PLX647
PLX647 物理性質
- 比重(密度) :
- 1.358±0.06 g/cm3(Predicted)
- 貯蔵温度 :
- 2-8°C
- 溶解性:
- DMSO:可溶20mg/mL、透明
- 外見 :
- 粉
- 酸解離定数(Pka):
- 13.73±0.40(Predicted)
- 色:
- 白からベージュ
メーカー |
製品番号 |
製品説明 |
CAS番号 |
包装 |
価格 |
更新時間 |
購入 |
Sigma-Aldrich Japan
|
SML0966 |
≥98% (HPLC)
PLX647 ≥98% (HPLC) |
873786-09-5 |
5mg |
¥21800 |
2018-12-25 |
購入 |
Sigma-Aldrich Japan
|
SML0966 |
≥98% (HPLC)
PLX647 ≥98% (HPLC) |
873786-09-5 |
25mg |
¥88000 |
2018-12-25 |
購入 |
PLX647 化学特性,用途語,生産方法
説明
PLX647 is a dual inhibitor of the receptor tyrosine kinases FMS and KIT (IC
50s = 28 and 16 nM, respectively). It is selective for FMS and KIT but does inhibit FLT3 and KDR (IC
50s = 91 and 130 nM, respectively) in a panel of 400 kinases at a concentration of 1 μM. PLX647 inhibits proliferation of Ba/F3 cells expressing constitutively active FMS or KIT (IC
50s = 92 and 180 nM, respectively) as well as ligand-dependent growth of M-NFS-60 and M-07e cells that express endogenous FMS and KIT, respectively (IC
50s = 380 and 230 nM, respectively). It has no effect on HEK293T or HepG2 cells that lack FMS and KIT (IC
50 = >50 μM) or Ba/F3 cells overexpressing KDR (IC
50 = >5 μM). PLX647 also inhibits differentiation of human osteoclast precursor cells (IC
50 = 170 nM).
In vivo, PLX647 (40 mg/kg) reduces TNF-α and IL-6 release in a rat model of LPS-induced cytokine release. It reduces mast cell degranulation in a mouse model of passive cutaneous anaphylaxis (PCA) and inhibits bone destruction and delays disease progression in a mouse model of collagen-induced arthritis (CIA). PLX647 also reverses bone osteolysis and allodynia in a syngeneic rat model of cancer-induced bone pain.
使用
PLX647 is a novel tyrosine kinase (TK) inhibitor, which selectively targets c-Kit and c-Fms.
PLX647 上流と下流の製品情報
原材料
準備製品
PLX647 生産企業
Global( 63)Suppliers
873786-09-5()キーワード:
- 873786-09-5
- PLX647
- PLC647
- 5-(1H-Pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]-2-pyridinamine
- [5-[(1H-Pyrrolo[2,3-b]pyridin-3-yl)methyl]pyridin-2-yl](4-trifluoromethylbenzyl)amine
- 2-Pyridinamine, 5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]-
- PLX 647;PLX-647
- CS-1696
- 5-({1H-pyrrolo[2,3-b]pyridin-3-yl}methyl)-N-{[4-(trifluoromethyl)phenyl]methyl}pyridin-2-amine