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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)

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分享: 2021/01/29 14:17:48

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


[来源:上海阿拉丁生化科技股份有限公司]

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