JNJ-10198409是一种相对选择性、口服活性和ATP竞争性的血小板源性生长因子受体酪氨酸激酶(platelet-derived growth factor receptor ,PDGF-RTK)抑制剂,也是一种双重机制、抗血管生成和抗肿瘤细胞增殖的药物,对PDGFRβ激酶和PDGFRα激酶有良好的抑制活性。


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| 产品名称 | PDGFR ↓ ↑ | PDGFRα ↓ ↑ | PDGFRβ ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Tyrphostin A9 |
+
PDGFR, IC50: 0.5 μM |
EGFR | 98% | ||||||||||||||||
| Tyrphostin AG1296 | 99%+ | ||||||||||||||||||
| Motesanib Diphosphate |
++
PDGFR, IC50: 84 nM |
97% | |||||||||||||||||
| Pazopanib |
++
PDGFR, IC50: 84 nM |
99% | |||||||||||||||||
| Imatinib |
+
PDGFR, IC50: 100 nM |
c-Kit | 98% | ||||||||||||||||
| Imatinib Mesylate |
+
PDGFR, IC50: 100 nM |
c-Kit | 99% | ||||||||||||||||
| Sennoside B | ✔ | 99%+ | |||||||||||||||||
| PP121 |
++++
PDGFR, IC50: 2 nM |
mTOR,VEGFR | 99%+ | ||||||||||||||||
| Crenolanib |
++++
PDGFRα, Kd: 2.1 nM |
++++
PDGFRβ, Kd: 3.2 nM |
99%+ | ||||||||||||||||
| Masitinib |
+
PDGFRα, IC50: 540 nM |
+
PDGFRβ, IC50: 800 nM |
99%+ | ||||||||||||||||
| Ki8751 |
++
PDGFRα, IC50: 67 nM |
c-Kit | 99% | ||||||||||||||||
| Tivozanib |
++
PDGFRα, IC50: 40 nM |
++
PDGFRβ, IC50: 49 nM |
99%+ | ||||||||||||||||
| Ponatinib |
++++
PDGFRα, IC50: 1.1 nM |
98% | |||||||||||||||||
| Amuvatinib |
++
PDGFRα (V561D), IC50: 40 nM |
99%+ | |||||||||||||||||
| Axitinib |
+++
PDGFRα, IC50: 5.0 nM |
++++
PDGFRβ, IC50: 1.6 nM |
98% | ||||||||||||||||
| CP-673451 |
+++
PDGFRα, IC50: 10 nM |
++++
PDGFRβ, IC50: 1 nM |
99%+ | ||||||||||||||||
| Telatinib |
+++
PDGFRα, IC50: 15 nM |
c-Kit | 99%+ | ||||||||||||||||
| Nintedanib |
++
PDGFRα, IC50: 59 nM |
++
PDGFRβ, IC50: 65 nM |
99+% | ||||||||||||||||
| Avapritinib |
++++
PDGFRα (D842V), IC50: 0.5 nM |
99%+ | |||||||||||||||||
| MK-2461 |
+++
PDGFRβ, IC50: 22 nM |
98%+ | |||||||||||||||||
| Lactate |
+++
PDGFRβ, IC50: 27 nM |
FLT3,c-Kit | 85% | ||||||||||||||||
| Linifanib |
++
PDGFRβ, IC50: 66 nM |
99%+ | |||||||||||||||||
| AZD2932 |
+++
PDGFRβ, IC50: 4 nM |
c-Kit | 99% | ||||||||||||||||
| Dovitinib |
+++
PDGFRβ, IC50: 27 nM |
FLT3,c-Kit | 99%+ | ||||||||||||||||
| Sorafenib |
++
mPDGFRβ, IC50: 57 nM PDGFRβ, IC50: 57 nM |
99% | |||||||||||||||||
| Sunitinib |
++++
PDGFRβ , IC50: 2 nM |
FLT3 | 98% | ||||||||||||||||
| Orantinib |
+++
PDGFRβ, Ki: 8 nM |
99%+ | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| Concentration | Treated Time | Description | References | |
| LN-229 | 500 nM | 72 hours | JNJ inhibited the proliferation of LN-229 cells with an IC50 of 39.0 ±1.1 nM and induced G2/M arrest followed by cell death. | Cells. 2018 Sep 6;7(9):131 |
| T98G | 500 nM | 72 hours | JNJ inhibited the proliferation of T98G cells with an IC50 of 26.1 ±1.2 nM and induced G2/M arrest followed by cell death. | Cells. 2018 Sep 6;7(9):131 |
| A172 | 500 nM | 72 hours | JNJ inhibited the proliferation of A172 cells with an IC50 of 44.7 ±1.2 nM and induced G2/M arrest followed by cell death. | Cells. 2018 Sep 6;7(9):131 |
| U87-MG | 500 nM | 72 hours | JNJ inhibited the proliferation of U87-MG cells with an IC50 of 40.4 ±1.1 nM and induced G2/M arrest followed by cell death. | Cells. 2018 Sep 6;7(9):131 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
3.07mL 0.61mL 0.31mL |
15.37mL 3.07mL 1.54mL |
30.74mL 6.15mL 3.07mL |
|
| CAS号 | 627518-40-5 |
| 分子式 | C18H16FN3O2 |
| 分子量 | 325.34 |
| SMILES Code | COC1=CC2=C(C=C1OC)CC3=C2NN=C3NC4=CC=CC(F)=C4 |
| MDL No. | N/A |
| 别名 | |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C |
| 溶解方案 |
DMSO: 85 mg/mL(261.27 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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