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首页 >  新闻动态 >  阿拉丁小分子抑制剂、激动剂、拮抗剂--血管生成信号通路(下)

阿拉丁小分子抑制剂、激动剂、拮抗剂--血管生成信号通路(下)

发布时间:2021-01-29

阿拉丁小分子抑制剂、激动剂、拮抗剂--血管生成信号通路(下)

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

   *JAK

项目号产品名称规格CAS包装细胞靶点IC50KiEC50
R126338Ruxolitinib (INCB018424)≥98%941678-49-55mg,25mg,50mg,100mg无细胞JAK13.3 nM

JAK22.8 nM

E129454Tofacitinib (CP-690550) Citrate≥99%540737-29-910mg,50mg,250mg
JAK1112 nM

JAK220 nM

JAK31 nM

A126326AZD1480≥98%935666-88-95mg,25mg,100mg无细胞JAK20.26 nM

T126330Fedratinib (SAR302503, TG101348)≥98%936091-26-85mg,25mg,100mg无细胞JAK23 nM

J126663JANEX-198%202475-60-35mg,10mg,50mg
JAK378 μM

W125855WHI-P97≥98%211555-05-410mg,50mg
JAK-3
0.09 μM
C127224CYT387≥98%1056634-68-45mg,10mg,50mg,100mg
JAK111 nM

JAK218 nM

T122330Tofacitinib≥98% (HPLC)477600-75-25mg,25mg,100mg,500mg,1g无细胞JAK31 nM

W129459WP1066≥98%857064-38-110mg,50mgHEL细胞JAK22.30 μM

STAT32.43 μM

T127523TG10120998%936091-14-45mg,25mg,100mg无细胞JAK26 nM

Flt325 nM

RET17 nM

L126490LY2784544≥98%1229236-86-55mg,10mg,50mg
JAK23 nM

N129609NVP-BSK805 2HCl≥97%1092499-93-85mg,10mg,50mg
JAK20.5 nM

B127687Baricitinib≥99%1187594-09-75mg,10mg,50mg无细胞JAK15.9 nM

JAK25.7 nM

A129464AZ 960≥99%905586-69-82mg,5mg,10mg
JAK2<3 nM<0.45 nM
C129474CEP-33779≥99%1257704-57-65mg,10mg,50mg
JAK21.8 nM

W125072WHI-P154≥98%211555-04-310mg,50mg
JAK31.8 μM

X127151XL019≥99%945755-56-6 5mg,25mg
JAK22.2 nM

S129613S-Ruxolitinib (INCB018424)≥99%941685-37-65mg,10mg,50mg
JAK13.3 nM

JAK22.8 nM

Z129618ZM 39923 HCl≥98%1021868-92-710mg,50mg,250mg
JAK1

4.4
JAK3

7.1
R171967Ruxolitinib phosphate salt97%1092939-17-7100mg
JAK


C114054莪术醇分析标准品,≥98%4871-97-020mg




 

 *EGFR

项目号产品名称规格CAS包装细胞靶点IC50Ki
L126696Lapatinib≥99%231277-92-225mg,100mg,250mg,500mg,1g,5g
ErbB29.2 nM
EGFR10.8 nM
L193141二甲苯磺酸拉帕替尼 一水合物0.98388082-78-81g,5g
EGFR10.8 nM
ErbB29.2 nM
E129310Erlotinib HCl (OSI-744)≥99%183319-69-9100mg,500mg,1g,5g无细胞EGFR2 nM
G125799Gefitinib (ZD1839)≥99%184475-35-250mg,250mg,1g,5g,25g,100gNR6wtEGFRTyr117337 nM
Tyr99237nM
NR6WTyr117326 nM
Tyr99257 nM
L129338二对甲苯磺酸拉帕替尼(GW-572016)≥98%388082-77-725mg,100mg,250mg,500mg,1g无细胞ErbB29.2 nM
EGFR10.8 nM
V125180Vandetanib (ZD6474)≥99%443913-73-325mg,100mg,500mg无细胞VEGFR240 nM
VEGFR3110 nM
EGFR500 nM
N126132Neratinib (HKI-272)≥99%698387-09-65mg,25mg,100mg无细胞ER259 nM
EGFR92 nM
C125447Canertinib (CI-1033)≥98%267243-28-710mg,50mg,250mg
EGFR1.5 nM
ErbB29.0 nM
A126525AG-490 (Tyrphostin B42)≥98%133550-30-820mg,50mg,250mg,1g无细胞EGFR0.1 μM
C129397CP-724714≥99%537705-08-15mg,10mg,25mg,50mg
HER2/ErbB210 nM
D129347Dacomitinib (PF299804, PF299)≥99%1110813-31-45mg,10mg,50mg,250mg
EGFR6 nM
W127713WZ4002≥98%1213269-23-810mg,50mg,100mgBaF3细胞系EGFR(L858R)2 nM
EGFR(T790M)8 nM
A129380AZD8931 (Sapitinib)≥98%848942-61-05mg,10mg,50mg无细胞EGFR4 nM
ErbB23 nM
ErbB34 nM
C127191CUDC-101≥98%1012054-59-910mg,25mg,50mg,100mg,250mg
HDAC4.4 nM
EGFR2.4 nM
HER215.7 nM
A126582AG-1478 (Tyrphostin AG-1478)≥98%153436-53-45mg,10mg,25mg,50mg无细胞EGFR3 nM
P129384PD153035 HCl≥98%(HPLC)183322-45-410mg,50mg,250mg无细胞EGFR29 pM5.2 pM
P125444Pelitinib≥98%257933-82-75mg,25mg,100mg
EGFR3.5 nM
Src282 nM
MEK/ERK800 nM
ErbB21255 nM
B126145AC480 (BMS-599626)≥98%714971-09-25mg,10mg,25mg,100mg
HER120 nM
HER230 nM
A126830AEE788 (NVP-AEE788)≥97%497839-62-05mg,25mg,100mg
EGFR2 nM
HER2/ErbB26 nM
A127691AP26113≥98%1197958-12-55mg,10mg,25mg,
ALK

EGFR

O125033OSI-420≥99%183320-51-61mg,5mg,10mg,50mg
EGFR2 nM
W127717WZ3146≥98%1214265-56-11mg,5mg,25mg,100mg
EGFR(L858R)2 nM
EGFR(E746_A750)2 nM
A126334ARRY-380≥98%937265-83-31mg,5mg,10mg,50mg
HER28 nM
W126471WZ8040≥98%1214265-57-21mg,5mg,25mg,50mg
EGFR

A129426AST-1306 TsOH≥98%1050500-29-25mg,10mg,50mg
EGFR0.5 nM
ErbB23 nM
C124905CO-1686 (AVL-301)≥99%1374640-70-65mg,10mg,50mg,100mg无细胞EGFRL858R/T790M21.5 nM
EGFRWT
303.3 nM
G106672金雀异黄酮分析标准品,≥98%446-72-020mg,1g,5gNIH-3T3细胞EGF12μM
胰岛素19 μM
G106673金雀异黄酮97%446-72-0100mg,500mg,1g,5g,25gNIH-3T3细胞EGF12μM
胰岛素19 μM
V129433Varlitinib≥96%845272-21-11mg,5mg,10mg,50mg
ErbB1(EGFR)7 nM
ErbB2(HER2)2 nM
I129405Icotinib≥99%610798-31-75mg,10mg,50mg
EGFR5 nM
T126234TAK-285≥98%871026-44-71mg,5mg,10mg,50mg
HER217 nM
EGFR(HER1)23 nM
W125072WHI-P154≥98%211555-04-310mg,50mg
JAK31.8 μM
D155111Daphnetin>90.0%(HPLC)486-35-150mg,100mg,250mg,1g
EGFR7.67 μM
PKA9.33 μM
PKC25.01 μM
P129447PD168393≥98%194423-15-910mg,50mg,250mg
EGFR0.70 nM
T129439Tyrphostin 9≥98%10537-47-025mg,50mg,100mg,500mg
EGFR460 μM
PDGFR0.5μM
T129445Tyrphostin 23≥98%118409-57-710mg,50mg,250mg
EGFR35 μM
T162509酪氨酸激酶抑制剂 AG 494>98.0%(HPLC)(N)133550-35-320mg,100mg
EGFR1.2 μM
EGF6 μM
O173511Olmutinib97%1353550-13-65mg,100mg



PD153035PD153035≥98%153436-54-510mg,50mg,250mg
EGFR
5.2 pM
E126691EBE-A22-229476-53-35mg,10mg,25mg,50mg,100mg



E107404(-)-表没食子儿茶素没食子酸98%989-51-5100mg,200mg,2.5g
EGF/HER-2

E107403(-)-表没食子儿茶素没食子酸分析标准品989-51-520mg,100mg
EGF/HER-2

E126633Erlotinib≥98%183321-74-6100mg,500mg,1g,5g
EGFR2 nM
D101144大黄酚97%481-74-350mg,250mg,1g
EGFR

mTOR

D101143大黄酚分析标准品,≥98%481-74-320mg
EGFR

mTOR

N159736Norcantharidin98%29745-04-81g,5g,25g
c-Met

EGFR

B135922Butein≥98.0%(HPLC)487-52-5100mg,1g
EGFR

 

*HER2

项目号产品名称规格CAS包装细胞靶点IC50
L129338二对甲苯磺酸拉帕替尼(GW-572016)≥98%388082-77-725mg,100mg,250mg,500mg,1g无细胞ErbB29.2 nM
EGFR10.8 nM
N126132Neratinib (HKI-272)≥99%698387-09-65mg,25mg,100mg无细胞HER259 nM
EGFR92 nM
C125447Canertinib (CI-1033)≥98%267243-28-710mg,50mg,250mg
EGFR1.5 nM
ErbB29.0 nM
L126696Lapatinib≥99%231277-92-225mg,100mg,250mg,500mg,1g,5g
ErbB29.2 nM
EGFR10.8 nM
C129397CP-724714≥99%537705-08-15mg,10mg,25mg,50mg
HER2/ErbB210 nM
D129347Dacomitinib (PF299804, PF299)≥99%1110813-31-45mg,10mg,50mg,250mg
EGFR6 nM
A129380AZD8931 (Sapitinib)≥98%848942-61-05mg,10mg,50mg无细胞EGFR4 nM
ErbB23 nM
ErbB34 nM
C127191CUDC-101≥98%1012054-59-910mg,25mg,50mg,10mmg,250mg
HDAC4.4 nM
EGFR2.4 nM
HER215.7 nM
M129797Mubritinib (TAK 165)≥99%366017-09-610mg,50mg,250mgT-474细胞HER2/ErbB26 nM
B126145AC480 (BMS-599626)≥98%714971-09-25mg,10mg,25mg,100mg
HER120 nM
HER230 nM
A126830AEE788 (NVP-AEE788)≥97%497839-62-05mg,25mg,100mg
EGFR2 nM
HER2/ErbB26 nM
T126234TAK-285≥98%871026-44-71mg,5mg,10mg,50mg
HER217 nM
EGFR(HER1)23 nM
T129799Tyrphostin AG 879≥98%148741-30-45mg,25mg,100mg
HER2/ErbB21 μM
N133726去甲二氢愈创木酸≥95%500-38-91g,5g
IGF-1R/HER2
L193141二甲苯磺酸拉帕替尼 一水合物0.98388082-78-81g,5g
EGFR10.8 nM
ErbB29.2 nM
E107404(-)-表没食子儿茶素没食子酸98%989-51-5100mg,200mg,2.5g
EGF/HER-2
E107403(-)-表没食子儿茶素没食子酸分析标准品989-51-520mg,100mg
EGF/HER-2

 

*HIF

产品号产品名称规格CAS包装细胞靶点IC50
M1259602-Methoxyestradiol (2-MeOE2)≥98%362-07-210mg,25mg,50mg,100mg,500mg


P101691芍药苷≥98%(HPLC)23180-57-610mg,500mg,5g


P101690芍药苷分析标准品,≥98%23180-57-620mg


F126178FG-4592≥98%808118-40-310mg,50mg,25mg
HIF-α脯氨酰羟化酶
I127127IOX2≥98%931398-72-05mg,25mg,100mg无细胞PHD221 nM
V171541Vadadustat97%1000025-07-9100mg


N170064N-acetylcysteine amide98% (HPLC)38520-57-95mg,25mg


D136754DMOG≥98% (HPLC)89464-63-150mg,100mg,250mg,1g
HIF prolyl hydroxylase

 

*Bcr-Abl

项目号产品名称规格CAS包装细胞靶点IC50ED50
D125110Dasatinib≥99%302962-49-825mg,100mg,500mg,1g,5g无细胞Abl<1 nM
Src0.8 nM 
c-Kit79 nM
I129225Imatinib Mesylate (STI571)≥99%220127-57-1100mg,250mg,1g,5g,25g
v-Abl0.6 μM
c-Kit0.1 μM
PDGFR0.1 μM
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
N126111Nilotinib (AMN-107)≥99%641571-10-025mg,100mg,250mg,1g小鼠骨髓祖细胞BCR-ABL<30 nM
D126182Danusertib (PHA-739358)≥98%827318-97-85mg,10mg,50mg无细胞Aurora A/B/C13 nM/79 nM/61 nM
Aurora A/B/C13 nM/79 nM/61 nM
Aurora A/B/C13 nM/79 nM/61 nM
B129232Bafetinib (INNO-406)≥98%859212-16-15mg,25mg,100mg无细胞Bcr-Abl5.8 nM
Lyn19 nM
K127169KW-2449≥98%1000669-72-65mg,25mg,100mg
Flt36.6 nM
N127928NVP-BHG712≥98%940310-85-05mg,25mg,100mg
EphB4
25 nM
c-Raf0.395 μM
c-Src1.266 μM
c-Abl1.667 μM
P126419PP121≥98%1092788-83-410mg,50mg
PDGFR2 nM
Hck8 nM
mTOR10 nM
VEGFR212 nM
Src14 nM
Abl18 nM
DNA-PK60 nM
D126373DCC-2036 (Rebastinib)≥99%1020172-07-910mg,50mg
Abl1(WT)0.8 nM
Abl1(T315I)4 nM
G129296GZD824≥99%1421783-64-35mg,25mg
Bcr-Abl(WT)0.34 nM
Bcr-Abl(T315I)0.68 nM
G126166GNF-2≥98%778270-11-45mg,25mg,50mg,250mg
Bcr-Abl

G177569GNF-797%839706-07-9100mg
M351T<5 nM
T315I61 nM
E255 V122 nM
G250E136 nM
c-Abl133 nM

 

*FAK

项目号产品名称规格CAS包装细胞靶点IC50
P129811PF-00562271≥97%939791-38-55mg,10mg,50mg
FAK1.5 nM
P126147PF-562271≥98%717907-75-05mg,10mg,50mg,100mg
FAK1.5 nM
P129908PRT062607 (P505-15, BIIB057) HCl≥98%1370261-97-45mg,25mg无细胞Syk1 nM
P129814PF-573228≥98%869288-64-210mg,50mg无细胞FAK4 nM
T129808TAE226 (NVP-TAE226)≥99%761437-28-95mg,10mg,50mg
FAK5.5 nM
P127543PF-03814735≥99%942487-16-31mg,5mg,10mg,50mg
Aurora A0.8 nM
Aurora B0.5 nM
P126394PND-1186≥98%1061353-68-15mg,25mg,100mg
FAK1.5 nM
P127348PF-431396≥98%717906-29-110mg,50mg
PYK211nM
FAK2 nM

 

*ALK

项目号产品名称规格CAS包装细胞靶点IC50Ki
C137735Crizotinib≥99%877399-52-510mg,50mg,100mg,250mg,500mg,1g,5g无细胞c-Met11 nM
ALK24 nM
T129819TAE684 (NVP-TAE684)≥98%761439-42-35mg,10mg,50mg无细胞ALK3 nM
C125242CH5424802≥98%1256580-46-75mg,25mg,100mg无细胞ALK1.9 nM
L127618LDK378≥99%1032900-25-65mg,25mg,100mg,250mg无细胞ALK0.2 nM
A127691AP26113≥98%1197958-12-55mg,10mg,25mg,50mg,100mg
ALK

EGFR

A125664AZD3463≥98%1356962-20-35mg,25mg,100mg
ALK
0.75 nM
A128022ASP3026≥98%1097917-15-15mg,25mg,100mg
ALK 3.5 nM
P167337PF-06463922 acetate98% (HPLC)1454846-35-55mg
ROS1
<0.02 nM
ALK (WT)
<0.07 nM
ALK (L1196M)
0.7 nM

 

*FGFR

产品号产品名称规格CAS包装细胞靶点IC50
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
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
N127052BGJ398 (NVP-BGJ398)≥98%872511-34-75mg,25mg,10mg无细胞FGFR10.9 nM
FGFR21.4 nM
FGFR31 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
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
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
A127209AZD4547≥99%1035270-39-35mg,10mg,25mg,50mg,100mg无细胞FGFR10.2 nM
FGFR22.5 nM
FGFR31.8 nM
D126182Danusertib (PHA-739358)≥98%827318-97-81mg,5mg,10mg,50mg无细胞Aurora A13 nM
Aurora B79 nM
Aurora C61 nM
L125518Lenvatinib (E7080)≥99%417716-92-85mg,10mg,50mg,100mg无细胞VEGFR2/KDR 4.0 nM
VEGFR3/FLT45.2 nM
B127317Brivanib (BMS-540215)≥98%649735-46-65mg,10mg,50mg
VEGFR225 nM
E126318ENMD-2076≥99%934353-76-15mg,10mg,50mg
Aurora A14 nM
Flt31.86 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
M129777MK-2461≥99%917879-39-11mg,5mg,10mg,50mg
c-Met(WT/mutants)0.4-2.5 nM
B129764Brivanib Alaninate (BMS-582664)≥95%649735-63-710mg,50mg
VEGFR225 nM
T129775Tyrphostin AG 1296≥99%146535-11-71mg,5mg,25mg
PDGFR0.3-0.5 μM
Swiss 3T3细胞FGFR12.3 μM
c-Kit 1.8 μM
L126507LY2874455≥99%1254473-64-75mg,10mg,50mg
FGFR12.8 nM
FGFR22.6 nM
FGFR36.4 nM
FGFR46 nM
VEGFR27 nM
F103701阿魏酸99%1135-24-65g,10g,25g,50g,100g,250g,500g,1kg


F103702阿魏酸分析标准品,≥99.5%(HPLC)1135-24-620mg


O173545ON-12330097%1357470-29-15mg,100mg
CDK43.9 nM
Ark5/NUAK15 nM
PDGFRβ26 nM
FGFR126 nM
RET9.2 nM
Fyn11nM
P132694PD-166866≥98%(HPLC)192705-79-65mg,25mg,100mg
FGFR152.4 nM
B174512BLU-993197%1538604-68-05mg,100mg
FGFR43 nM


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