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| 产品名称 | FGFR ↓ ↑ | FGFR1 ↓ ↑ | FGFR2 ↓ ↑ | FGFR3 ↓ ↑ | FGFR4 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Tyrphostin AG1296 |
+
FGFR (Swiss 3T3), IC50: 12.3 μM |
PDGFR | 99%+ | ||||||||||||||||
| Pazopanib |
+
FGFR, IC50: 140 nM |
99% | |||||||||||||||||
| Erdafitinib | ✔ | RET | 99%+ | ||||||||||||||||
| Gambogenic acid | ✔ | 98+% | |||||||||||||||||
| Sulfatinib |
+++
FGFR1, IC50: 15 nM |
99+% | |||||||||||||||||
| Nintedanib esylate |
+
FGFR1, IC50: 69 nM |
++
FGFR2, IC50: 37 nM |
+
FGFR3, IC50: 108 nM |
98% | |||||||||||||||
| Zoligratinib |
+++
FGFR1, IC50: 9.3 nM |
+++
FGFR2, IC50: 7.6 nM |
++
FGFR3, IC50: 22 nM |
+
FGFR4, IC50: 290 nM |
99%+ | ||||||||||||||
| MK-2461 |
+
FGFR1, IC50: 65 nM |
++
FGFR2, IC50: 39 nM |
++
FGFR3, IC50: 50 nM |
98%+ | |||||||||||||||
| SU 5402 |
++
FGFR1, IC50: 30 nM |
98% | |||||||||||||||||
| Brivanib |
+
FGFR1, IC50: 148 nM |
99%+ | |||||||||||||||||
| Lucitanib |
++
FGFR1, IC50: 17.5 nM |
+
FGFR2, IC50: 82.5 nM |
99%+ | ||||||||||||||||
| Ponatinib |
++++
FGFR1, IC50: 2.2 nM |
98% | |||||||||||||||||
| PD-166866 |
+
FGFR1, IC50: 52.4 nM |
99% | |||||||||||||||||
| Narazaciclib |
++
FGFR1, IC50: 26 nM |
RET | 99%+ | ||||||||||||||||
| Lactate |
+++
FGFR1, IC50: 8 nM |
+++
FGFR3, IC50: 9 nM |
FLT3,c-Kit | 85% | |||||||||||||||
| Lenvatinib mesylate |
++
FGFR1, IC50: 46 nM |
c-RET | 99% | ||||||||||||||||
| LY2874455 |
++++
FGFR1, IC50: 2.8 nM |
++++
FGFR2, IC50: 2.6 nM |
+++
FGFR3, IC50: 6.4 nM |
+++
FGFR4, IC50: 6 nM |
99%+ | ||||||||||||||
| FIIN-2 |
+++
FGFR1, IC50: 3.09 nM |
+++
FGFR2, IC50: 4.3 nM |
++
FGFR3, IC50: 27 nM |
++
FGFR4, IC50: 45.3 nM |
99% | ||||||||||||||
| FIIN-3 |
+++
FGFR1, IC50: 13.1 nM |
++
FGFR2, IC50: 21 nM |
++
FGFR3, IC50: 31.4 nM |
++
FGFR4, IC50: 35.3 nM |
98% | ||||||||||||||
| Infigratinib |
++++
FGFR1, IC50: 0.9 nM |
++++
FGFR2, IC50: 1.4 nM |
++++
FGFR3, IC50: 1.0 nM FGFR3 (K650E), IC50: 4.9 nM |
+
FGFR4, IC50: 60 nM |
99%+ | ||||||||||||||
| Danusertib |
++
FGFR1, IC50: 47 nM |
RET | 99%+ | ||||||||||||||||
| R1530 |
++
FGFR1, IC50: 28 nM |
98% | |||||||||||||||||
| ENMD-2076 |
+
FGFR1, IC50: 92.7 nM |
+
FGFR2, IC50: 70.8 nM |
RET,FLT3 | 98% | |||||||||||||||
| Dovitinib |
+++
FGFR1, IC50: 8 nM |
+++
FGFR3, IC50: 9 nM |
FLT3,c-Kit | 99%+ | |||||||||||||||
| Sorafenib |
+
FGFR1, IC50: 580 nM |
99% | |||||||||||||||||
| SSR128129E |
+
FGFR1, IC50: 1.9 μM |
99%+ | |||||||||||||||||
| AZD-4547 |
++++
FGFR1, IC50: 0.2 nM |
++++
FGFR2, IC50: 2.5 nM |
++++
FGFR3, IC50: 1.8 nM |
98% | |||||||||||||||
| Lenvatinib |
++
FGFR1, IC50: 46 nM |
RET | 98% | ||||||||||||||||
| PD173074 |
++
FGFR1, IC50: ~25 nM |
99%+ | |||||||||||||||||
| S49076 |
++
FGFR1, IC50: 18 nM |
+++
FGFR2, IC50: 17 nM |
+++
FGFR3, IC50: 15 nM |
98% | |||||||||||||||
| Futibatinib |
++++
FGFR1, IC50: 1.8 nM |
++++
FGFR2, IC50: 1.4 nM |
++++
FGFR3, IC50: 1.6 nM |
+++
FGFR4, IC50: 3.7 nM |
99%+ | ||||||||||||||
| Ferulic Acid |
+
FGFR1, IC50: 3.78 μM |
+
FGFR2, IC50: 12.5 μM |
98% | ||||||||||||||||
| Nintedanib |
+
FGFR1, IC50: 69 nM |
++
FGFR2, IC50: 37 nM |
+
FGFR3, IC50: 108 nM |
+
FGFR4, IC50: 610 nM |
99+% | ||||||||||||||
| ASP5878 |
++++
FGFR1, IC50: 0.47 nM |
++++
FGFR2, IC50: 0.6 nM |
++++
FGFR3, IC50: 0.74 nM |
+++
FGFR4, IC50: 3.5 nM |
99% | ||||||||||||||
| PRN1371 |
++++
FGFR1, IC50: 0.6 nM |
++++
FGFR2, IC50: 1.3 nM |
+++
FGFR3, IC50: 4.1 nM |
++
FGFR4, IC50: 19.3 nM |
99% | ||||||||||||||
| Derazantinib |
+++
FGFR1, IC50: 4.5 nM |
++++
FGFR2, IC50: 1.8 nM |
+++
FGFR3, IC50: 4.5 nM |
++
FGFR4, IC50: 34 nM |
RET | 99%+ | |||||||||||||
| ODM-203 |
+++
FGFR1, IC50: 11 nM |
+++
FGFR2, IC50: 16 nM |
+++
FGFR3, IC50: 6 nM |
++
FGFR4, IC50: 35 nM |
99%+ | ||||||||||||||
| Pemigatinib |
++++
FGFR1, IC50: 0.4 nM |
++++
FGFR2, IC50: 0.5 nM |
++++
FGFR3, IC50: 1.2 nM |
++
FGFR4, IC50: 30 nM |
99%+ | ||||||||||||||
| SKLB 610 | ✔ | PDGFR | 99%+ | ||||||||||||||||
| Alofanib | ✔ | 99%+ | |||||||||||||||||
| Lirafugratinib | ✔ | 99% | |||||||||||||||||
| Masitinib mesylate | ✔ | FAK | 99%+ | ||||||||||||||||
| BLU9931 |
+
FGFR3, IC50: 150 nM |
+++
FGFR4, IC50: 3 nM |
99%+ | ||||||||||||||||
| BO-264 | ✔ | 99%+ | |||||||||||||||||
| Fisogatinib |
+++
FGFR4, IC50: 5 nM |
99%+ | |||||||||||||||||
| H3B-6527 |
++++
FGFR4, IC50: <1.2 nM |
99%+ | |||||||||||||||||
| Roblitinib |
++++
FGFR4, IC50: 1.9 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。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | PRN1371 is an irreversible covalent FGFR inhibitor used for the treatment of solid tumor. |
| Concentration | Treated Time | Description | References | |
| KAI-3 | KAI-3 | PRN371 inhibited the downstream effector proteins of JAK3-STAT signaling in KAI-3 cells | Leukemia. 2018 May;32(5):1147-1156. | |
| NK92 | NK92 | PRN371 inhibited the downstream effector proteins of JAK3-STAT signaling in NK92 cells | Leukemia. 2018 May;32(5):1147-1156. | |
| CMK | CMK | PRN371 dose-dependently suppressed the growth of CMK cells and induced apoptosis through abrogation of JAK3-STAT signaling | Leukemia. 2018 May;32(5):1147-1156. | |
| NK-S1 | NK-S1 | PRN371 dose-dependently suppressed the growth of NK-S1 cells and induced apoptosis through abrogation of JAK3-STAT signaling | Leukemia. 2018 May;32(5):1147-1156. |
| Administration | Dosage | Frequency | Description | References | ||
| NOD/SCID mice | NK-S1 subcutaneous xenograft model | Intraperitoneal injection | 25 or 50 mg/kg | Once daily for 14 days | PRN371 significantly inhibited tumor growth in the NK-S1 xenograft model without causing significant weight loss or toxicity | Leukemia. 2018 May;32(5):1147-1156. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.78mL 0.36mL 0.18mL |
8.91mL 1.78mL 0.89mL |
17.81mL 3.56mL 1.78mL |
|
| CAS号 | 1802929-43-6 |
| 分子式 | C26H30Cl2N6O4 |
| 分子量 | 561.46 |
| SMILES Code | O=C1C(C2=C(Cl)C(OC)=CC(OC)=C2Cl)=CC3=CN=C(NC)N=C3N1CCCN4CCN(C(C=C)=O)CC4 |
| MDL No. | MFCD31560471 |
| 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, inert atmosphere, store in freezer, under -20°C |
| 溶解方案 |
DMSO: 25 mg/mL(44.53 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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