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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IC50Ki
S129593Sorafenib Tosylate≥99%475207-59-150mg,100mg,250mg,1g,5g无细胞Raf-16 nM
B-Raf22 nM

VEGFR-290 nM
VEGFR-320 nM
PDGFR-β57 nM
Flt-359 nM
c-KIT68 nM
T127762Tozasertib≥98%639089-54-625mg,100mg
FLT330 nM
S125267SP600125≥98%129-56-625mg,100mg,500mg,1g,5g无细胞JNK140 nM
JNK240 nM
JNK390 nM
F127011Foretinib (GSK1363089)≥98%849217-64-75mg,25mg,100mg无细胞Met0.4 nM
KDR0.9 nM
Q127558Quizartinib (AC220)≥99%950769-58-15mg,10mg,50mg,500mgMV4-11Flt3(ITD)1.1 nM/4.2 nM
 RS4;11Flt3(WT)1.1 nM/4.2 nM
D126778Dovitinib (TKI-258, CHIR-258)≥99%405169-16-610mg,50mg,250mg无细胞FLT31 nM
c-Kit2 nM
T126330Fedratinib (SAR302503, TG101348)≥98%936091-26-85mg,25mg,100mg无细胞JAK23 nM
L126993Linifanib (ABT-869)≥99%796967-16-35mg,10mg,50mg
KDR4 nM
CSF-1R3 nM
Flt-1/33 nM/4 nM
PDGFRβ66 nM
C127776Crenolanib (CP-868596)≥99%670220-88-95mg,10mg,50mg
PDGFRα2.1 nM
PDGFRβ3.2 nM
R129910R406 (free base)≥99%841290-80-05mg,10mg,25mg,50mg,100mg
Syk41 nM
M127412Amuvatinib (MP-470)≥98%850879-09-35mg,25mg,100mg
c-Kit10 nM
PDGFα40 nM
Flt381 nM
T125150Tandutinib (MLN518)≥98%387867-13-225mg,100mg,500mg
FLT30.22 μM
T127523TG10120998%936091-14-45mg,25mg,100mg无细胞JAK26 nM

Flt325 nM

RET17 nM
K127169KW-2449≥98%1000669-72-65mg,25mg,100mg
Flt36.6 nM
E126318ENMD-2076≥99%934353-76-15mg,10mg,50mg
Aurora A14 nM
Flt31.86 nM
L127618LDK378≥99%1032900-25-65mg,25mg,100mg,250mg无细胞ALK0.2 nM

IGF-1R8 nM

InsR7 nM

STK22D23 nM

FLT360 nM
P129908PRT062607 (P505-15, BIIB057) HCl≥98%1370261-97-45mg,25mg无细胞Syk1 nM
S125098Sorafenib≥99%284461-73-0250mg,1g无细胞Raf-16 nM
B-Raf22 nM

VEGFR-290 nM
VEGFR-320 nM
PDGFR-β57 nM
Flt-359 nM
c-KIT68 nM
C129757Cabozantinib malate (XL184)≥99%1140909-48-310mg,25mg,50mg,100mg,250mg
VEGFR20.035 nM
无细胞c-Met1.3 nM
Ret4 nM
Kit4.6 nM
Flt-1/3/412 nM/11.3 nM/6 nM
Tie214.3 nM
AXL7 nM
T129806TCS 359≥99%301305-73-710mg,25mg,50mg
FLT343 nM
E129946ENMD-2076 L-(+)-Tartaric acid≥99%1291074-87-75mg,25mg
Aurora A14 nM
VEGFR(Flt3)1.86 nM
L127298LY2801653-1206799-15-65mg,10mg,50mg
MET
2 nM
C168062Crotonoside95% (HPLC)1818-71-95mg,10mg,25mg
FLT3

HDAC3/6

G172979Gilteritinib97%1254053-43-45mg,100mg
FLT30.29 nM
AXL0.73 nM
P171724Pexidartinib97%1029044-16-35mg,100mg
CSF-1R20 nM
Kit10 nM
FLT3160 nM

 

*DNA alkylator

项目号产品名称规格CAS包装细胞靶点IC50EC50Ki
S129593Sorafenib Tosylate≥99%475207-59-110mg,50mg,250mg,1g,5g无细胞Raf-16 nM

B-Raf22 nM


VEGFR-290 nM

VEGFR-320 nM

PDGFR-β57 nM

Flt-359 nM

c-KIT68 nM

E129728Sunitinib Malate≥99%341031-54-7100mg,500mg,1g无细胞VEGFR2 (Flk-1)80 nM

PDGFRβ2 nM

L125046Lenalidomide≥99%191732-72-650mg,250mg,1g,5gPBMCsTNF-α13 nM

C126195Cabozantinib (XL184, BMS-907351)≥98%849217-68-15mg,10mg,50mg,100mg,250mg无细胞VEGFR20.035 nM


c-Met1.3 nM

 Ret4 nM

Kit4.6 nM

Flt-1/3/412 nM/11.3 nM/6 nM

Tie214.3 nM

AXL7 nM

P127550Ponatinib (AP24534)≥99%943319-70-810mg,50mg,250mg无细胞Abl0.37 nM

PDGFRα1.1 nM

VEGFR21.5 nM

FGFR12.2 nM

Src5.4 nM

K125585Ki20227≥98%623142-96-110mg,50mg
KDR2 nM

VEGFR-212 nM

c-Kit451 nM

PDGFRβ217 nM

A129732Axitinib≥99%319460-85-010mg,50mg,250mg,1g猪主动脉内皮细胞VEGFR10.1 nM

VEGFR20.2 nM

VEGFR30.1-0.3 nM

PDGFRβ1.6 nM

c-Kit1.7 nM

F127011Foretinib (GSK1363089)≥98%849217-64-75mg,25mg,100mg无细胞Met0.4 nM

KDR0.9 nM

N129725Nintedanib (BIBF 1120)≥98%656247-17-55mg,10mg,25mg,50mg,100mg,500mg无细胞VEGFR134 nM

VEGFR213 nM

VEGFR313 nM

FGFR169 nM

FGFR237 nM

FGFR3108 nM

PDGFRα59 nM

PDGFRβ65 nM

V125180Vandetanib (ZD6474)≥99%443913-73-325mg,100mg,500mg无细胞VEGFR240 nM

VEGFR3110 nM

EGFR500 nM

R127804Regorafenib (BAY 73-4506)≥99%755037-03-75mg,10mg,25mg,100mg无细胞VEGFR113 nM

VEGFR24.2 nM

VEGFR346 nM

PDGFR-β22 nM

Kit7 nM

RET1.5 nM

Raf-12.5 nM

P129722Pazopanib HCl (GW786034 HCl)≥98%635702-64-625mg,100mg,250mg,1g无细胞VEGFR110 nM

VEGFR230 nM

VEGFR347 nM

PDGFR84 nM

FGFR74 nM

c-Kit140 nM

c-fms146 nM

C125911Cediranib≥98%288383-20-010mg,50mg
VEGFR(KDR)<1 nM

Flt1/45 nM/≤3 nM

P125865PD173074≥99%219580-11-75mg,10mg,50mg
FGFR125 nM

VEGFR2100-200 nM

D126778Dovitinib (TKI-258, CHIR-258)≥99%405169-16-610mg,50mg,250mg无细胞FLT31 nM

c-Kit2 nM

L126993Linifanib (ABT-869)≥99%796967-16-35mg,10mg,50mg
KDR4 nM

CSF-1R3 nM

Flt-1/33 nM/4 nM

PDGFRβ66 nM

V125857Vatalanib (PTK787) 2HCl≥99%212141-51-010mg,50mg无细胞VEGFR2/KDR37 nM

R127906RAF265 (CHIR-265)≥98%927880-90-81mg,5mg,10mg,50mg
VEGFR2
30 nM
B-Raf3-60 nM

T126012Tivozanib (AV-951)≥98%475108-18-05mg,25mg,100mg
VEGFR10.21 nM

VEGFR20.16 nM

VEGFR30.24 nM

M129736Motesanib Diphosphate (AMG-706)≥98%857876-30-35mg,10mg,50mg
VEGFR12 nM

VEGFR23 nM

VEGFR36 nM

L125518Lenvatinib (E7080)≥99%417716-92-85mg,10mg,50mg,100mg
VEGFR2(KDR)4 nM

VEGFR3(Flt-4)5.2 nM

B127317Brivanib (BMS-540215)≥98%649735-46-65mg,10mg,50mg
VEGFR225 nM

M127064MGCD-265≥98%875337-44-31mg,5mg,10mg,50mg
c-Met1 nM

VEGFR1/2/33 nM/3 nM/4 nM
A126830AEE788 (NVP-AEE788)≥97%497839-62-05mg,25mg,100mg
EGFR2 nM

HER2/ErbB26 nM

E126318ENMD-2076≥99%934353-76-15mg,10mg,50mg
Aurora A14 nM

Flt31.86 nM

O126155OSI-930≥99%728033-96-31mg,5mg,25mg,50mg
Kit80 nM

KDR9 nM

CSF-1R15 nM

C126929CYC116≥99%693228-63-61mg,10mg,50mg
Aurora A

8.0 nM
Aurora B

9.2 nM
VEGFR2

44 nM
K125876Ki8751≥98%228559-41-95mg,25mg,100mg
VEGFR20.9 nM

T129747Telatinib≥99%332012-40-51mg,5mg,10mg,50mg
VEGFR2/36 nM/4 nM

c-Kit1 nM

PDGFRα15 nM

P126419PP121≥98%1092788-83-410mg,50mg
PDGFR2 nM

Hck8 nM

mTOR10 nM

VEGFR212 nM

Src14 nM

Abl18 nM

DNA-PK60 nM

P125184Pazopanib≥99%444731-52-625mg,100mg,500mg
GFR110 nM

VEGFR230 nM

VEGFR347 nM

PDGFR84 nM

FGFR74 nM

c-Kit140 nM

c-Fms/CSF1R146 nM

K125907KRN-633≥97%286370-15-85mg,25mg,100mg
VEGFR1170 nM

VEGFR2160 nM

VEGFR3125 nM

S126571SAR131675≥99%1433953-83-31mg,10mg,50mg
VEGFR323 nM
12 nM
B129768BMS-794833≥99%1174046-72-01mg,5mg,10mg,50mg
Met1.7 nM

VEGFR215 nM

S125098Sorafenib≥99%284461-73-0250mg,1g无细胞Raf-16 nM

B-Raf22 nM


VEGFR-290 nM

VEGFR-320 nM

PDGFR-β57 nM

Flt-359 nM

c-KIT68 nM

C129757Cabozantinib malate (XL184)≥99%1140909-48-310mg,25mg,50mg,100mg,250mg
VEGFR20.035 nM

c-Met1.3 nM

Ret4 nM

Kit4.6 nM

Flt-1/3/412 nM/11.3 nM/6 nM

Tie214.3 nM

AXL7 nM

B129764Brivanib Alaninate (BMS-582664)≥95%649735-63-710mg,50mg
VEGFR225 nM

E126304Golvatinib (E7050)≥99%928037-13-21mg,5mg,10mg,50mg
c-Met14 nM

VEGFR-216 nM

Z129748ZM 306416≥98%690206-97-410mg,50mg
VEGFR10.33 μM

EGFR<10 nM

Z129761ZM 323881 HCl≥99%193000-39-41mg,10mg,50mg
VEGFR2<2 nM

E129946ENMD-2076 L-(+)-Tartaric acid≥99%1291074-87-75mg,25mg
Aurora A14 nM

VEGFR(Flt3)1.86 nM

L126507LY2874455≥99%1254473-64-75mg,10mg,50mg
FGFR12.8 nM

FGFR22.6 nM

FGFR36.4 nM

FGFR46 nM

VEGFR27 nM

S167823SU149898% (HPLC)168835-82-35mg,25mg
KDR0.7 μM

D126474DCC-2618-1225278-16-95mg,10mg,50mg




S126061苏尼替尼0.99557795-19-4100mg,500mg,1g,5g,25g
VEGFR2(Flk-1)80 nM

PDGFRβ2 nM

D1673182-D0898% (HPLC)144707-18-65mg,25mg
Axl0.49 nM

IRAK43.9 nM

ROS15.3 nM

MLK49.8 nM

GSK3β11 nM

RET11 nM

KDR17 nM

PI3Kα35 nM

 

*BTK

产品号产品名称规格CAS包装靶点IC50
P127143Ibrutinib (PCI-32765)≥98%936563-96-15mg,10mg,50mg,250mgBTK0.5 nM
A127694AVL-29298%1202757-89-85mg,10mg,50mg,100mgBTK0.5 nM
O173511Olmutinib97%1353550-13-65mg,100mg

 

*PDGFR

KDR0.86 nM

产品号产品名称规格CAS包装细胞靶点IC50
S129593Sorafenib Tosylate≥99%475207-59-150mg,100mg,250mg,1g,5g无细胞Raf-16 nM

VEGFR2/Flk115 nM
无细胞B-Raf22 nM

B-Raf (V599E)38 nM
PDGFRβ57 nM
mPDGFRβ57 nM
FLT358 nM
c-Kit68 nM
VEGFR290 nM
FGFR1580 nM
I129225Imatinib Mesylate (STI571)≥99%220127-57-1100mg,250mg,1g,5g,25g无细胞PDGFR100 nM
c-Kit100 nM
v-Abl600 nM
E129728Sunitinib Malate≥99%341031-54-7100mg,500mg,1g无细胞PDGFRβ 2 nM
VEGFR280 nM

FLT3

Kit 

P127550Ponatinib (AP24534)≥99%943319-70-810mg,250mg,50mg无细胞Abl0.37 nM
PDGFRα1.1 nM
VEGFR21.5 nM
FGFR12.2 nM
c-Src5.4 nM
c-Kit12.5 nM
A129732Axitinib≥99%319460-85-010mg,250mg,50mg,1g
VEGFR1/FLT10.1 nM
VEGFR2/Flk10.18 nM
VEGFR2/KDR0.2 nM
VEGFR30.1 nM-0.3 nM
PDGFRβ1.6 nM
Kit1.7 nM
PDGFRα5.0 nM 
I124963Imatinib (STI571)≥99%152459-95-51g,5g,25g,250mg
PDGFR100 nM
c-Kit100 nM
v-Abl600 nM
F127011Foretinib (GSK1363089)≥99%849217-64-75mg,100mg,25mg无细胞Met0.4 nM

Tie-21.1 nM
VEGFR3/FLT42.8 nM
RON3 nM
FLT33.6 nM
PDGFRα3.6 nM
Kit6.7 nM
VEGFR1/FLT16.8 nM
PDGFRβ9.6 nM




 

*Src

项目号产品名称规格CAS包装细胞靶点IC50
D125110Dasatinib≥99%302962-49-825mg,100mg,500mg,1g,5g无细胞Abl 0.6 nM

Src0.8 nM
c-Kit (D816V)37 nM
c-Kit (wt)79 nM
P127550Ponatinib (AP24534)≥99%943319-70-810mg,50mg,250mg无细胞Abl0.37 nM

PDGFRα1.1 nM
VEGFR21.5 nM
FGFR12.2 nM
c-Src5.4 nM
c-Kit12.5 nM
B129905Bosutinib (SKI-606)≥99%380843-75-410mg,50mg,100mg
S6 kinase 
ERK 
STAT3 
无细胞Abl1 nM
Src1.2 nM
P125444Pelitinib≥98%257933-82-75mg,25mg,100mg
EGFR38.5 nM
Src282 nM
MEK/ERK800 nM
ErbB2 1.255 μM
Raf 3.353 μM
K126255KX2-391≥99%897016-82-91mg,5mg,10mg,50mg
Src (HuH7)9 nM
Src (PLC/PRF/5)13 nM
Src (Hep 3B)26 nM
Src (Hep G2)60 nM
N127928NVP-BHG712≥98%940310-85-05mg,25mg,100mg
EphB425 nM(ED50)
C-Raf0.395 μM
c-Src1.266 μM
c-Abl1.667 μM
E126318ENMD-2076≥99%934353-76-15mg,10mg,50mg
FLT31.86 nM
RET10.4 nM
Aurora A14 nM
VEGFR3/FLT415.9 nM
Src20.2 nM
NTRK1/TRKA24.2 nM 
CSF-1R/c-Fms24.8 nM
LCK43.7 nM
FAK54.9 nM
PDGFRα56.4 nM
VEGFR2/KDR58.2 nM
BLK69.4 nM
FGFR270.8 nM
YES178.4 nM
Abl1 (T315I)81.3 nM
FGFR192.7 nM
Fyn112 nM
JAK2120 nM
Kit120 nM
Aurora B350 nM
P129908PRT062607 (P505-15, BIIB057) HCl≥98%1370261-97-45mg,25mg,无细胞Syk1 nM

FGR81 nM
MLK188 nM
PYK2108 nM
YES123 nM
FLT3139 nM
PAK5166 nM
Lyn192 nM
cSRC244 nM
LCK249 nM
FAK415 nM
P125361PP2≥98%172889-27-95mg,25mg,100mg无细胞LCK4 nM
Fyn5 nM
P126419PP121≥98%1092788-83-410mg,50mg
PDGFR2 nM
Hck8 nM
VEGFR12 nM
mTOR13 nM
Src14 nM
Abl18 nM
p110α52 nM
DNA-PK60 nM
p110δ150 nM
EphB4190 nM
Q111274槲皮素95.00%117-39-51g,10g,50g,250g
Sirtuin
Src
PKC
PI3Kγ2.4 μM
PI3Kδ3.0 μM
PI3Kβ5.4 μM
Q111273槲皮素分析标准品,≥98.5%117-39-520mg
Sirtuin
Src
PKC
PI3Kγ2.4 μM
PI3Kδ3.0 μM
PI3Kβ5.4 μM

 

*Syk

项目号产品名称规格CAS包装细胞靶点IC50
R129913R788 (Fostamatinib) Disodium≥98%1025687-58-450mg,1mg,5mg,10mg无细胞Syk41 nM
R129910R406 (free base)≥99%841290-80-025mg,50mg,100mg,5mg,10mg无细胞Syk41 nM
FLT3
P129908PRT062607 (P505-15, BIIB057) HCl≥98%1370261-97-45mg,25mg无细胞Syk1 nM 

FGR81 nM 
MLK188 nM
PYK2108 nM
YES123 nM 
FLT3139 nM 
PAK5166 nM 
Lyn192 nM
cSRC244 nM
LCK249 nM
FAK415 nM
F129915Fostamatinib (R788)≥98%901119-35-5 50mg,5mg,10mg
Syk41 nM
Adenosine A3 receptor 81 nM
Adenosine transporter1.84 μM
Monoamine transporter2.74 μM

 

*VDA

项目号产品名称规格CAS包装细胞靶点IC50Ki
D129922DMXAA (Vadimezan)≥98% 117570-53-3 5mg,25mg,100mg,250mg无细胞DT-diaphorase62.5 μM20 μM
P126141Plinabulin (NPI-2358)≥97%714272-27-25mg,10mg,50mg,1g肿瘤细胞
Tubulin		9.8~18 nM
V129759 Verteporfin≥97%129497-78-525mg,50mg,1mg,5mg,10mg
 
VDA

YAP/TEAD interaction


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