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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), IC50: 2 nM EGFR (E746_A750/T790M), IC50: 14 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 (L858R), IC50: 0.2 nM EGFR (WT), IC50: 0.3 nM |
98% | |||||||||||||||||
| Erlotinib |
++++
EGFR, IC50: 2 nM |
95% | |||||||||||||||||
| Saracatinib |
+++
EGFR (L861Q), IC50: 4 nM EGFR, IC50: 5 nM |
99%+ | |||||||||||||||||
| AG1557 | ✔ | 99% | |||||||||||||||||
| Rociletinib |
++
EGFR (L858R/T790M), Ki: 21.5 nM EGFR (wt), Ki: 303.3 nM |
98% | |||||||||||||||||
| AG490 |
+
EGFR, IC50: 0.1 μM |
98% | |||||||||||||||||
| Cetuximab |
++++
EGFR, Kd: 0.39 nM |
95% | |||||||||||||||||
| Osimertinib |
++
WT EGFR, IC50: 12.92 nM L858R/T790M EGFR, IC50: 11.44 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/T790M), IC50: 8 nM EGFR (L858R), IC50: 2 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 |
++++
WT EGFR, IC50: 76 nM L858R/T790M EGFR, IC50: 2 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 | ✔ | PARP,Caspase | 99% | ||||||||||||||||
| Zipalertinib |
+++
EGFR WT, IC50: 8 nM EGFR (L861Q), IC50: 4.1 nM |
+++
HER4, IC50: 4 nM |
++++
EGFR(d746-750), IC50: 1.4 nM EGFR L858R, IC50: 2 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 |
++++
EGFRL858R/T790M, IC50: 0.51 nM EGFRT790M, IC50: 0.79 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 (L858R/T790M), IC50: 0.4 nM EGFR (wt), IC50: 0.5 nM |
++
HER2, IC50: 14 nM |
98% | ||||||||||||||||
| Canertinib 2HCl |
+++
EGFR, IC50: 7.4 nM |
+++
ErbB2, IC50: 9 nM |
99% | ||||||||||||||||
| Allitinib tosylate |
++++
EGFR (T790M/L858R), IC50: 12 nM EGFR, IC50: 0.5 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 |
ALK,FLT3 | 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 | ALK1 ↓ ↑ | ALK2 ↓ ↑ | ALK3 ↓ ↑ | ALK4 ↓ ↑ | ALK6 ↓ ↑ | Smad3 ↓ ↑ | TGF-β ↓ ↑ | TGFβRI/ALK5 ↓ ↑ | TGFβRII ↓ ↑ | 其他靶点 | 纯度 | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| LDN193189 |
++++
ALK1, IC50: 0.8 nM |
++++
ALK2, IC50: 0.8 nM |
+++
ALK3, IC50: 5.3 nM |
+++
ALK6, IC50: 16.7 nM |
99%+ | ||||||||||||||
| LDN-212854 |
++++
ALK1, IC50: 2.4 nM |
++++
ALK2, IC50: 1.3 nM |
+
ALK3, IC50: 85.8 nM |
+
ALK4, IC50: 2133 nM |
+
ALK5, IC50: 9276 nM |
99%+ | |||||||||||||
| ML347 |
++
ALK1, IC50: 46 nM |
++
ALK2, IC50: 32 nM |
98% | ||||||||||||||||
| K02288 |
++++
ALK1, IC50: 1.8 nM |
++++
ALK2, IC50: 1.1 nM |
++
ALK3, IC50: 34.4 nM |
+++
ALK6, IC50: 6.4 nM |
99%+ | ||||||||||||||
| LDN-193189 2HCl |
++++
ALK1, IC50: 0.8 nM |
++++
ALK2, IC50: 0.8 nM |
+++
ALK3, IC50: 5.3 nM |
+++
ALK6, IC50: 16.7 nM |
99% | ||||||||||||||
| LDN-214117 |
++
ALK2, IC50: 24 nM |
98% | |||||||||||||||||
| DMH-1 |
+
ALK2, IC50: 107.9 nM |
99%+ | |||||||||||||||||
| SB-505124 |
+
ALK4, IC50: 129 nM |
++
ALK5, IC50: 47 nM |
99%+ | ||||||||||||||||
| Vactosertib |
+++
ALK4, IC50: 13 nM |
+++
ALK5, IC50: 11 nM |
99%+ | ||||||||||||||||
| Alantolactone | ✔ | 98% | |||||||||||||||||
| (E/Z)-SIS3 free base | ✔ | 97% | |||||||||||||||||
| Pirfenidone | ✔ | 98% | |||||||||||||||||
| Hesperetin | ✔ | 97% | |||||||||||||||||
| RepSox |
++++
TGFβR1(ALK5), IC50: 4 nM |
98% | |||||||||||||||||
| GW788388 |
+++
ALK5, IC50: 18 nM |
98% | |||||||||||||||||
| LY364947 |
++
TGFβRI, IC50: 59 nM |
+
TGFβRII, IC50: 0.4 μM |
98% | ||||||||||||||||
| SD-208 |
++
TGF-βRI (ALK5), IC50: 48 nM |
99% | |||||||||||||||||
| SB-525334 |
+++
TGFβR1(ALK5), IC50: 14.3 nM |
99%+ | |||||||||||||||||
| LY2109761 |
++
TβRI, Ki: 38 nM |
+
TβRII, Ki: 300 nM |
99%+ | ||||||||||||||||
| Galunisertib |
++
TβRI, IC50: 56 nM |
98% | |||||||||||||||||
| SB 431542 |
+
ALK5, IC50: 94 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 | Abl ↓ ↑ | Bcr-Abl ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| NVP-BHG 712 |
+
c-Abl, IC50: 1.667 μM |
99%+ | |||||||||||||||||
| KW-2449 |
+++
Abl, IC50: 14 nM Abl (T315I), IC50: 4 nM |
FLT3 | 99%+ | ||||||||||||||||
| Ponatinib |
++++
Abl, IC50: 0.37 nM |
98% | |||||||||||||||||
| AT9283 | 99%+ | ||||||||||||||||||
| Imatinib Mesylate |
+
v-Abl, IC50: 600 nM |
c-Kit,PDGFR | 99% | ||||||||||||||||
| Danusertib |
++
Abl, IC50: 25 nM |
RET | 99%+ | ||||||||||||||||
| Rebastinib |
++++
p-Abl1 (native), IC50: 0.75 nM u-Abl1 (T315I), IC50: 5 nM |
Tie-2,FLT3 | 99%+ | ||||||||||||||||
| PP121 |
++
Abl, IC50: 18 nM |
PDGFR,VEGFR | 99%+ | ||||||||||||||||
| GNF-7 |
+++
E255V, IC50: 122 nM M351T, IC50: 133 nM |
99%+ | |||||||||||||||||
| Olverembatinib dimesylate |
++++
Abl (G250E), IC50: 0.35 nM Abl, IC50: 0.34 nM |
98% | |||||||||||||||||
| Dasatinib monohydrate |
++++
Abl , IC50: 0.6 nM |
Src | 98% | ||||||||||||||||
| Dasatinib |
++++
Abl, IC50: 0.6 nM |
Src | 98% | ||||||||||||||||
| Bafetinib |
+++
Abl, IC50: 5.8 nM |
98+% | |||||||||||||||||
| GNF-2 |
+
Bcr-Abl (SUP-B15 cell line), IC50: 268 nM Bcr-Abl (K562 cell line), IC50: 273 nM |
98%+ | |||||||||||||||||
| Degrasyn |
+
Bcr-Abl, IC50: 1.8 μM |
DUB/Deubiquitinase | 99+% | ||||||||||||||||
| GNF-5 |
++
Bcr-Abl, IC50: 220 nM |
99% | |||||||||||||||||
| Radotinib |
++
BCR-ABL1, IC50: 34 nM |
98+% | |||||||||||||||||
| PD173955 | Src | 99%+ | |||||||||||||||||
| Nilotinib |
++
Bcr-Abl, IC50: <30 nM |
98% | |||||||||||||||||
| 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 |
c-Kit,FLT3 | 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 |
c-Kit,FLT3 | 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 |
+++
hVEGFR2, IC50: 9 nM mVEGF2, IC50: 165 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 |
RET,FLT3 | 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 | ZM-306416, a vascular endothelial growth factor receptor (VEGFR) antagonist, was identified as a potent inhibitor of EGFR function[3]. The VEGFR1/2 inhibitors, ZM306416 and KRN633, lead to a dose-dependent decrease in mineralization[4]. ZM-306416 induced selective anti-proliferative effect toward the EGFR addicted NSCLC cell lines H3255 and HCC4011 (IC50=0.09±0.007 μM and 0.072±0.001 μM respectively), while sparing the wild type EGFR cell lines A549 and H2030 (IC50>10 μM). ZM-306416 is also found to inhibit the ABL in vitro kinase activity with a less potent IC50 value of 1.3±0.2 μM toward the ABL kinase[3]. Ki8751, a selective VEGFR2 inhibitor, completely suppressed the effect of VEGF121 on SCE cell permeability, although ZM306416, a selective VEGFR1 inhibitor, did not affect the VEGF121-induced decrease in TEER (transendothelial electrical resistance)[5]. |
| Concentration | Treated Time | Description | References | |
| Rat Brain Capillary Endothelial Cells (RBEC) | 0.33 µM | Blocked Sema3A-induced paracellular permeability increase in RBEC | Sci Rep. 2015 Jan 20;5:7890. | |
| SVF cells | 25 μM | 160 h | ZM 306416 inhibits VEGFR-1, thereby inhibiting stalk cell phenotype. | In Vitro Cell Dev Biol Anim. 2018 Jan;54(1):32-40. |
| Human iPSC-derived pericytes | 10 µM | 6, 12, 24 h | Validate VEGFA-SMAD3 interactions, found that VEGFR2 inhibitor treatment significantly increased SMAD3 expression | Nat Commun. 2024 Jun 20;15(1):4758. |
| Administration | Dosage | Frequency | Description | References | ||
| Zebrafish | Tg(kdrl:GFP) transgenic zebrafish | Treatment in water | 10 µM | 3 hours per day for three consecutive days | Validate VEGFA-SMAD3 interactions and their impact on BBB integrity, found that VEGFR2 blocker treatment increased the percentage of pSMAD3+ endothelial cells and pericytes, and impaired vascular integrity | Nat Commun. 2024 Jun 20;15(1):4758. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
3.00mL 0.60mL 0.30mL |
14.98mL 3.00mL 1.50mL |
29.96mL 5.99mL 3.00mL |
|
| CAS号 | 690206-97-4 |
| 分子式 | C16H13ClFN3O2 |
| 分子量 | 333.74 |
| SMILES Code | COC1=CC2=NC=NC(NC3=CC=C(Cl)C=C3F)=C2C=C1OC |
| MDL No. | MFCD02683969 |
| 别名 | CB 676475 |
| 运输 | 蓝冰 |
| InChI Key | YHUIUSRCUKUUQA-UHFFFAOYSA-N |
| Pubchem ID | 5329006 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry,2-8°C |
| 溶解方案 |
DMSO: 50 mg/mL(149.82 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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