小分子抑制剂、激动剂、拮抗剂--血管生成信号通路 - 图文

血管生成

血管生成，即从已存在的血管中生成新血管。此通路是通过人体中存在的诸多互补和复杂的信号途径调节的。正常情况下，血管生成的相关诱导剂和抑制剂之间保持平衡状态。但对于创伤、缺氧或炎症继发等微环境破坏的条件下，此通路能做出迅速的应答。在各种慢性病理和肿瘤的情况下，血管生成的平衡状态被打破，导致异常的血管生成或新生血管。

血管生成信号通路转导过程

血管生成的激活导致促血管生成生长因子（VEGF、PDGF、FGF和TGF等）的释放，这些因子将其受体结合到已有血管内的内皮细胞上，从而诱导PI3K/Akt、Erk1/2、Smad和Notch等多种途径的信号转导，引起内皮细胞增殖和迁移。内皮细胞利用基质金属蛋白酶和整合素来消化细胞外基质，迁移到新的区域，在那里它们延长并形成管子，产生新的血管。

在肿瘤血管生成过程中，癌细胞刺激新血管的形成，为肿瘤输送氧气和营养。随着肿瘤的生长，位于肿瘤中心的细胞缺氧，使得转录因子HIF-1α（缺氧诱导因子-1）稳定表达。该转录因子与HIF-1β结合上调几种促血管生成基因的表达。此外，生长因子信号还刺激HIF-1活性，以维持生长细胞的氧稳态。

血管生成信号通路图

按靶点分类

*FLT 名称 CAS 细胞 无细胞 Sorafenib Tosylate 475207-59-1 靶点 Raf-1 B-Raf VEGFR-2 VEGFR-3 PDGFR-β Flt-3 c-KIT Tozasertib SP600125 639089-54-6 129-56-6 FLT3 JNK1 无细胞 JNK2 JNK3 Foretinib (GSK1363089) 849217-64-7 无细胞 Met KDR Quizartinib (AC220) 950769-58-1 MV4-11 Flt3(ITD) RS4;11 Flt3(WT) Dovitinib (TKI-258, CHIR-258) Fedratinib (SAR302503, TG101348) 405169-16-6 936091-26-8 无细胞 FLT3 c-Kit 无细胞 JAK2 Linifanib (ABT-869) 796967-16-3 KDR CSF-1R Flt-1/3 PDGFRβ Crenolanib (CP-868596) R406 (free base) Amuvatinib (MP-470) Tandutinib (MLN518) TG101209 KW-2449 ENMD-2076 LDK378 670220-88-9 841290-80-0 850879-09-3 387867-13-2 936091-14-4 1000669-72-6 934353-76-1 1032900-25-6 PDGFRα PDGFRβ Syk c-Kit PDGFα Flt3 FLT3 无细胞 JAK2 Flt3 RET Flt3 Aurora A Flt3 无细胞 ALK IGF-1R 6 nM 22 nM 90 nM 20 nM 57 nM 59 nM 68 nM 30 nM 40 nM 40 nM 90 nM 0.4 nM 0.9 nM 1.1 nM/4.2 nM 1.1 nM/4.2 nM 1 nM 2 nM 3 nM 4 nM 3 nM 3 nM/4 nM 66 nM 2.1 nM 3.2 nM 41 nM 10 nM 40 nM 81 nM 0.22 μM 6 nM 25 nM 17 nM 6.6 nM 14 nM 1.86 nM 0.2 nM 8 nM IC50 Ki

PRT062607 (P505-15, BIIB057) HCl 1370261-97-4 InsR STK22D FLT3 Raf-1 B-Raf VEGFR-2 VEGFR-3 PDGFR-β Flt-3 c-KIT 7 nM 23 nM 60 nM 1 nM 6 nM 22 nM 90 nM 20 nM 57 nM 59 nM 68 nM 0.035 nM 1.3 nM 4 nM 4.6 nM 12 nM/11.3 nM/6 nM 14.3 nM 7 nM 43 nM 14 nM 0.29 nM 0.73 nM 20 nM 10 nM 160 nM 2 nM 无细胞 Syk 无细胞 Sorafenib 284461-73-0 VEGFR2 c-Met Ret Kit Cabozantinib malate (XL184) 1140909-48-3 无细胞 Flt-1/3/4 Tie2 AXL TCS 359 ENMD-2076 L-(+)-Tartaric acid LY2801653 Crotonoside Gilteritinib 301305-73-7 1291074-87-7 1206799-15-6 1818-71-9 1254053-43-4 FLT3 Aurora A VEGFR(Flt3) 1.86 nM Pexidartinib *DNA alkylator 名称 CAS 细胞 无细胞 Sorafenib Tosylate 475207-59-1 靶点 Raf-1 B-Raf VEGFR-2 VEGFR-3 PDGFR-β Flt-3 c-KIT Sunitinib Malate 341031-54-7 无细胞 VEGFR2 (Flk-1) PDGFRβ IC50 6 nM 22 nM 90 nM 20 nM 57 nM 59 nM 68 nM 80 nM 2 nM EC50 1029044-16-3 MET FLT3 HDAC3/6 FLT3 AXL CSF-1R Kit FLT3 Ki

Lenalidomide 191732-72-6 PBMCs 无细胞 TNF-α VEGFR2 c-Met Ret Kit 13 nM 0.035 nM 1.3 nM 4 nM 4.6 nM 12 nM/11.3 nM/6 nM 14.3 nM 7 nM 0.37 nM 1.1 nM 1.5 nM 2.2 nM 5.4 nM 2 nM 12 nM 451 nM 217 nM 0.1 nM 0.2 nM 0.1-0.3 nM 1.6 nM 1.7 nM 0.4 nM 0.9 nM 34 nM 13 nM 13 nM 69 nM 37 nM 108 nM 59 nM 65 nM 40 nM 110 nM 500 nM 13 nM 4.2 nM 46 nM 22 nM 7 nM 1.5 nM 2.5 nM Cabozantinib (XL184, BMS-907351) 849217-68-1 Flt-1/3/4 Tie2 AXL Abl PDGFRα Ponatinib (AP24534) 943319-70-8 无细胞 VEGFR2 FGFR1 Src Ki20247 623142-96-1 KDR VEGFR-2 c-Kit PDGFRβ VEGFR1 VEGFR2 VEGFR3 PDGFRβ c-Kit Met KDR VEGFR1 VEGFR2 VEGFR3 FGFR1 FGFR2 FGFR3 PDGFRα PDGFRβ VEGFR2 Axitinib 猪主动319460-85-0 脉内皮细胞 Foretinib (GSK1363089) 849217-64-7 无细胞 Nintedanib (BIBF 1120) 656247-17-5 无细胞 Vandetanib (ZD6474) 443913-73-3 无细胞 VEGFR3 EGFR VEGFR1 VEGFR2 VEGFR3 Regorafenib (BAY 73-4506) 755037-03-7 无细胞 PDGFR-β Kit RET Raf-1

VEGFR1 VEGFR2 VEGFR3 Pazopanib HCl (GW786034 HCl) 635702-64-6 无细胞 PDGFR FGFR c-Kit c-fms Cediranib 288383-20-0 PD173074 219580-11-7 VEGFR(KDR) Flt1/4 FGFR1 VEGFR2 FLT3 c-Kit KDR CSF-1R Flt-1/3 PDGFRβ Vatalanib (PTK787) 2HCl RAF265 (CHIR-265) 212141-51-0 无细胞 927880-90-8 Tivozanib (AV-951) 475108-18-0 Motesanib Diphosphate (AMG-706) 857876-30-3 Lenvatinib (E7080) Brivanib (BMS-540215) MGCD-265 AEE788 (NVP-AEE788) ENMD-2076 417716-92-8 649735-46-6 875337-44-3 497839-62-0 934353-76-1 OSI-930 728033-96-3 CYC116 693228-63-6 Aurora B VEGFR2/KDR VEGFR2 B-Raf VEGFR1 VEGFR2 VEGFR3 VEGFR1 VEGFR2 VEGFR3 VEGFR3(Flt-4) VEGFR2 c-Met VEGFR1/2/3 EGFR HER2/ErbB2 Aurora A Flt3 Kit KDR CSF-1R Aurora A 10 nM 30 nM 47 nM 84 nM 74 nM 140 nM 146 nM <1 nM 5 nM/≤3 nM 25 nM 100-200 nM 1 nM 2 nM 4 nM 3 nM 66 nM 37 nM 3-60 nM 0.21 nM 0.16 nM 0.24 nM 2 nM 3 nM 6 nM 30 nM 8.0 nM 9.2 nM Dovitinib (TKI-258, CHIR-258) 405169-16-6 无细胞 Linifanib (ABT-869) 796967-16-3 3 nM/4 nM VEGFR2(KDR) 4 nM 5.2 nM 25 nM 1 nM 2 nM 6 nM 14 nM 1.86 nM 80 nM 9 nM 15 nM 3 nM/3 nM/4 nM

VEGFR2 Ki8751 Telatinib 228559-41-9 332012-40-5 VEGFR2 VEGFR2/3 c-Kit PDGFRα PDGFR Hck PP121 1092788-83-4 mTOR VEGFR2 Src Abl DNA-PK GFR1 VEGFR2 VEGFR3 Pazopanib 444731-52-6 PDGFR FGFR c-Kit KRN-633 286370-15-8 1433953-83-3 1174046-72-0 VEGFR1 VEGFR2 VEGFR3 SAR131675 BMS-794833 VEGFR3 Met VEGFR2 无细胞 Sorafenib 284461-73-0 Raf-1 B-Raf VEGFR-2 VEGFR-3 PDGFR-β Flt-3 c-KIT VEGFR2 c-Met Ret Cabozantinib malate (XL184) 1140909-48-3 Kit Flt-1/3/4 Tie2 AXL Brivanib Alaninate (BMS-582664) 649735-63-7 Golvatinib (E7050) 928037-13-2 VEGFR2 c-Met VEGFR-2 0.9 nM 1 nM 15 nM 2 nM 8 nM 10 nM 12 nM 14 nM 18 nM 60 nM 10 nM 30 nM 47 nM 84 nM 74 nM 140 nM 170 nM 160 nM 125 nM 23 nM 1.7 nM 15 nM 6 nM 22 nM 90 nM 20 nM 57 nM 59 nM 68 nM 0.035 nM 1.3 nM 4 nM 4.6 nM 12 nM/11.3 nM/6 nM 14.3 nM 7 nM 25 nM 14 nM 16 nM 44 nM 12 nM 6 nM/4 nM c-Fms/CSF1R 146 nM

ZM 306416 ZM 323881 HCl ENMD-2076 L-(+)-Tartaric acid 690206-97-4 VEGFR1 EGFR VEGFR2 Aurora A FGFR1 FGFR2 FGFR3 FGFR4 VEGFR2 KDR VEGFR2(Flk-1) PDGFRβ Axl IRAK4 ROS1 MLK4 GSK3β RET KDR PI3Kα 0.33 μM <10 nM <2 nM 14 nM 2.8 nM 2.6 nM 6.4 nM 6 nM 7 nM 0.7 μM 193000-39-4 1291074-87-7 VEGFR(Flt3) 1.86 nM LY2874455 1254473-64-7 SU1498 DCC-2618 168835-82-3 1225278-16-9 557795-19-4 苏尼替尼 80 nM 2 nM 0.49 nM 3.9 nM 5.3 nM 9.8 nM 11 nM 11 nM 17 nM 35 nM 2-D08 144707-18-6 *BTK 名称 Ibrutinib (PCI-32765) AVL-292 Olmutinib *PDGFR KDR0.86 nM 名称 CAS Sorafenib Tosylate 475207-59-1 无细胞 细胞 无细胞 靶点 Raf-1 VEGFR2/Flk1 B-Raf PDGFRβ mPDGFRβ FLT3 IC50 6 nM 15 nM 22 nM 57 nM 57 nM 58 nM CAS 936563-96-1 1202757-89-8 1353550-13-6 BTK BTK 靶点 IC50 0.5 nM 0.5 nM B-Raf (V599E) 38 nM

c-Kit VEGFR2 FGFR1 PDGFR Imatinib Mesylate (STI571) 220127-57-1 无细胞 c-Kit v-Abl 无细胞 Sunitinib Malate 341031-54-7 PDGFRβ VEGFR2 FLT3 Kit Abl PDGFRα Ponatinib (AP24534) 943319-70-8 无细胞 VEGFR2 FGFR1 c-Src c-Kit VEGFR1/FLT1 VEGFR2/Flk1 VEGFR2/KDR Axitinib 319460-85-0 VEGFR3 PDGFRβ Kit PDGFRα Imatinib (STI571) 152459-95-5 PDGFR c-Kit v-Abl 无细胞 VEGFR3/FLT4 RON Foretinib (GSK1363089) 849217-64-7 FLT3 PDGFRα Kit VEGFR1/FLT1 PDGFRβ *Src 名称 CAS 细胞 无细胞 Abl Src Met 90 nM 580 nM 100 nM 100 nM 600 nM 2 nM 80 nM 0.37 nM 1.1 nM 1.5 nM 2.2 nM 5.4 nM 12.5 nM 0.1 nM 0.18 nM 0.2 nM 0.1 nM-0.3 nM 1.6 nM 1.7 nM 5.0 nM 100 nM 100 nM 600 nM 0.4 nM Tie-2 1.1 nM 2.8 nM 3 nM 3.6 nM 3.6 nM 6.7 nM 6.8 nM 9.6 nM 68 nM 靶点 IC50 0.6 nM 0.8 nM 37 nM 79 nM 0.37 nM Dasatinib 302962-49-8 c-Kit (D816V) c-Kit (wt) 无细胞 Abl Ponatinib (AP24534) 943319-70-8

PDGFRα VEGFR2 FGFR1 c-Src c-Kit 1.1 nM 1.5 nM 2.2 nM 5.4 nM 12.5 nM 1 nM 1.2 nM 38.5 nM 282 nM 800 nM 1.255 μM 3.353 μM 9 nM 13 nM 26 nM 60 nM 25 nM(ED50) 0.395 μM 1.266 μM 1.667 μM 1.86 nM 10.4 nM 14 nM 15.9 nM 20.2 nM 24.2 nM 24.8 nM 43.7 nM 54.9 nM 56.4 nM 58.2 nM 69.4 nM 70.8 nM 78.4 nM 81.3 nM 92.7 nM 112 nM 120 nM 120 nM 350 nM 1 nM 81 nM Bosutinib (SKI-606) 380843-75-4 无细胞 Pelitinib 257933-82-7 S6 kinase ERK STAT3 Abl Src EGFR Src MEK/ERK ErbB2 Raf KX2-391 897016-82-9 Src (HuH7) Src (PLC/PRF/5) Src (Hep 3B) Src (Hep G2) NVP-BHG712 940310-85-0 EphB4 C-Raf c-Src c-Abl FLT3 RET Aurora A VEGFR3/FLT4 Src NTRK1/TRKA CSF-1R/c-Fms LCK FAK PDGFRα VEGFR2/KDR BLK FGFR2 YES1 Abl1 (T315I) FGFR1 Fyn JAK2 Kit Aurora B ENMD-2076 934353-76-1 PRT062607 (P505-15, BIIB057) HCl 1370261-97-4 无细胞 Syk FGR

MLK1 PYK2 YES FLT3 PAK5 Lyn cSRC LCK FAK PP2 172889-27-9 无细胞 LCK Fyn PDGFR Hck VEGFR mTOR PP121 1092788-83-4 Src Abl p110α DNA-PK p110δ EphB4 Sirtuin Src 槲皮素 117-39-5 PKC PI3Kγ PI3Kδ PI3Kβ Sirtuin Src 槲皮素 117-39-5 PKC PI3Kγ PI3Kδ PI3Kβ *Syk 名称 R788 (Fostamatinib) Disodium R406 (free base) CAS 1025687-58-4 841290-80-0 细胞 无细胞 无细胞 无细胞 Syk Syk FLT3 Syk FGR MLK1 PYK2 靶点 88 nM 108 nM 123 nM 139 nM 166 nM 192 nM 244 nM 249 nM 415 nM 4 nM 5 nM 2 nM 8 nM 12 nM 13 nM 14 nM 18 nM 52 nM 60 nM 150 nM 190 nM 2.4 μM 3.0 μM 5.4 μM 2.4 μM 3.0 μM 5.4 μM IC50 41 nM 41 nM 1 nM 81 nM 88 nM 108 nM PRT062607 (P505-15, BIIB057) HCl 1370261-97-4

YES FLT3 PAK5 Lyn cSRC LCK FAK Fostamatinib (R788) 901119-35-5 Syk Adenosine transporter Monoamine transporter *VDA 名称 DMXAA (Vadimezan) Plinabulin (NPI-2358) CAS 117570-53-3 714272-27-2 细胞 无细胞 靶点 DT-diaphorase IC50 62.5 μM 9.8~18 nM 123 nM 139 nM 166 nM 192 nM 244 nM 249 nM 415 nM 41 nM 1.84 μM 2.74 μM Adenosine A3 receptor 81 nM Ki 20 μM 肿瘤细胞 Tubulin VDA Verteporfin *JAK

名称 129497-78-5 YAP/TEAD interaction CAS 941678-49-5 细胞 无细胞 靶点 JAK1 JAK2 JAK1 JAK2 JAK3 IC50 3.3 nM 2.8 nM 112 nM 20 nM 1 nM 0.26 nM 3 nM 78 μM 11 nM 18 nM 1 nM Ki EC50 Ruxolitinib (INCB018424) Tofacitinib (CP-690550) Citrate AZD1480 Fedratinib (SAR302503, TG101348) JANEX-1 WHI-P97 CYT387 Tofacitinib WP1066 540737-29-9 935666-88-9 936091-26-8 202475-60-3 211555-05-4 1056634-68-4 477600-75-2 857064-38-1 无细胞 无细胞 无细胞 HEL细胞 JAK2 JAK2 JAK3 JAK-3 JAK1 JAK2 JAK3 JAK2 STAT3 JAK2 Flt3 RET JAK2 JAK2 0.09 μM 2.30 μM 2.43 μM 6 nM 25 nM 17 nM 3 nM 0.5 nM TG101209 LY2784544 NVP-BSK805 2HCl 936091-14-4 1229236-86-5 1092499-93-8 无细胞

Baricitinib AZ 960 CEP-33779 WHI-P154 XL019 S-Ruxolitinib (INCB018424) ZM 39923 HCl Ruxolitinib phosphate salt 莪术醇 *EGFR 名称 Lapatinib 二甲苯磺酸拉帕替尼 一水合物 Erlotinib HCl (OSI-744) 1187594-09-7 905586-69-8 1257704-57-6 211555-04-3 无细胞 JAK1 JAK2 JAK2 JAK2 JAK3 JAK2 JAK1 JAK2 JAK1 JAK3 JAK 5.9 nM 5.7 nM ＜3 nM 1.8 nM 1.8 μM 2.2 nM 3.3 nM 2.8 nM ＜0.45 nM 4.4 7.1 945755-56-6 941685-37-6 1021868-92-7 1092939-17-7 4871-97-0 CAS 231277-92-2 388082-78-8 183319-69-9 细胞 EGFR EGFR 靶点 ErbB2 IC50 9.2 nM 10.8 nM 10.8 nM 9.2 nM 2 nM 37 nM 37nM 26 nM 57 nM 9.2 nM 10.8 nM 40 nM 110 nM 500 nM 59 nM 92 nM 1.5 nM 9.0 nM 0.1 μM 10 nM 6 nM 2 nM 8 nM 4 nM 3 nM 4 nM 4.4 nM 2.4 nM Ki ErbB2 无细胞 NR6wtEGFR EGFR Tyr1173 Tyr992 Tyr1173 Tyr992 ErbB2 EGFR VEGFR2 VEGFR3 EGFR ER2 EGFR EGFR ErbB2 无细胞 BaF3细胞系 EGFR HER2/ErbB2 EGFR EGFR(L858R) EGFR(T790M) EGFR ErbB2 ErbB3 HDAC EGFR Gefitinib (ZD1839) 184475-35-2 NR6W 二对甲苯磺酸拉帕替尼(GW-572016) 388082-77-7 无细胞 Vandetanib (ZD6474) 443913-73-3 无细胞 Neratinib (HKI-272) Canertinib (CI-1033) AG-490 (Tyrphostin B42) CP-724714 Dacomitinib (PF299804, PF299) WZ4002 698387-09-6 267243-28-7 133550-30-8 537705-08-1 1110813-31-4 1213269-23-8 无细胞 AZD8931 (Sapitinib) 848942-61-0 无细胞 CUDC-101 1012054-59-9

HER2 AG-1478 (Tyrphostin AG-1478) PD153035 HCl 153436-53-4 183322-45-4 无细胞 无细胞 Pelitinib 257933-82-7 EGFR EGFR EGFR Src MEK/ERK ErbB2 AC480 (BMS-599626) AEE788 (NVP-AEE788) AP26113 OSI-420 WZ3146 ARRY-380 WZ8040 AST-1306 TsOH 714971-09-2 497839-62-0 1197958-12-5 183320-51-6 1214265-56-1 937265-83-3 1214265-57-2 1050500-29-2 HER1 HER2 EGFR HER2/ErbB2 ALK EGFR EGFR EGFR(L858R) HER2 EGFR EGFR ErbB2 EGFRL858R/T790M CO-1686 (AVL-301) 1374640-70-6 无细胞 EGFRWT 金雀异黄酮 金雀异黄酮 Varlitinib Icotinib TAK-285 WHI-P154 Daphnetin PD168393 Tyrphostin 9 Tyrphostin 23 酪氨酸激酶抑制剂 AG 494 Olmutinib PD153035 446-72-0 446-72-0 845272-21-1 610798-31-7 871026-44-7 211555-04-3 486-35-1 194423-15-9 10537-47-0 118409-57-7 133550-35-3 1353550-13-6 153436-54-5 NIH-3T3细胞 NIH-3T3细胞 EGF 胰岛素 EGF 胰岛素 ErbB1(EGFR) ErbB2(HER2) EGFR HER2 EGFR(HER1) JAK3 EGFR PKA PKC EGFR EGFR PDGFR EGFR EGFR EGF EGFR 15.7 nM 3 nM 29 pM 3.5 nM 282 nM 800 nM 1255 nM 20 nM 30 nM 2 nM 6 nM 2 nM 2 nM 8 nM 0.5 nM 3 nM 5.2 pM 21.5 nM EGFR(E746_A750) 2 nM 12μM 19 μM 12μM 19 μM 7 nM 2 nM 5 nM 17 nM 23 nM 1.8 μM 7.67 μM 9.33 μM 0.70 nM 460 μM 0.5μM 35 μM 1.2 μM 6 μM 303.3 nM 5.2 pM 25.01 μM

EBE-A22 (-)-表没食子儿茶素没食子酸 (-)-表没食子儿茶素没食子酸 Erlotinib 大黄酚 大黄酚 Norcantharidin Butein *HER2 名称 二对甲苯磺酸拉帕替尼(GW-572016) Neratinib (HKI-272) Canertinib (CI-1033) Lapatinib CP-724714 Dacomitinib (PF299804, PF299) AZD8931 (Sapitinib) 229476-53-3 989-51-5 989-51-5 183321-74-6 481-74-3 481-74-3 29745-04-8 487-52-5 EGF/HER-2 EGF/HER-2 EGFR EGFR mTOR EGFR mTOR c-Met EGFR EGFR 2 nM CAS 388082-77-7 698387-09-6 267243-28-7 231277-92-2 537705-08-1 1110813-31-4 848942-61-0 细胞 无细胞 无细胞 无细胞 靶点 ErbB2 EGFR HER2 EGFR EGFR ErbB2 ErbB2 EGFR HER2/ErbB2 EGFR EGFR ErbB2 ErbB3 HDAC EGFR HER2 IC50 9.2 nM 10.8 nM 59 nM 92 nM 1.5 nM 9.0 nM 9.2 nM 10.8 nM 10 nM 6 nM 4 nM 3 nM 4 nM 4.4 nM 2.4 nM 15.7 nM 6 nM 20 nM 30 nM 2 nM 6 nM 17 nM 23 nM 1 μM 10.8 nM 9.2 nM CUDC-101 Mubritinib (TAK 165) AC480 (BMS-599626) AEE788 (NVP-AEE788) TAK-285 Tyrphostin AG 879 去甲二氢愈创木酸 二甲苯磺酸拉帕替尼 一水合物 (-)-表没食子儿茶素没食子酸 (-)-表没食子儿茶素没食子酸 1012054-59-9 366017-09-6 714971-09-2 497839-62-0 871026-44-7 148741-30-4 500-38-9 388082-78-8 989-51-5 989-51-5 T-474细胞 HER2/ErbB2 HER1 HER2 EGFR HER2/ErbB2 HER2 EGFR(HER1) HER2/ErbB2 IGF-1R/HER2 EGFR ErbB2 EGF/HER-2 EGF/HER-2

*HIF 名称 2-Methoxyestradiol (2-MeOE2) 芍药苷 芍药苷 FG-4592 IOX2 Vadadustat N-acetylcysteine amide DMOG *Bcr-Abl 名称 Dasatinib CAS 302962-49-8 细胞 Abl 无细胞 220127-57-1 Src c-Kit Imatinib Mesylate (STI571) v-Abl c-Kit PDGFR Abl PDGFRα Ponatinib (AP24534) 943319-70-8 无细胞 VEGFR2 FGFR1 Src Nilotinib (AMN-107) Danusertib (PHA-739358) 641571-10-0 827318-97-8 小鼠骨髓祖细胞 BCR-ABL Aurora A/B/C 无细胞 Aurora A/B/C Aurora A/B/C Bafetinib (INNO-406) KW-2449 859212-16-1 无细胞 Bcr-Abl Lyn Flt3 EphB4 c-Raf c-Src c-Abl PDGFR Hck mTOR PP121 1092788-83-4 VEGFR2 Src Abl DNA-PK DCC-2036 (Rebastinib) 1020172-07-9 Abl1(WT) 靶点 <1 nM 0.8 nM 79 nM 0.6 μM 0.1 μM 0.1 μM 0.37 nM 1.1 nM 1.5 nM 2.2 nM 5.4 nM ＜30 nM 13 nM/79 nM/61 nM 13 nM/79 nM/61 nM 13 nM/79 nM/61 nM 5.8 nM 19 nM 6.6 nM 0.395 μM 1.266 μM 1.667 μM 2 nM 8 nM 10 nM 12 nM 14 nM 18 nM 60 nM 0.8 nM 25 nM IC50 ED50 CAS 362-07-2 23180-57-6 23180-57-6 808118-40-3 931398-72-0 1000025-07-9 38520-57-9 89464-63-1 细胞 无细胞 HIF-α脯氨酰羟化酶 PHD2 HIF prolyl hydroxylase 21 nM 靶点 IC50 1000669-72-6 NVP-BHG712 940310-85-0

Abl1(T315I) GZD824 GNF-2 1421783-64-3 778270-11-4 GNF-7 839706-07-9 Bcr-Abl(WT) Bcr-Abl(T315I) Bcr-Abl M351T T315I E255 V G250E c-Abl *FAK 名称 PF-00562271 PF-562271 PRT062607 (P505-15, BIIB057) HCl PF-573228 TAE226 (NVP-TAE226) PF-03814735 PND-1186 PF-431396 *ALK 名称 Crizotinib TAE684 (NVP-TAE684) CH5424802 LDK378 AP26113 AZD3463 ASP3026 PF-06463922 acetate *FGFR 名称 Sorafenib Tosylate CAS 475207-59-1 细胞 无细胞 CAS 877399-52-5 761439-42-3 1256580-46-7 1032900-25-6 1197958-12-5 1356962-20-3 1097917-15-1 1454846-35-5 细胞 无细胞 无细胞 无细胞 无细胞 ALK ALK ALK ALK ALK EGFR ALK ALK ROS1 ALK (WT) ALK (L1196M) 靶点 c-Met CAS 939791-38-5 717907-75-0 1370261-97-4 869288-64-2 761437-28-9 942487-16-3 1061353-68-1 717906-29-1 无细胞 无细胞 细胞 4 nM 0.34 nM 0.68 nM <5 nM 61 nM 122 nM 136 nM 133 nM 靶点 FAK FAK Syk FAK FAK Aurora A Aurora B FAK PYK2 FAK IC50 1.5 nM 1.5 nM 1 nM 4 nM 5.5 nM 0.8 nM 0.5 nM 1.5 nM 11nM 2 nM IC50 11 nM 24 nM 3 nM 1.9 nM 0.2 nM 3.5 nM Ki 0.75 nM <0.02 nM <0.07 nM 0.7 nM 靶点 Raf-1 6 nM IC50

B-Raf VEGFR-2 VEGFR-3 PDGFR-β Flt-3 c-KIT Abl PDGFRα Ponatinib (AP24534) 943319-70-8 无细胞 VEGFR2 FGFR1 Src FGFR1 BGJ398 (NVP-BGJ398) 872511-34-7 无细胞 FGFR2 FGFR3 VEGFR1 VEGFR2 VEGFR3 Nintedanib (BIBF 1120) 656247-17-5 无细胞 FGFR1 FGFR2 FGFR3 PDGFRα PDGFRβ VEGFR1 VEGFR2 VEGFR3 Pazopanib HCl (GW786034 HCl) 635702-64-6 无细胞 PDGFR FGFR c-Kit c-fms PD173074 Dovitinib (TKI-258, CHIR-258) 219580-11-7 405169-16-6 FGFR1 VEGFR2 无细胞 FLT3 c-Kit FGFR1 AZD4547 1035270-39-3 无细胞 FGFR2 FGFR3 Aurora A Danusertib (PHA-739358) 827318-97-8 无细胞 Aurora B Aurora C Lenvatinib (E7080) Brivanib (BMS-540215) ENMD-2076 Pazopanib 417716-92-8 649735-46-6 934353-76-1 444731-52-6 无细胞 VEGFR2/KDR VEGFR3/FLT4 VEGFR2 Aurora A Flt3 GFR1 22 nM 90 nM 20 nM 57 nM 59 nM 68 nM 0.37 nM 1.1 nM 1.5 nM 2.2 nM 5.4 nM 0.9 nM 1.4 nM 1 nM 34 nM 13 nM 13 nM 69 nM 37 nM 108 nM 59 nM 65 nM 10 nM 30 nM 47 nM 84 nM 74 nM 140 nM 146 nM 25 nM 100-200 nM 1 nM 2 nM 0.2 nM 2.5 nM 1.8 nM 13 nM 79 nM 61 nM 4.0 nM 5.2 nM 25 nM 14 nM 1.86 nM 10 nM

VEGFR2 VEGFR3 PDGFR FGFR c-Kit c-Fms/CSF1R MK-2461 Brivanib Alaninate (BMS-582664) Tyrphostin AG 1296 917879-39-1 649735-63-7 146535-11-7 Swiss 3T3细胞 LY2874455 1254473-64-7 30 nM 47 nM 84 nM 74 nM 140 nM 146 nM c-0.4-2.5 nM Met(WT/mutants) VEGFR2 PDGFR FGFR c-Kit FGFR1 FGFR2 FGFR3 FGFR4 VEGFR2 25 nM 0.3-0.5 μM 12.3 μM 1.8 μM 2.8 nM 2.6 nM 6.4 nM 6 nM 7 nM 3.9 nM 5 nM 26 nM 26 nM 9.2 nM 11nM 52.4 nM 3 nM 阿魏酸 阿魏酸 1135-24-6 1135-24-6 CDK4 Ark5/NUAK1 PDGFRβ FGFR1 RET Fyn ON-123300 1357470-29-1 PD-166866 BLU-9931

192705-79-6 1538604-68-0 FGFR1 FGFR4