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| 产品名称 | EGFR/ErbB1 ↓ ↑ | ErbB3 ↓ ↑ | ErbB4 ↓ ↑ | HER2/ErbB2 ↓ ↑ | mutant EGFR ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| WZ-3146 |
++++
EGFR (E746_A750/T790M), IC50: 14 nM EGFR (E746_A750), IC50: 2 nM |
99%+ | |||||||||||||||||
| Daphnetin |
+
EGFR, IC50: 7.67 μM |
PKA,PKC | 95% | ||||||||||||||||
| Lifirafenib |
++
EGFR, IC50: 29 nM |
+
EGFR(T790M/L858R), IC50: 495 nM |
98% | ||||||||||||||||
| PD168393 |
++++
EGFR, IC50: 0.70 nM |
99%+ | |||||||||||||||||
| Nazartinib |
++
mutant EGFR, Ki: 0.031 μM |
++
mutant EGFR, Ki: 0.031 μM |
98% | ||||||||||||||||
| Norcantharidin | ✔ | 98% | |||||||||||||||||
| CL-387785 |
++++
EGFR, IC50: 370 pM |
98% | |||||||||||||||||
| WHI-P154 |
+++
EGFR, IC50: 4 nM |
Src,VEGFR | 98% | ||||||||||||||||
| Tyrphostin A9 |
+
EGFR, IC50: 460 μM |
PDGFR | 98% | ||||||||||||||||
| AG 555 |
+
EGFR, IC50: 0.7 μM |
98% | |||||||||||||||||
| AG 494 |
+
EGFR, IC50: 1.2 μM |
99%+ | |||||||||||||||||
| AG-556 |
+
EGFR, IC50: 5 μM |
98% | |||||||||||||||||
| RG13022 |
+
EGFR, IC50: 4 μM |
99%+ | |||||||||||||||||
| Tyrphostin RG 14620 | ✔ | 99%+ | |||||||||||||||||
| Vandetanib |
+
EGFR, IC50: 500 nM |
99% | |||||||||||||||||
| CNX-2006 |
++
mutant EGFR, IC50: <20 nM |
++
mutant EGFR, IC50: <20 nM |
99% | ||||||||||||||||
| AZD3759 |
++++
EGFR (WT), IC50: 0.3 nM EGFR (L858R), IC50: 0.2 nM |
98% | |||||||||||||||||
| Erlotinib |
++++
EGFR, IC50: 2 nM |
95% | |||||||||||||||||
| Saracatinib |
+++
EGFR, IC50: 5 nM EGFR (L861Q), IC50: 4 nM |
99%+ | |||||||||||||||||
| AG1557 | ✔ | 99% | |||||||||||||||||
| Rociletinib |
++
EGFR (wt), Ki: 303.3 nM EGFR (L858R/T790M), Ki: 21.5 nM |
98% | |||||||||||||||||
| AG490 |
+
EGFR, IC50: 0.1 μM |
98% | |||||||||||||||||
| Cetuximab |
++++
EGFR, Kd: 0.39 nM |
95% | |||||||||||||||||
| Osimertinib |
++
L858R/T790M EGFR, IC50: 11.44 nM WT EGFR, IC50: 12.92 nM |
98% | |||||||||||||||||
| Osimertinib mesylate | ✔ | 98% (Content MsOH 15.2-18.2%) | |||||||||||||||||
| Chrysophanol | ✔ | mTOR | 98% | ||||||||||||||||
| PD153035 |
++++
EGFR, Ki: 5.2 pM |
99%+ | |||||||||||||||||
| Olmutinib | ✔ | BTK | 99%+ | ||||||||||||||||
| WZ4002 |
++++
EGFR (L858R), IC50: 2 nM EGFR (L858R/T790M), IC50: 8 nM |
99%+ | |||||||||||||||||
| Icotinib |
+++
EGFR, IC50: 5 nM |
99% | |||||||||||||||||
| Desmethyl Erlotinib HCl |
++++
EGFR, IC50: 2 nM |
98% | |||||||||||||||||
| Cyasterone | ✔ | 99%+ | |||||||||||||||||
| PP 3 |
+
EGFR tyrosine kinase, IC50: 2.7 μM |
98% | |||||||||||||||||
| WZ8040 | ✔ | 99%+ | |||||||||||||||||
| (-)-Epigallocatechin Gallate | ✔ | 99% | |||||||||||||||||
| AG 18 |
+
EGFR, IC50: 35 μM |
99%+ | |||||||||||||||||
| O-Desmethyl gefitinib |
++
EGFR, IC50: 36 nM |
99% | |||||||||||||||||
| Falnidamol | ✔ | 99%+ | |||||||||||||||||
| AZ-5104 |
++++
EGFR (L858R), IC50: 6 nM EGFR (L861Q) , IC50: <1 nM |
+++
ErbB4, IC50: 7 nM |
BRK | 99%+ | |||||||||||||||
| Butein | ✔ | 95% | |||||||||||||||||
| Genistein | ✔ | 98% | |||||||||||||||||
| SU5214 |
+
EGFR, IC50: 36.7 μM |
99%+ | |||||||||||||||||
| Naquotinib | ✔ | 99%+ | |||||||||||||||||
| Gefitinib |
++
EGFR, IC50: 15.5 nM |
+
EGFR (858R/T790M), IC50: 823.3 nM |
98% | ||||||||||||||||
| Theliatinib |
+++
WT EGFR, IC50: 3 nM |
++
EGFR T790M/L858R, IC50: 22 nM |
99% | ||||||||||||||||
| Lazertinib |
++++
L858R/T790M EGFR, IC50: 2 nM WT EGFR, IC50: 76 nM |
++++
Del19/T790M, IC50: 1.7 nM |
99%+ | ||||||||||||||||
| Gefitinib-based PROTAC 3 |
++
EGFR, DC50: 22.3 nM |
99%+ | |||||||||||||||||
| MTX-211 | ✔ | PI3K | 98% | ||||||||||||||||
| (E)-AG 99 | ✔ | 99%+ | |||||||||||||||||
| Licochalcone D | ✔ | Caspase,PARP | 99% | ||||||||||||||||
| Zipalertinib |
+++
EGFR WT, IC50: 8 nM EGFR (L861Q), IC50: 4.1 nM |
+++
HER4, IC50: 4 nM |
++++
EGFR L858R, IC50: 2 nM EGFR(d746-750), IC50: 1.4 nM |
97% | |||||||||||||||
| JND3229 |
+++
EGFR WT, IC50: 6.8 nM |
++
EGFR L858R/T790M, IC50: 30.5 nM |
99%+ | ||||||||||||||||
| Firmonertinib mesylate | ✔ | 99%+ | |||||||||||||||||
| Tyrphostin AG30 | ✔ | 99%+ | |||||||||||||||||
| EGFR-IN-12 |
++
EGFR, IC50: 21 nM |
99%+ | |||||||||||||||||
| Mobocertinib | ✔ | 98% | |||||||||||||||||
| (Rac)-JBJ-04-125-02 | ✔ | 95% | |||||||||||||||||
| (S)-Sunvozertinib | ✔ | 99% | |||||||||||||||||
| BLU-945 | ✔ | 95% | |||||||||||||||||
| Poziotinib |
+++
HER1, IC50: 3.2 nM |
++
HER4, IC50: 23.5 nM |
+++
HER2, IC50: 5.3 nM |
98% | |||||||||||||||
| TAK-285 |
++
EGFR/HER1, IC50: 23 nM |
+
HER4, IC50: 260 nM |
++
HER2, IC50: 17 nM |
99%+ | |||||||||||||||
| ARRY-380 analog | ✔ | 99% | |||||||||||||||||
| Canertinib |
++++
EGFR, IC50: 1.5 nM |
+++
ErbB2, IC50: 9.0 nM |
99%+ | ||||||||||||||||
| Dacomitinib |
+++
EGFR, IC50: 6.0 nM |
+
ErbB4, IC50: 73.7 nM |
+
ErbB2, IC50: 45.7 nM |
98% | |||||||||||||||
| EGFR/ErbB-2/ErbB-4 inhibitor-2 |
+
ErbB4, IC50: 1.91 μM |
+
ErbB2, IC50: 0.08 μM |
99%+ | ||||||||||||||||
| (E/Z)-CP-724714 |
++
HER2/ErbB2, IC50: 10 nM |
95% | |||||||||||||||||
| Lapatinib |
++
EGFR, IC50: 10.8 nM |
+
ErbB4, IC50: 367 nM |
+++
ErbB2, IC50: 9.2 nM |
98% | |||||||||||||||
| AEE788 |
++++
EGFR, IC50: 2 nM |
+
HER4/ErbB4, IC50: 160 nM |
+++
HER2/ErbB2, IC50: 6 nM |
c-Fms/CSF1R | 98+% | ||||||||||||||
| AV-412 free base |
++++
EGFR, IC50: 0.75 nM |
++
ErbB2, IC50: 19 nM |
++++
EGFRT790M, IC50: 0.79 nM EGFRL858R/T790M, IC50: 0.51 nM |
98+% | |||||||||||||||
| Neratinib |
+
EGFR, IC50: 92 nM |
+
HER2, IC50: 59 nM |
Src | 98% | |||||||||||||||
| BMS-599626 |
++
HER1, IC50: 20 nM |
+
HER4, IC50: 190 nM |
++
HER2, IC50: 30 nM |
98% | |||||||||||||||
| Tucatinib |
+++
ErbB2, IC50: 8 nM |
98% | |||||||||||||||||
| Allitinib |
++++
EGFR, IC50: 0.5 nM |
++++
ErbB4, IC50: 0.8 nM |
+++
ErbB2, IC50: 3.0 nM |
99% | |||||||||||||||
| Pelitinib |
+
EGFR, IC50: 38.5 nM |
+
ErbB2, IC50: 1.255 μM |
Src,Raf | 99%+ | |||||||||||||||
| Sapitinib |
+++
EGFR, IC50: 4 nM |
+++
ErbB3, IC50: 4 nM |
+++
ErbB2, IC50: 3 nM |
99%+ | |||||||||||||||
| CUDC-101 |
+++
EGFR, IC50: 2.4 nM |
++
HER2, IC50: 15.7 nM |
HDAC | 99%+ | |||||||||||||||
| Varlitinib |
+++
ErbB1, IC50: 7 nM |
++++
ErbB2, IC50: 2 nM |
99%+ | ||||||||||||||||
| Afatinib dimaleate |
++++
EGFR (wt), IC50: 0.5 nM EGFR (L858R/T790M), IC50: 0.4 nM |
++
HER2, IC50: 14 nM |
98% | ||||||||||||||||
| Canertinib 2HCl |
+++
EGFR, IC50: 7.4 nM |
+++
ErbB2, IC50: 9 nM |
99% | ||||||||||||||||
| Allitinib tosylate |
++++
EGFR, IC50: 0.5 nM EGFR (T790M/L858R), IC50: 12 nM |
++++
ErbB4, IC50: 0.8 nM |
+++
ErbB2, IC50: 3.0 nM |
99% | |||||||||||||||
| Tyrphostin AG 528 |
+
EGFR, IC50: 4.9 μM |
+
HER2, IC50: 2.1 μM |
97% | ||||||||||||||||
| Afatinib |
++++
EGFR (wt), IC50: 0.5 nM EGFR (L858R), IC50: 10 nM |
++++
ErbB4, IC50: 1 nM |
++
HER2, IC50: 14 nM |
99% | |||||||||||||||
| Pyrotinib dimaleate |
++
EGFR, IC50: 0.013 μM |
++
HER2, IC50: 0.038 μM |
98% | ||||||||||||||||
| Epertinib HCl |
++++
EGFR, IC50: 1.48 nM |
+++
HER4, IC50: 2.49 nM |
+++
HER2, IC50: 7.15 nM |
99% | |||||||||||||||
| Tuxobertinib |
++++
EGFR, Kd: 0.2 nM |
++++
HER2, Kd: 0.76 nM |
99% | ||||||||||||||||
| ALK-IN-1 |
++
EGFR(del19), IC50: 36.8 nM EGFR(C797S/del19), IC50: 138.6 nM |
ALK | 99% | ||||||||||||||||
| Brigatinib |
+
EGFR(C797S/T790M/del19), IC50: 67.2 nM EGFR(del19), IC50: 39.9 nM |
FLT3,ALK | 98% | ||||||||||||||||
| Avitinib |
++++
EGFR L858R/T790M, IC50: 0.18 nM |
BTK | 99%+ | ||||||||||||||||
| EAI045 | ✔ | 97% | |||||||||||||||||
| Almonertinib | ✔ | 99% | |||||||||||||||||
| BI-4020 |
++++
EGFRdel19 T790M C797S, IC50: 0.2 nM |
99%+ | |||||||||||||||||
| EGFR-IN-7 |
++++
EGFRL858R/T790M, IC50: 0.19 nM EGFRd746-750/T790M/C797S, IC50: 0.26 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。 | |||||||||||||||||||
| 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 |
VEGFR,mTOR | 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。 | |||||||||||||||||||
| 产品名称 | VEGFR1 ↓ ↑ | VEGFR2 ↓ ↑ | VEGFR3 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Motesanib Diphosphate |
++++
VEGFR1, IC50: 2 nM |
++++
VEGFR2/Flk1, IC50: 3 nM VEGFR2, IC50: 3 nM |
+++
VEGFR3, IC50: 6 nM |
RET,PDGFR | 97% | ||||||||||||||
| Tivozanib |
++
VEGFR1, IC50: 30 nM |
+++
VEGFR2, IC50: 6.5 nM |
++
VEGFR3, IC50: 15 nM |
99%+ | |||||||||||||||
| Brivanib |
+
VEGFR1, IC50: 380 nM |
++
Flk1, IC50: 25 nM VEGFR2, IC50: 25 nM |
99%+ | ||||||||||||||||
| Regorafenib |
+++
VEGFR1, IC50: 13 nM |
+++
VEGFR2, IC50: 4.2 nM |
+
VEGFR3, IC50: 46 nM |
RET | 98% | ||||||||||||||
| Pazopanib |
+++
VEGFR1, IC50: 10 nM |
++
VEGFR2, IC50: 30 nM |
+
VEGFR3, IC50: 47 nM |
c-Kit,PDGFR,FGFR | 99% | ||||||||||||||
| Sitravatinib |
+++
VEGFR1 (FLT1), IC50: 6 nM |
+++
VEGFR2 (KDR), IC50: 5 nM |
++++
VEGFR3 (FLT4), IC50: 2 nM |
99%+ | |||||||||||||||
| Foretinib |
+++
VEGFR1/FLT1, IC50: 6.8 nM |
++++
KDR, IC50: 0.86 nM |
++++
VEGFR3/FLT4, IC50: 2.8 nM |
Tie-2 | 99%+ | ||||||||||||||
| MGCD-265 analog |
++++
VEGFR1, IC50: 3 nM |
++++
VEGFR2, IC50: 3 nM |
++++
VEGFR3, IC50: 4 nM |
Tie-2 | 99%+ | ||||||||||||||
| Lactate |
+++
VEGFR1/FLT1, IC50: 10 nM |
+++
VEGFR2/Flk1, IC50: 13 nM |
+++
VEGFR3/FLT4, IC50: 8 nM |
FLT3,c-Kit | 85% | ||||||||||||||
| AEE788 |
+
FLT1, IC50: 59 nM |
+
KDR, IC50: 77 nM |
EGFR | 98+% | |||||||||||||||
| Linifanib |
++++
VEGFR1/FLT1, IC50: 3 nM |
++++
VEGFR2/KDR, IC50: 4 nM |
+
VEGFR3/FLT4, IC50: 190 nM |
FLT3 | 99%+ | ||||||||||||||
| Vatalanib 2HCl |
+
VEGFR1/FLT1, IC50: 77 nM |
++
VEGFR2/Flk1, IC50: 270 nM VEGFR2/KDR, IC50: 37 nM |
+
VEGFR3/FLT4, IC50: 660 nM |
c-Kit,c-Fms/CSF1R | 99%+ | ||||||||||||||
| Axitinib |
++++
VEGFR1/FLT1, IC50: 0.1 nM |
++++
VEGFR2/Flk1, IC50: 0.18 nM VEGFR2/KDR, IC50: 0.2 nM |
98% | ||||||||||||||||
| Dovitinib |
+++
VEGFR1/FLT1, IC50: 10 nM |
+++
VEGFR2/Flk1, IC50: 13 nM |
+++
VEGFR3/FLT4, IC50: 8 nM |
FLT3,c-Kit | 99%+ | ||||||||||||||
| ZM 306416 |
+
VEGFR1, IC50: 0.33 μM |
Src | 99%+ | ||||||||||||||||
| KRN-633 |
+
VEGFR1, IC50: 170 nM |
+
VEGFR2, IC50: 160 nM |
+
VEGFR3, IC50: 125 nM |
BTK,c-Kit | 98% | ||||||||||||||
| OSI-930 |
+++
FLT1, IC50: 8 nM |
+++
KDR, IC50: 9 nM |
99%+ | ||||||||||||||||
| Lenvatinib |
++
VEGFR1/FLT1, IC50: 22 nM |
++++
VEGFR2/KDR, IC50: 4.0 nM |
+++
VEGFR3/FLT4, IC50: 5.2 nM |
98% | |||||||||||||||
| NVP-BAW2881 |
+
hVEGFR1, IC50: 820 nM |
+++
mVEGF2, IC50: 165 nM hVEGFR2, IC50: 9 nM |
+
hVEGFR3, IC50: 420 nM |
99% | |||||||||||||||
| Cediranib |
+++
VEGFR1/FLT1, IC50: 5 nM |
++++
VEGFR2/KDR, IC50: 0.5 nM |
c-Kit | 99%+ | |||||||||||||||
| Nintedanib |
++
VEGFR1, IC50: 34 nM |
+++
VEGFR2, IC50: 13 nM |
+++
VEGFR3, IC50: 13 nM |
FLT3 | 99+% | ||||||||||||||
| BMS-794833 |
++
VEGFR2, IC50: 15 nM |
99%+ | |||||||||||||||||
| SKLB1002 |
++
VEGFR2, IC50: 32 nM |
99% | |||||||||||||||||
| Cabozantinib S-malate |
++++
VEGFR2/KDR, IC50: 0.035 nM |
99+% | |||||||||||||||||
| Ki8751 |
++++
VEGFR2, IC50: 0.9 nM |
c-Kit | 99% | ||||||||||||||||
| SU 5402 |
++
VEGFR2, IC50: 20 nM |
98% | |||||||||||||||||
| Apatinib mesylate |
++++
VEGFR2, IC50: 1 nM |
RET | 98+% | ||||||||||||||||
| Ponatinib |
++++
VEGFR2, IC50: 1.5 nM |
98% | |||||||||||||||||
| LY2874455 |
+++
VEGFR2, IC50: 7 nM |
99%+ | |||||||||||||||||
| ZM323881 HCl |
++++
VEGFR2, IC50: <2 nM |
98% | |||||||||||||||||
| AZD2932 |
+++
VEGFR-2, IC50: 8 nM |
c-Kit | 99% | ||||||||||||||||
| Cabozantinib |
++++
VEGFR2/KDR, IC50: 0.035 nM |
98% | |||||||||||||||||
| Sorafenib |
++
VEGFR2/Flk1, IC50: 90 nM VEGFR2, IC50: 90 nM |
99% | |||||||||||||||||
| CYC-116 |
++
VEGFR2, Ki: 44 nM |
FLT3 | 99%+ | ||||||||||||||||
| Golvatinib |
++
VEGFR2, IC50: 16 nM |
99%+ | |||||||||||||||||
| Sunitinib |
+
VEGFR2 , IC50: 80 nM |
FLT3 | 98% | ||||||||||||||||
| RAF265 |
++
VEGFR2, EC50: 30 nM |
99%+ | |||||||||||||||||
| PD173074 | 99%+ | ||||||||||||||||||
| BFH772 |
++++
VEGFR2, IC50: 3 nM |
98% | |||||||||||||||||
| Semaxinib |
+
VEGFR2/Flk1, IC50: 1.23 μM |
98% | |||||||||||||||||
| Vandetanib |
++
VEGFR2, IC50: 40 nM |
+
VEGFR3, IC50: 110 nM |
EGFR | 99% | |||||||||||||||
| SAR131675 |
++
VEGFR3, IC50: 23 nM |
99%+ | |||||||||||||||||
| ENMD-2076 |
+
VEGFR2/KDR, IC50: 58.2 nM |
++
VEGFR3/FLT4, IC50: 15.9 nM |
FLT3,RET | 98% | |||||||||||||||
| Telatinib |
+++
VEGFR2, IC50: 6 nM |
++++
VEGFR3, IC50: 4 nM |
c-Kit | 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 | SU5402 is potent and selective vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) inhibitor. |
| Concentration | Treated Time | Description | References | |
| Human periodontal ligament cells | 10 µM | 24-48 hours | To evaluate the effect of SU5402 on reversing FGF-2-mediated inhibition of SDF-1 α expression, results showed that SU5402 could inhibit the FGF-2-reduced expression of SDF-1 α | Int J Mol Med. 2012 Apr;29(4):569-73. |
| Primary dental pulp cells | 5, 10, 20 µM | 3 to 7 days | Inhibited FGFR signaling pathway, reducing FGF2-mediated increases in Dmp1 and Dspp expression | J Dent Res. 2015 Nov;94(11):1582-90. |
| Primate astrocytes | 25 µM | 48 hours | To assess the effect of SU5402 on primate astrocyte migration and proliferation, results showed that SU5402 completely inhibited astrocyte migration and proliferation. | J Neurosci. 2012 May 30;32(22):7477-92. |
| Mouse spermatogonial stem cells (mSPG) | 10 µM | 5 days | Blocking sFGF2 signaling significantly reduced the in vitro propagation of high-density cultured mSPG, leading to decreased mitosis and increased apoptosis | Cell Res. 2012 Apr;22(4):773-6. |
| Bladder tumour cell lines | 0–50 µM | 5 days | To evaluate the effect of SU5402 on the proliferation and viability of bladder tumour cells, results showed that SU5402 inhibited the proliferation and viability of FGFR3 mutant and wild-type cell lines at micromolar concentrations. | Br J Cancer. 2011 Jan 4;104(1):75-82. |
| Human pluripotent stem cells (hPSCs) | 10 µM | 8 days | SU5402, in combination with CHIR99021 and DAPT, accelerates the differentiation of hPSCs into neurons and induces TUBB3 expression by day 10. | Nat Biotechnol. 2012 Jul 1;30(7):715-20. |
| Human pluripotent stem cells | 10 µM | 8 days | SU5402, in combination with Activin A, further decreased the expression of the early eye field/neural retina marker Rax, indicating its role in directing cells toward the retinal pigment epithelium (RPE) fate during the optic vesicle to optic cup stages of eye development. | Stem Cells Transl Med. 2013 May;2(5):384-93. |
| Mouse embryonic fibroblasts (MEFs) | 10 µM | MSPG did not expand in the 5F-MCM-SU5402 medium, indicating that the IVP-promoting effect of sFGF2 was mediated by receptors both on mSPG and on MEFs under normal culture conditions | Cell Res. 2012 Apr;22(4):773-6. | |
| MDCK cells | 10 µM | 48 hours | Assessment of /H9004F508-CFTR chloride channel activity by short-circuit current analysis in Ussing chambers | Mol Cell Proteomics. 2012 Sep;11(9):745-57. |
| BHK cells | 10 µM | 48 hours | Validation of /H9004F508-CFTR cell surface expression by flow cytometry | Mol Cell Proteomics. 2012 Sep;11(9):745-57. |
| Administration | Dosage | Frequency | Description | References | ||
| Chicken | NMDA-induced retinal damage model | Intravitreal injection | 0.8 μg/dose | Injected 6 hours and 24 hours after NMDA treatment, lasting for 3 days | Inhibit FGF receptor, reduce proliferation of Müller glia | Glia. 2009 Jan 15;57(2):166-81 |
| C57BL/6 mice | Chronic Unpredictable Stress Model | Intracerebroventricular injection | 2.5 μg/day | Once daily for 9 days | SU5402 blocked the antidepressant behavioral effects of fluoxetine in the CUS model and blocked fluoxetine-induced cell proliferation in the PFC | Biol Psychiatry. 2012 Aug 15;72(4):258-65 |
| Zebrafish | Spinal cord injury model | Injection at the lesion site | 5 µg/µl | Single injection, observed up to 3 weeks | To assess the effect of SU5402 on glial cell proliferation, migration, and axonal regeneration post-spinal cord injury in zebrafish, results showed that SU5402 inhibited glial cell proliferation and migration and prevented axonal regeneration. | J Neurosci. 2012 May 30;32(22):7477-92. |
| Mice | Sumf1/ mice | Intraperitoneal injection | 500 µM | Single injection, analyzed at P21–P27 | By inhibiting FGF1 signaling in vivo with SU5402, the terminal differentiation of Sumf1/ mice was unlocked. The results showed that SU5402 significantly increased the frequency of intermediate precursors and terminally differentiated CD71Ter119+ cells in the BM, indicating the rescue of the block of erythroid lineage differentiation | J Exp Med. 2010 Aug 2;207(8):1647-60 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
3.37mL 0.67mL 0.34mL |
16.87mL 3.37mL 1.69mL |
33.75mL 6.75mL 3.37mL |
|
| CAS号 | 215543-92-3 |
| 分子式 | C17H16N2O3 |
| 分子量 | 296.32 |
| SMILES Code | O=C(O)CCC1=C(/C=C2C(NC3=C\2C=CC=C3)=O)NC=C1C |
| MDL No. | MFCD08235144 |
| 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, 2-8°C |
| 溶解方案 |
DMSO: 30 mg/mL(101.24 mM),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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