阿拉丁小分子抑制剂、激动剂、拮抗剂--血管生成信号通路（上）

发布人：上海阿拉丁生化科技股份有限公司

发布日期:2021/1/29 13:42:12

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