitor of the transforming growth factor-beta1 (TGF-beta1) recep...

Activin-Like Kinase 5 (ALK5) Mediates Abnormal Proliferation of Vascular Smooth Muscle Cells from Patients with Familial Pulmonary Arterial Hypertension and Is Involved in the Progression of Experimental Pulmonary Arterial Hypertension Induced by Monocrotaline

Am. J. Pathol. 174(2) , 380-9, (2009)

Mutations in the gene for the transforming growth factor (TGF)-β superfamily receptor, bone morphogenetic protein receptor II, underlie heritable forms of pulmonary arterial hypertension (PAH). Aberra...

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