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    阿拉丁小分子抑制剂、激动剂、拮抗剂--血管生成信号通路(上)
发表时间:2021-01-29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

产品列表
*FLT
| 项目号 | 产品名称 | 规格 | CAS | 包装 | 细胞 | 靶点 | IC50 | Ki | 
|---|---|---|---|---|---|---|---|---|
| S129593 | Sorafenib Tosylate | ≥99% | 475207-59-1 | 50mg,100mg,250mg,1g,5g | 无细胞 | Raf-1 | 6 nM | |
| B-Raf | 22 nM | |||||||
| VEGFR-2 | 90 nM | |||||||
| VEGFR-3 | 20 nM | |||||||
| PDGFR-β | 57 nM | |||||||
| Flt-3 | 59 nM | |||||||
| c-KIT | 68 nM | |||||||
| T127762 | Tozasertib | ≥98% | 639089-54-6 | 25mg,100mg | FLT3 | 30 nM | ||
| S125267 | SP600125 | ≥98% | 129-56-6 | 25mg,100mg,500mg,1g,5g | 无细胞 | JNK1 | 40 nM | |
| JNK2 | 40 nM | |||||||
| JNK3 | 90 nM | |||||||
| F127011 | Foretinib (GSK1363089) | ≥98% | 849217-64-7 | 5mg,25mg,100mg | 无细胞 | Met | 0.4 nM | |
| KDR | 0.9 nM | |||||||
| Q127558 | Quizartinib (AC220) | ≥99% | 950769-58-1 | 5mg,10mg,50mg,500mg | MV4-11 | Flt3(ITD) | 1.1 nM/4.2 nM | |
| RS4;11 | Flt3(WT) | 1.1 nM/4.2 nM | ||||||
| D126778 | Dovitinib (TKI-258, CHIR-258) | ≥99% | 405169-16-6 | 10mg,50mg,250mg | 无细胞 | FLT3 | 1 nM | |
| c-Kit | 2 nM | |||||||
| T126330 | Fedratinib (SAR302503, TG101348) | ≥98% | 936091-26-8 | 5mg,25mg,100mg | 无细胞 | JAK2 | 3 nM | |
| L126993 | Linifanib (ABT-869) | ≥99% | 796967-16-3 | 5mg,10mg,50mg | KDR | 4 nM | ||
| CSF-1R | 3 nM | |||||||
| Flt-1/3 | 3 nM/4 nM | |||||||
| PDGFRβ | 66 nM | |||||||
| C127776 | Crenolanib (CP-868596) | ≥99% | 670220-88-9 | 5mg,10mg,50mg | PDGFRα | 2.1 nM | ||
| PDGFRβ | 3.2 nM | |||||||
| R129910 | R406 (free base) | ≥99% | 841290-80-0 | 5mg,10mg,25mg,50mg,100mg | Syk | 41 nM | ||
| M127412 | Amuvatinib (MP-470) | ≥98% | 850879-09-3 | 5mg,25mg,100mg | c-Kit | 10 nM | ||
| PDGFα | 40 nM | |||||||
| Flt3 | 81 nM | |||||||
| T125150 | Tandutinib (MLN518) | ≥98% | 387867-13-2 | 25mg,100mg,500mg | FLT3 | 0.22 μM | ||
| T127523 | TG101209 | 98% | 936091-14-4 | 5mg,25mg,100mg | 无细胞 | JAK2 | 6 nM | |
| Flt3 | 25 nM | |||||||
| RET | 17 nM | |||||||
| K127169 | KW-2449 | ≥98% | 1000669-72-6 | 5mg,25mg,100mg | Flt3 | 6.6 nM | ||
| E126318 | ENMD-2076 | ≥99% | 934353-76-1 | 5mg,10mg,50mg | Aurora A | 14 nM | ||
| Flt3 | 1.86 nM | |||||||
| L127618 | LDK378 | ≥99% | 1032900-25-6 | 5mg,25mg,100mg,250mg | 无细胞 | ALK | 0.2 nM | |
| IGF-1R | 8 nM | |||||||
| InsR | 7 nM | |||||||
| STK22D | 23 nM | |||||||
| FLT3 | 60 nM | |||||||
| P129908 | PRT062607 (P505-15, BIIB057) HCl | ≥98% | 1370261-97-4 | 5mg,25mg | 无细胞 | Syk | 1 nM | |
| S125098 | Sorafenib | ≥99% | 284461-73-0 | 250mg,1g | 无细胞 | Raf-1 | 6 nM | |
| B-Raf | 22 nM | |||||||
| VEGFR-2 | 90 nM | |||||||
| VEGFR-3 | 20 nM | |||||||
| PDGFR-β | 57 nM | |||||||
| Flt-3 | 59 nM | |||||||
| c-KIT | 68 nM | |||||||
| C129757 | Cabozantinib malate (XL184) | ≥99% | 1140909-48-3 | 10mg,25mg,50mg,100mg,250mg | VEGFR2 | 0.035 nM | ||
| 无细胞 | c-Met | 1.3 nM | ||||||
| Ret | 4 nM | |||||||
| Kit | 4.6 nM | |||||||
| Flt-1/3/4 | 12 nM/11.3 nM/6 nM | |||||||
| Tie2 | 14.3 nM | |||||||
| AXL | 7 nM | |||||||
| T129806 | TCS 359 | ≥99% | 301305-73-7 | 10mg,25mg,50mg | FLT3 | 43 nM | ||
| E129946 | ENMD-2076 L-(+)-Tartaric acid | ≥99% | 1291074-87-7 | 5mg,25mg | Aurora A | 14 nM | ||
| VEGFR(Flt3) | 1.86 nM | |||||||
| L127298 | LY2801653 | - | 1206799-15-6 | 5mg,10mg,50mg | MET | 2 nM | ||
| C168062 | Crotonoside | 95% (HPLC) | 1818-71-9 | 5mg,10mg,25mg | FLT3 | |||
| HDAC3/6 | ||||||||
| G172979 | Gilteritinib | 97% | 1254053-43-4 | 5mg,100mg | FLT3 | 0.29 nM | ||
| AXL | 0.73 nM | |||||||
| P171724 | Pexidartinib | 97% | 1029044-16-3 | 5mg,100mg | CSF-1R | 20 nM | ||
| Kit | 10 nM | |||||||
| FLT3 | 160 nM | 
*DNA alkylator
| 项目号 | 产品名称 | 规格 | CAS | 包装 | 细胞 | 靶点 | IC50 | EC50 | Ki | 
|---|---|---|---|---|---|---|---|---|---|
| S129593 | Sorafenib Tosylate | ≥99% | 475207-59-1 | 10mg,50mg,250mg,1g,5g | 无细胞 | Raf-1 | 6 nM | ||
| B-Raf | 22 nM | ||||||||
| VEGFR-2 | 90 nM | ||||||||
| VEGFR-3 | 20 nM | ||||||||
| PDGFR-β | 57 nM | ||||||||
| Flt-3 | 59 nM | ||||||||
| c-KIT | 68 nM | ||||||||
| E129728 | Sunitinib Malate | ≥99% | 341031-54-7 | 100mg,500mg,1g | 无细胞 | VEGFR2 (Flk-1) | 80 nM | ||
| PDGFRβ | 2 nM | ||||||||
| L125046 | Lenalidomide | ≥99% | 191732-72-6 | 50mg,250mg,1g,5g | PBMCs | TNF-α | 13 nM | ||
| C126195 | Cabozantinib (XL184, BMS-907351) | ≥98% | 849217-68-1 | 5mg,10mg,50mg,100mg,250mg | 无细胞 | VEGFR2 | 0.035 nM | ||
| c-Met | 1.3 nM | ||||||||
| Ret | 4 nM | ||||||||
| Kit | 4.6 nM | ||||||||
| Flt-1/3/4 | 12 nM/11.3 nM/6 nM | ||||||||
| Tie2 | 14.3 nM | ||||||||
| AXL | 7 nM | ||||||||
| P127550 | Ponatinib (AP24534) | ≥99% | 943319-70-8 | 10mg,50mg,250mg | 无细胞 | Abl | 0.37 nM | ||
| PDGFRα | 1.1 nM | ||||||||
| VEGFR2 | 1.5 nM | ||||||||
| FGFR1 | 2.2 nM | ||||||||
| Src | 5.4 nM | ||||||||
| K125585 | Ki20227 | ≥98% | 623142-96-1 | 10mg,50mg | KDR | 2 nM | |||
| VEGFR-2 | 12 nM | ||||||||
| c-Kit | 451 nM | ||||||||
| PDGFRβ | 217 nM | ||||||||
| A129732 | Axitinib | ≥99% | 319460-85-0 | 10mg,50mg,250mg,1g | 猪主动脉内皮细胞 | VEGFR1 | 0.1 nM | ||
| VEGFR2 | 0.2 nM | ||||||||
| VEGFR3 | 0.1-0.3 nM | ||||||||
| PDGFRβ | 1.6 nM | ||||||||
| c-Kit | 1.7 nM | ||||||||
| F127011 | Foretinib (GSK1363089) | ≥98% | 849217-64-7 | 5mg,25mg,100mg | 无细胞 | Met | 0.4 nM | ||
| KDR | 0.9 nM | ||||||||
| N129725 | Nintedanib (BIBF 1120) | ≥98% | 656247-17-5 | 5mg,10mg,25mg,50mg,100mg,500mg | 无细胞 | VEGFR1 | 34 nM | ||
| VEGFR2 | 13 nM | ||||||||
| VEGFR3 | 13 nM | ||||||||
| FGFR1 | 69 nM | ||||||||
| FGFR2 | 37 nM | ||||||||
| FGFR3 | 108 nM | ||||||||
| PDGFRα | 59 nM | ||||||||
| PDGFRβ | 65 nM | ||||||||
| V125180 | Vandetanib (ZD6474) | ≥99% | 443913-73-3 | 25mg,100mg,500mg | 无细胞 | VEGFR2 | 40 nM | ||
| VEGFR3 | 110 nM | ||||||||
| EGFR | 500 nM | ||||||||
| R127804 | Regorafenib (BAY 73-4506) | ≥99% | 755037-03-7 | 5mg,10mg,25mg,100mg | 无细胞 | VEGFR1 | 13 nM | ||
| VEGFR2 | 4.2 nM | ||||||||
| VEGFR3 | 46 nM | ||||||||
| PDGFR-β | 22 nM | ||||||||
| Kit | 7 nM | ||||||||
| RET | 1.5 nM | ||||||||
| Raf-1 | 2.5 nM | ||||||||
| P129722 | Pazopanib HCl (GW786034 HCl) | ≥98% | 635702-64-6 | 25mg,100mg,250mg,1g | 无细胞 | VEGFR1 | 10 nM | ||
| VEGFR2 | 30 nM | ||||||||
| VEGFR3 | 47 nM | ||||||||
| PDGFR | 84 nM | ||||||||
| FGFR | 74 nM | ||||||||
| c-Kit | 140 nM | ||||||||
| c-fms | 146 nM | ||||||||
| C125911 | Cediranib | ≥98% | 288383-20-0 | 10mg,50mg | VEGFR(KDR) | <1 nM | |||
| Flt1/4 | 5 nM/≤3 nM | ||||||||
| P125865 | PD173074 | ≥99% | 219580-11-7 | 5mg,10mg,50mg | FGFR1 | 25 nM | |||
| VEGFR2 | 100-200 nM | ||||||||
| D126778 | Dovitinib (TKI-258, CHIR-258) | ≥99% | 405169-16-6 | 10mg,50mg,250mg | 无细胞 | FLT3 | 1 nM | ||
| c-Kit | 2 nM | ||||||||
| L126993 | Linifanib (ABT-869) | ≥99% | 796967-16-3 | 5mg,10mg,50mg | KDR | 4 nM | |||
| CSF-1R | 3 nM | ||||||||
| Flt-1/3 | 3 nM/4 nM | ||||||||
| PDGFRβ | 66 nM | ||||||||
| V125857 | Vatalanib (PTK787) 2HCl | ≥99% | 212141-51-0 | 10mg,50mg | 无细胞 | VEGFR2/KDR | 37 nM | ||
| R127906 | RAF265 (CHIR-265) | ≥98% | 927880-90-8 | 1mg,5mg,10mg,50mg | VEGFR2 | 30 nM | |||
| B-Raf | 3-60 nM | ||||||||
| T126012 | Tivozanib (AV-951) | ≥98% | 475108-18-0 | 5mg,25mg,100mg | VEGFR1 | 0.21 nM | |||
| VEGFR2 | 0.16 nM | ||||||||
| VEGFR3 | 0.24 nM | ||||||||
| M129736 | Motesanib Diphosphate (AMG-706) | ≥98% | 857876-30-3 | 5mg,10mg,50mg | VEGFR1 | 2 nM | |||
| VEGFR2 | 3 nM | ||||||||
| VEGFR3 | 6 nM | ||||||||
| L125518 | Lenvatinib (E7080) | ≥99% | 417716-92-8 | 5mg,10mg,50mg,100mg | VEGFR2(KDR) | 4 nM | |||
| VEGFR3(Flt-4) | 5.2 nM | ||||||||
| B127317 | Brivanib (BMS-540215) | ≥98% | 649735-46-6 | 5mg,10mg,50mg | VEGFR2 | 25 nM | |||
| M127064 | MGCD-265 | ≥98% | 875337-44-3 | 1mg,5mg,10mg,50mg | c-Met | 1 nM | |||
| VEGFR1/2/3 | 3 nM/3 nM/4 nM | ||||||||
| A126830 | AEE788 (NVP-AEE788) | ≥97% | 497839-62-0 | 5mg,25mg,100mg | EGFR | 2 nM | |||
| HER2/ErbB2 | 6 nM | ||||||||
| E126318 | ENMD-2076 | ≥99% | 934353-76-1 | 5mg,10mg,50mg | Aurora A | 14 nM | |||
| Flt3 | 1.86 nM | ||||||||
| O126155 | OSI-930 | ≥99% | 728033-96-3 | 1mg,5mg,25mg,50mg | Kit | 80 nM | |||
| KDR | 9 nM | ||||||||
| CSF-1R | 15 nM | ||||||||
| C126929 | CYC116 | ≥99% | 693228-63-6 | 1mg,10mg,50mg | Aurora A | 8.0 nM | |||
| Aurora B | 9.2 nM | ||||||||
| VEGFR2 | 44 nM | ||||||||
| K125876 | Ki8751 | ≥98% | 228559-41-9 | 5mg,25mg,100mg | VEGFR2 | 0.9 nM | |||
| T129747 | Telatinib | ≥99% | 332012-40-5 | 1mg,5mg,10mg,50mg | VEGFR2/3 | 6 nM/4 nM | |||
| c-Kit | 1 nM | ||||||||
| PDGFRα | 15 nM | ||||||||
| P126419 | PP121 | ≥98% | 1092788-83-4 | 10mg,50mg | PDGFR | 2 nM | |||
| Hck | 8 nM | ||||||||
| mTOR | 10 nM | ||||||||
| VEGFR2 | 12 nM | ||||||||
| Src | 14 nM | ||||||||
| Abl | 18 nM | ||||||||
| DNA-PK | 60 nM | ||||||||
| P125184 | Pazopanib | ≥99% | 444731-52-6 | 25mg,100mg,500mg | GFR1 | 10 nM | |||
| VEGFR2 | 30 nM | ||||||||
| VEGFR3 | 47 nM | ||||||||
| PDGFR | 84 nM | ||||||||
| FGFR | 74 nM | ||||||||
| c-Kit | 140 nM | ||||||||
| c-Fms/CSF1R | 146 nM | ||||||||
| K125907 | KRN-633 | ≥97% | 286370-15-8 | 5mg,25mg,100mg | VEGFR1 | 170 nM | |||
| VEGFR2 | 160 nM | ||||||||
| VEGFR3 | 125 nM | ||||||||
| S126571 | SAR131675 | ≥99% | 1433953-83-3 | 1mg,10mg,50mg | VEGFR3 | 23 nM | 12 nM | ||
| B129768 | BMS-794833 | ≥99% | 1174046-72-0 | 1mg,5mg,10mg,50mg | Met | 1.7 nM | |||
| VEGFR2 | 15 nM | ||||||||
| S125098 | Sorafenib | ≥99% | 284461-73-0 | 250mg,1g | 无细胞 | Raf-1 | 6 nM | ||
| B-Raf | 22 nM | ||||||||
| VEGFR-2 | 90 nM | ||||||||
| VEGFR-3 | 20 nM | ||||||||
| PDGFR-β | 57 nM | ||||||||
| Flt-3 | 59 nM | ||||||||
| c-KIT | 68 nM | ||||||||
| C129757 | Cabozantinib malate (XL184) | ≥99% | 1140909-48-3 | 10mg,25mg,50mg,100mg,250mg | VEGFR2 | 0.035 nM | |||
| c-Met | 1.3 nM | ||||||||
| Ret | 4 nM | ||||||||
| Kit | 4.6 nM | ||||||||
| Flt-1/3/4 | 12 nM/11.3 nM/6 nM | ||||||||
| Tie2 | 14.3 nM | ||||||||
| AXL | 7 nM | ||||||||
| B129764 | Brivanib Alaninate (BMS-582664) | ≥95% | 649735-63-7 | 10mg,50mg | VEGFR2 | 25 nM | |||
| E126304 | Golvatinib (E7050) | ≥99% | 928037-13-2 | 1mg,5mg,10mg,50mg | c-Met | 14 nM | |||
| VEGFR-2 | 16 nM | ||||||||
| Z129748 | ZM 306416 | ≥98% | 690206-97-4 | 10mg,50mg | VEGFR1 | 0.33 μM | |||
| EGFR | <10 nM | ||||||||
| Z129761 | ZM 323881 HCl | ≥99% | 193000-39-4 | 1mg,10mg,50mg | VEGFR2 | <2 nM | |||
| E129946 | ENMD-2076 L-(+)-Tartaric acid | ≥99% | 1291074-87-7 | 5mg,25mg | Aurora A | 14 nM | |||
| VEGFR(Flt3) | 1.86 nM | ||||||||
| L126507 | LY2874455 | ≥99% | 1254473-64-7 | 5mg,10mg,50mg | FGFR1 | 2.8 nM | |||
| FGFR2 | 2.6 nM | ||||||||
| FGFR3 | 6.4 nM | ||||||||
| FGFR4 | 6 nM | ||||||||
| VEGFR2 | 7 nM | ||||||||
| S167823 | SU1498 | 98% (HPLC) | 168835-82-3 | 5mg,25mg | KDR | 0.7 μM | |||
| D126474 | DCC-2618 | - | 1225278-16-9 | 5mg,10mg,50mg | |||||
| S126061 | 苏尼替尼 | 0.99 | 557795-19-4 | 100mg,500mg,1g,5g,25g | VEGFR2(Flk-1) | 80 nM | |||
| PDGFRβ | 2 nM | ||||||||
| D167318 | 2-D08 | 98% (HPLC) | 144707-18-6 | 5mg,25mg | Axl | 0.49 nM | |||
| IRAK4 | 3.9 nM | ||||||||
| ROS1 | 5.3 nM | ||||||||
| MLK4 | 9.8 nM | ||||||||
| GSK3β | 11 nM | ||||||||
| RET | 11 nM | ||||||||
| KDR | 17 nM | ||||||||
| PI3Kα | 35 nM | ||||||||
*BTK
| 产品号 | 产品名称 | 规格 | CAS | 包装 | 靶点 | IC50 | 
|---|---|---|---|---|---|---|
| P127143 | Ibrutinib (PCI-32765) | ≥98% | 936563-96-1 | 5mg,10mg,50mg,250mg | BTK | 0.5 nM | 
| A127694 | AVL-292 | 98% | 1202757-89-8 | 5mg,10mg,50mg,100mg | BTK | 0.5 nM | 
| O173511 | Olmutinib | 97% | 1353550-13-6 | 5mg,100mg | 
*PDGFR
KDR0.86 nM
| 产品号 | 产品名称 | 规格 | CAS | 包装 | 细胞 | 靶点 | IC50 | |
|---|---|---|---|---|---|---|---|---|
| S129593 | Sorafenib Tosylate | ≥99% | 475207-59-1 | 50mg,100mg,250mg,1g,5g | 无细胞 | Raf-1 | 6 nM | |
| VEGFR2/Flk1 | 15 nM | |||||||
| 无细胞 | B-Raf | 22 nM | ||||||
| B-Raf (V599E) | 38 nM | |||||||
| PDGFRβ | 57 nM | |||||||
| mPDGFRβ | 57 nM | |||||||
| FLT3 | 58 nM | |||||||
| c-Kit | 68 nM | |||||||
| VEGFR2 | 90 nM | |||||||
| FGFR1 | 580 nM | |||||||
| I129225 | Imatinib Mesylate (STI571) | ≥99% | 220127-57-1 | 100mg,250mg,1g,5g,25g | 无细胞 | PDGFR | 100 nM | |
| c-Kit | 100 nM | |||||||
| v-Abl | 600 nM | |||||||
| E129728 | Sunitinib Malate | ≥99% | 341031-54-7 | 100mg,500mg,1g | 无细胞 | PDGFRβ | 2 nM | |
| VEGFR2 | 80 nM | |||||||
| FLT3 | ||||||||
| Kit | ||||||||
| P127550 | Ponatinib (AP24534) | ≥99% | 943319-70-8 | 10mg,250mg,50mg | 无细胞 | Abl | 0.37 nM | |
| PDGFRα | 1.1 nM | |||||||
| VEGFR2 | 1.5 nM | |||||||
| FGFR1 | 2.2 nM | |||||||
| c-Src | 5.4 nM | |||||||
| c-Kit | 12.5 nM | |||||||
| A129732 | Axitinib | ≥99% | 319460-85-0 | 10mg,250mg,50mg,1g | VEGFR1/FLT1 | 0.1 nM | ||
| VEGFR2/Flk1 | 0.18 nM | |||||||
| VEGFR2/KDR | 0.2 nM | |||||||
| VEGFR3 | 0.1 nM-0.3 nM | |||||||
| PDGFRβ | 1.6 nM | |||||||
| Kit | 1.7 nM | |||||||
| PDGFRα | 5.0 nM | |||||||
| I124963 | Imatinib (STI571) | ≥99% | 152459-95-5 | 1g,5g,25g,250mg | PDGFR | 100 nM | ||
| c-Kit | 100 nM | |||||||
| v-Abl | 600 nM | |||||||
| F127011 | Foretinib (GSK1363089) | ≥99% | 849217-64-7 | 5mg,100mg,25mg | 无细胞 | Met | 0.4 nM | |
| Tie-2 | 1.1 nM | |||||||
| VEGFR3/FLT4 | 2.8 nM | |||||||
| RON | 3 nM | |||||||
| FLT3 | 3.6 nM | |||||||
| PDGFRα | 3.6 nM | |||||||
| Kit | 6.7 nM | |||||||
| VEGFR1/FLT1 | 6.8 nM | |||||||
| PDGFRβ | 9.6 nM | |||||||
*Src
| 项目号 | 产品名称 | 规格 | CAS | 包装 | 细胞 | 靶点 | IC50 | 
|---|---|---|---|---|---|---|---|
| D125110 | Dasatinib | ≥99% | 302962-49-8 | 25mg,100mg,500mg,1g,5g | 无细胞 | Abl | 0.6 nM | 
| Src | 0.8 nM | ||||||
| c-Kit (D816V) | 37 nM | ||||||
| c-Kit (wt) | 79 nM | ||||||
| P127550 | Ponatinib (AP24534) | ≥99% | 943319-70-8 | 10mg,50mg,250mg | 无细胞 | Abl | 0.37 nM | 
| PDGFRα | 1.1 nM | ||||||
| VEGFR2 | 1.5 nM | ||||||
| FGFR1 | 2.2 nM | ||||||
| c-Src | 5.4 nM | ||||||
| c-Kit | 12.5 nM | ||||||
| B129905 | Bosutinib (SKI-606) | ≥99% | 380843-75-4 | 10mg,50mg,100mg | S6 kinase | ||
| ERK | |||||||
| STAT3 | |||||||
| 无细胞 | Abl | 1 nM | |||||
| Src | 1.2 nM | ||||||
| P125444 | Pelitinib | ≥98% | 257933-82-7 | 5mg,25mg,100mg | EGFR | 38.5 nM | |
| Src | 282 nM | ||||||
| MEK/ERK | 800 nM | ||||||
| ErbB2 | 1.255 μM | ||||||
| Raf | 3.353 μM | ||||||
| K126255 | KX2-391 | ≥99% | 897016-82-9 | 1mg,5mg,10mg,50mg | Src (HuH7) | 9 nM | |
| Src (PLC/PRF/5) | 13 nM | ||||||
| Src (Hep 3B) | 26 nM | ||||||
| Src (Hep G2) | 60 nM | ||||||
| N127928 | NVP-BHG712 | ≥98% | 940310-85-0 | 5mg,25mg,100mg | EphB4 | 25 nM(ED50) | |
| C-Raf | 0.395 μM | ||||||
| c-Src | 1.266 μM | ||||||
| c-Abl | 1.667 μM | ||||||
| E126318 | ENMD-2076 | ≥99% | 934353-76-1 | 5mg,10mg,50mg | FLT3 | 1.86 nM | |
| RET | 10.4 nM | ||||||
| Aurora A | 14 nM | ||||||
| VEGFR3/FLT4 | 15.9 nM | ||||||
| Src | 20.2 nM | ||||||
| NTRK1/TRKA | 24.2 nM | ||||||
| CSF-1R/c-Fms | 24.8 nM | ||||||
| LCK | 43.7 nM | ||||||
| FAK | 54.9 nM | ||||||
| PDGFRα | 56.4 nM | ||||||
| VEGFR2/KDR | 58.2 nM | ||||||
| BLK | 69.4 nM | ||||||
| FGFR2 | 70.8 nM | ||||||
| YES1 | 78.4 nM | ||||||
| Abl1 (T315I) | 81.3 nM | ||||||
| FGFR1 | 92.7 nM | ||||||
| Fyn | 112 nM | ||||||
| JAK2 | 120 nM | ||||||
| Kit | 120 nM | ||||||
| Aurora B | 350 nM | ||||||
| P129908 | PRT062607 (P505-15, BIIB057) HCl | ≥98% | 1370261-97-4 | 5mg,25mg, | 无细胞 | Syk | 1 nM | 
| FGR | 81 nM | ||||||
| MLK1 | 88 nM | ||||||
| PYK2 | 108 nM | ||||||
| YES | 123 nM | ||||||
| FLT3 | 139 nM | ||||||
| PAK5 | 166 nM | ||||||
| Lyn | 192 nM | ||||||
| cSRC | 244 nM | ||||||
| LCK | 249 nM | ||||||
| FAK | 415 nM | ||||||
| P125361 | PP2 | ≥98% | 172889-27-9 | 5mg,25mg,100mg | 无细胞 | LCK | 4 nM | 
| Fyn | 5 nM | ||||||
| P126419 | PP121 | ≥98% | 1092788-83-4 | 10mg,50mg | PDGFR | 2 nM | |
| Hck | 8 nM | ||||||
| VEGFR | 12 nM | ||||||
| mTOR | 13 nM | ||||||
| Src | 14 nM | ||||||
| Abl | 18 nM | ||||||
| p110α | 52 nM | ||||||
| DNA-PK | 60 nM | ||||||
| p110δ | 150 nM | ||||||
| EphB4 | 190 nM | ||||||
| Q111274 | 槲皮素 | 95.00% | 117-39-5 | 1g,10g,50g,250g | Sirtuin | ||
| Src | |||||||
| PKC | |||||||
| PI3Kγ | 2.4 μM | ||||||
| PI3Kδ | 3.0 μM | ||||||
| PI3Kβ | 5.4 μM | ||||||
| Q111273 | 槲皮素 | 分析标准品,≥98.5% | 117-39-5 | 20mg | Sirtuin | ||
| Src | |||||||
| PKC | |||||||
| PI3Kγ | 2.4 μM | ||||||
| PI3Kδ | 3.0 μM | ||||||
| PI3Kβ | 5.4 μM | 
*Syk
| 项目号 | 产品名称 | 规格 | CAS | 包装 | 细胞 | 靶点 | IC50 | 
|---|---|---|---|---|---|---|---|
| R129913 | R788 (Fostamatinib) Disodium | ≥98% | 1025687-58-4 | 50mg,1mg,5mg,10mg | 无细胞 | Syk | 41 nM | 
| R129910 | R406 (free base) | ≥99% | 841290-80-0 | 25mg,50mg,100mg,5mg,10mg | 无细胞 | Syk | 41 nM | 
| FLT3 | |||||||
| P129908 | PRT062607 (P505-15, BIIB057) HCl | ≥98% | 1370261-97-4 | 5mg,25mg | 无细胞 | Syk | 1 nM | 
| FGR | 81 nM | ||||||
| MLK1 | 88 nM | ||||||
| PYK2 | 108 nM | ||||||
| YES | 123 nM | ||||||
| FLT3 | 139 nM | ||||||
| PAK5 | 166 nM | ||||||
| Lyn | 192 nM | ||||||
| cSRC | 244 nM | ||||||
| LCK | 249 nM | ||||||
| FAK | 415 nM | ||||||
| F129915 | Fostamatinib (R788) | ≥98% | 901119-35-5 | 50mg,5mg,10mg | Syk | 41 nM | |
| Adenosine A3 receptor | 81 nM | ||||||
| Adenosine transporter | 1.84 μM | ||||||
| Monoamine transporter | 2.74 μM | 
*VDA
| 项目号 | 产品名称 | 规格 | CAS | 包装 | 细胞 | 靶点 | IC50 | Ki | 
|---|---|---|---|---|---|---|---|---|
| D129922 | DMXAA (Vadimezan) | ≥98% | 117570-53-3 | 5mg,25mg,100mg,250mg | 无细胞 | DT-diaphorase | 62.5 μM | 20 μM | 
| P126141 | Plinabulin (NPI-2358) | ≥97% | 714272-27-2 | 5mg,10mg,50mg,1g | 肿瘤细胞 | Tubulin  | 9.8~18 nM | |
| V129759 | Verteporfin | ≥97% | 129497-78-5 | 25mg,50mg,1mg,5mg,10mg |   VDA  | |||
| YAP/TEAD interaction | 
    


