阿拉丁小分子抑制剂、激动剂、拮抗剂--血管生成信号通路（下）

发布人：上海阿拉丁生化科技股份有限公司

发布日期:2021/1/29 13:41:04

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 IC50 Ki

EC50

R126338

Ruxolitinib (INCB018424)

≥98%

941678-49-5

5mg,25mg,50mg,100mg

无细胞

JAK1

3.3 nM

JAK2

2.8 nM

E129454

Tofacitinib (CP-690550) Citrate

≥99%

540737-29-9

10mg,50mg,250mg

JAK1

112 nM

JAK2

20 nM

JAK3

1 nM

A126326

AZD1480

≥98%

935666-88-9

5mg,25mg,100mg

无细胞

JAK2

0.26 nM

T126330

Fedratinib (SAR302503, TG101348)

≥98%

936091-26-8

5mg,25mg,100mg

无细胞

JAK2

3 nM

J126663

JANEX-1

98%

202475-60-3

5mg,10mg,50mg

JAK3

78 μM

W125855

WHI-P97

≥98%

211555-05-4

10mg,50mg

JAK-3

0.09 μM

C127224

CYT387

≥98%

1056634-68-4

5mg,10mg,50mg,100mg

JAK1

11 nM

JAK2

18 nM

T122330

Tofacitinib

≥98% (HPLC)

477600-75-2

5mg,25mg,100mg,500mg,1g

无细胞

JAK3

1 nM

W129459

WP1066

≥98%

857064-38-1

10mg,50mg

HEL细胞

JAK2

2.30 μM

STAT3

2.43 μM

T127523

TG101209

98%

936091-14-4

5mg,25mg,100mg

无细胞

JAK2

6 nM

Flt3

25 nM

RET

17 nM

L126490

LY2784544

≥98%

1229236-86-5

5mg,10mg,50mg

JAK2

3 nM

N129609

NVP-BSK805 2HCl

≥97%

1092499-93-8

5mg,10mg,50mg

JAK2

0.5 nM

B127687

Baricitinib

≥99%

1187594-09-7

5mg,10mg,50mg

无细胞

JAK1

5.9 nM

JAK2

5.7 nM

A129464

AZ 960

≥99%

905586-69-8

2mg,5mg,10mg

JAK2

＜3 nM

＜0.45 nM

C129474

CEP-33779

≥99%

1257704-57-6

5mg,10mg,50mg

JAK2

1.8 nM

W125072

WHI-P154

≥98%

211555-04-3

10mg,50mg

JAK3

1.8 μM

X127151

XL019

≥99%

945755-56-6

5mg,25mg

JAK2

2.2 nM

S129613

S-Ruxolitinib (INCB018424)

≥99%

941685-37-6

5mg,10mg,50mg

JAK1

3.3 nM

JAK2

2.8 nM

Z129618

ZM 39923 HCl

≥98%

1021868-92-7

10mg,50mg,250mg

JAK1

4.4

JAK3

7.1

R171967

Ruxolitinib phosphate salt

97%

1092939-17-7

100mg

JAK

C114054

莪术醇

分析标准品,≥98%

4871-97-0

20mg

*EGFR

▼

▲

项目号产品名称规格 CAS 包装细胞靶点 IC50 Ki

L126696

Lapatinib

≥99%

231277-92-2

25mg,100mg,250mg,500mg,1g,5g

ErbB2

9.2 nM

EGFR

10.8 nM

L193141

二甲苯磺酸拉帕替尼一水合物

0.98

388082-78-8

1g,5g

EGFR

10.8 nM

ErbB2

9.2 nM

E129310

Erlotinib HCl (OSI-744)

≥99%

183319-69-9

100mg,500mg,1g,5g

无细胞

EGFR

2 nM

G125799

Gefitinib (ZD1839)

≥99%

184475-35-2

50mg,250mg,1g,5g,25g,100g

NR6wtEGFR

Tyr1173

37 nM

Tyr992

37nM

NR6W

Tyr1173

26 nM

Tyr992

57 nM

L129338

二对甲苯磺酸拉帕替尼(GW-572016)

≥98%

388082-77-7

25mg,100mg,250mg,500mg,1g

无细胞

ErbB2

9.2 nM

EGFR

10.8 nM

V125180

Vandetanib (ZD6474)

≥99%

443913-73-3

25mg,100mg,500mg

无细胞

VEGFR2

40 nM

VEGFR3

110 nM

EGFR

500 nM

N126132

Neratinib (HKI-272)

≥99%

698387-09-6

5mg,25mg,100mg

无细胞

ER2

59 nM

EGFR

92 nM

C125447

Canertinib (CI-1033)

≥98%

267243-28-7

10mg,50mg,250mg

EGFR

1.5 nM

ErbB2

9.0 nM

A126525

AG-490 (Tyrphostin B42)

≥98%

133550-30-8

20mg,50mg,250mg,1g

无细胞

EGFR

0.1 μM

C129397

CP-724714

≥99%

537705-08-1

5mg,10mg,25mg,50mg

HER2/ErbB2

10 nM

D129347

Dacomitinib (PF299804, PF299)

≥99%

1110813-31-4

5mg,10mg,50mg,250mg

EGFR

6 nM

W127713

WZ4002

≥98%

1213269-23-8

10mg,50mg,100mg

BaF3细胞系

EGFR(L858R)

2 nM

EGFR(T790M)

8 nM

A129380

AZD8931 (Sapitinib)

≥98%

848942-61-0

5mg,10mg,50mg

无细胞

EGFR

4 nM

ErbB2

3 nM

ErbB3

4 nM

C127191

CUDC-101

≥98%

1012054-59-9

10mg,25mg,50mg,100mg,250mg

HDAC

4.4 nM

EGFR

2.4 nM

HER2

15.7 nM

A126582

AG-1478 (Tyrphostin AG-1478)

≥98%

153436-53-4

5mg,10mg,25mg,50mg

无细胞

EGFR

3 nM

P129384

PD153035 HCl

≥98%(HPLC)

183322-45-4

10mg,50mg,250mg

无细胞

EGFR

29 pM

5.2 pM

P125444

Pelitinib

≥98%

257933-82-7

5mg,25mg,100mg

EGFR

3.5 nM

Src

282 nM

MEK/ERK

800 nM

ErbB2

1255 nM

B126145

AC480 (BMS-599626)

≥98%

714971-09-2

5mg,10mg,25mg,100mg

HER1

20 nM

HER2

30 nM

A126830

AEE788 (NVP-AEE788)

≥97%

497839-62-0

5mg,25mg,100mg

EGFR

2 nM

HER2/ErbB2

6 nM

A127691

AP26113

≥98%

1197958-12-5

5mg,10mg,25mg,

ALK

EGFR

O125033

OSI-420

≥99%

183320-51-6

1mg,5mg,10mg,50mg

EGFR

2 nM

W127717

WZ3146

≥98%

1214265-56-1

1mg,5mg,25mg,100mg

EGFR(L858R)

2 nM

EGFR(E746_A750)

2 nM

A126334

ARRY-380

≥98%

937265-83-3

1mg,5mg,10mg,50mg

HER2

8 nM

W126471

WZ8040

≥98%

1214265-57-2

1mg,5mg,25mg,50mg

EGFR

A129426

AST-1306 TsOH

≥98%

1050500-29-2

5mg,10mg,50mg

EGFR

0.5 nM

ErbB2

3 nM

C124905

CO-1686 (AVL-301)

≥99%

1374640-70-6

5mg,10mg,50mg,100mg

无细胞

EGFRL858R/T790M

21.5 nM

EGFRWT

303.3 nM

G106672

金雀异黄酮

分析标准品,≥98%

446-72-0

20mg,1g,5g

NIH-3T3细胞

EGF

12μM

胰岛素

19 μM

G106673

金雀异黄酮

97%

446-72-0

100mg,500mg,1g,5g,25g

NIH-3T3细胞

EGF

12μM

胰岛素

19 μM

V129433

Varlitinib

≥96%

845272-21-1

1mg,5mg,10mg,50mg

ErbB1(EGFR)

7 nM

ErbB2(HER2)

2 nM

I129405

Icotinib

≥99%

610798-31-7

5mg,10mg,50mg

EGFR

5 nM

T126234

TAK-285

≥98%

871026-44-7

1mg,5mg,10mg,50mg

HER2

17 nM

EGFR(HER1)

23 nM

W125072

WHI-P154

≥98%

211555-04-3

10mg,50mg

JAK3

1.8 μM

D155111

Daphnetin

>90.0%(HPLC)

486-35-1

50mg,100mg,250mg,1g

EGFR

7.67 μM

PKA

9.33 μM

PKC

25.01 μM

P129447

PD168393

≥98%

194423-15-9

10mg,50mg,250mg

EGFR

0.70 nM

T129439

Tyrphostin 9

≥98%

10537-47-0

25mg,50mg,100mg,500mg

EGFR

460 μM

PDGFR

0.5μM

T129445

Tyrphostin 23

≥98%

118409-57-7

10mg,50mg,250mg

EGFR

35 μM

T162509

酪氨酸激酶抑制剂 AG 494

>98.0%(HPLC)(N)

133550-35-3

20mg,100mg

EGFR

1.2 μM

EGF

6 μM

O173511

Olmutinib

97%

1353550-13-6

5mg,100mg

PD153035

≥98%

153436-54-5

10mg,50mg,250mg

EGFR

5.2 pM

E126691

EBE-A22

229476-53-3

5mg,10mg,25mg,50mg,100mg

E107404

(-)-表没食子儿茶素没食子酸

98%

989-51-5

100mg,200mg,2.5g

EGF/HER-2

E107403

(-)-表没食子儿茶素没食子酸

分析标准品

989-51-5

20mg,100mg

EGF/HER-2

E126633

Erlotinib

≥98%

183321-74-6

100mg,500mg,1g,5g

EGFR

2 nM

D101144

大黄酚

97%

481-74-3

50mg,250mg,1g

EGFR

mTOR

D101143

大黄酚

分析标准品,≥98%

481-74-3

20mg

EGFR

mTOR

N159736

Norcantharidin

98%

29745-04-8

1g,5g,25g

c-Met

EGFR

B135922

Butein

≥98.0%(HPLC)

487-52-5

100mg,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%

388082-77-7

25mg,100mg,250mg,500mg,1g

无细胞

ErbB2

9.2 nM

EGFR

10.8 nM

N126132

Neratinib (HKI-272)

≥99%

698387-09-6

5mg,25mg,100mg

无细胞

HER2

59 nM

EGFR

92 nM

C125447

Canertinib (CI-1033)

≥98%

267243-28-7

10mg,50mg,250mg

EGFR

1.5 nM

ErbB2

9.0 nM

L126696

Lapatinib

≥99%

231277-92-2

25mg,100mg,250mg,500mg,1g,5g

ErbB2

9.2 nM

EGFR

10.8 nM

C129397

CP-724714

≥99%

537705-08-1

5mg,10mg,25mg,50mg

HER2/ErbB2

10 nM

D129347

Dacomitinib (PF299804, PF299)

≥99%

1110813-31-4

5mg,10mg,50mg,250mg

EGFR

6 nM

A129380

AZD8931 (Sapitinib)

≥98%

848942-61-0

5mg,10mg,50mg

无细胞

EGFR

4 nM

ErbB2

3 nM

ErbB3

4 nM

C127191

CUDC-101

≥98%

1012054-59-9

10mg,25mg,50mg,10mmg,250mg

HDAC

4.4 nM

EGFR

2.4 nM

HER2

15.7 nM

M129797

Mubritinib (TAK 165)

≥99%

366017-09-6

10mg,50mg,250mg

T-474细胞

HER2/ErbB2

6 nM

B126145

AC480 (BMS-599626)

≥98%

714971-09-2

5mg,10mg,25mg,100mg

HER1

20 nM

HER2

30 nM

A126830

AEE788 (NVP-AEE788)

≥97%

497839-62-0

5mg,25mg,100mg

EGFR

2 nM

HER2/ErbB2

6 nM

T126234

TAK-285

≥98%

871026-44-7

1mg,5mg,10mg,50mg

HER2

17 nM

EGFR(HER1)

23 nM

T129799

Tyrphostin AG 879

≥98%

148741-30-4

5mg,25mg,100mg

HER2/ErbB2

1 μM

N133726

去甲二氢愈创木酸

≥95%

500-38-9

1g,5g

IGF-1R/HER2

L193141

二甲苯磺酸拉帕替尼一水合物

0.98

388082-78-8

1g,5g

EGFR

10.8 nM

ErbB2

9.2 nM

E107404

(-)-表没食子儿茶素没食子酸

98%

989-51-5

100mg,200mg,2.5g

EGF/HER-2

E107403

(-)-表没食子儿茶素没食子酸

分析标准品

989-51-5

20mg,100mg

EGF/HER-2

*HIF

▼

▲

产品号产品名称规格 CAS 包装细胞靶点 IC50

M125960

2-Methoxyestradiol (2-MeOE2)

≥98%

362-07-2

10mg,25mg,50mg,100mg,500mg

P101691

芍药苷

≥98%(HPLC)

23180-57-6

10mg,500mg,5g

P101690

芍药苷

分析标准品,≥98%

23180-57-6

20mg

F126178

FG-4592

≥98%

808118-40-3

10mg,50mg,25mg

HIF-α脯氨酰羟化酶

I127127

IOX2

≥98%

931398-72-0

5mg,25mg,100mg

无细胞

PHD2

21 nM

V171541

Vadadustat

97%

1000025-07-9

100mg

N170064

N-acetylcysteine amide

98% (HPLC)

38520-57-9

5mg,25mg

D136754

DMOG

≥98% (HPLC)

89464-63-1

50mg,100mg,250mg,1g

HIF prolyl hydroxylase

*Bcr-Abl

▼

▲

项目号产品名称规格 CAS 包装细胞靶点 IC50

ED50

D125110

Dasatinib

≥99%

302962-49-8

25mg,100mg,500mg,1g,5g

无细胞

Abl

<1 nM

Src

0.8 nM

c-Kit

79 nM

I129225

Imatinib Mesylate (STI571)

≥99%

220127-57-1

100mg,250mg,1g,5g,25g

v-Abl

0.6 μM

c-Kit

0.1 μM

PDGFR

0.1 μM

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

N126111

Nilotinib (AMN-107)

≥99%

641571-10-0

25mg,100mg,250mg,1g

小鼠骨髓祖细胞

BCR-ABL

＜30 nM

D126182

Danusertib (PHA-739358)

≥98%

827318-97-8

5mg,10mg,50mg

无细胞

Aurora A/B/C

13 nM/79 nM/61 nM

Aurora A/B/C

13 nM/79 nM/61 nM

Aurora A/B/C

13 nM/79 nM/61 nM

B129232

Bafetinib (INNO-406)

≥98%

859212-16-1

5mg,25mg,100mg

无细胞

Bcr-Abl

5.8 nM

Lyn

19 nM

K127169

KW-2449

≥98%

1000669-72-6

5mg,25mg,100mg

Flt3

6.6 nM

N127928

NVP-BHG712

≥98%

940310-85-0

5mg,25mg,100mg

EphB4

25 nM

c-Raf

0.395 μM

c-Src

1.266 μM

c-Abl

1.667 μM

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

D126373

DCC-2036 (Rebastinib)

≥99%

1020172-07-9

10mg,50mg

Abl1(WT)

0.8 nM

Abl1(T315I)

4 nM

G129296

GZD824

≥99%

1421783-64-3

5mg,25mg

Bcr-Abl(WT)

0.34 nM

Bcr-Abl(T315I)

0.68 nM

G126166

GNF-2

≥98%

778270-11-4

5mg,25mg,50mg,250mg

Bcr-Abl

G177569

GNF-7

97%

839706-07-9

100mg

M351T

<5 nM

T315I

61 nM

E255 V

122 nM

G250E

136 nM

c-Abl

133 nM

*FAK

▼

▲

项目号产品名称规格 CAS 包装细胞靶点 IC50

P129811

PF-00562271

≥97%

939791-38-5

5mg,10mg,50mg

FAK

1.5 nM

P126147

PF-562271

≥98%

717907-75-0

5mg,10mg,50mg,100mg

FAK

1.5 nM

P129908

PRT062607 (P505-15, BIIB057) HCl

≥98%

1370261-97-4

5mg,25mg

无细胞

Syk

1 nM

P129814

PF-573228

≥98%

869288-64-2

10mg,50mg

无细胞

FAK

4 nM

T129808

TAE226 (NVP-TAE226)

≥99%

761437-28-9

5mg,10mg,50mg

FAK

5.5 nM

P127543

PF-03814735

≥99%

942487-16-3

1mg,5mg,10mg,50mg

Aurora A

0.8 nM

Aurora B

0.5 nM

P126394

PND-1186

≥98%

1061353-68-1

5mg,25mg,100mg

FAK

1.5 nM

P127348

PF-431396

≥98%

717906-29-1

10mg,50mg

PYK2

11nM

FAK

2 nM

*ALK

▼

▲

项目号产品名称规格 CAS 包装细胞靶点 IC50

C137735

Crizotinib

≥99%

877399-52-5

10mg,50mg,100mg,250mg,500mg,1g,5g

无细胞

c-Met

11 nM

ALK

24 nM

T129819

TAE684 (NVP-TAE684)

≥98%

761439-42-3

5mg,10mg,50mg

无细胞

ALK

3 nM

C125242

CH5424802

≥98%

1256580-46-7

5mg,25mg,100mg

无细胞

ALK

1.9 nM

L127618

LDK378

≥99%

1032900-25-6

5mg,25mg,100mg,250mg

无细胞

ALK

0.2 nM

A127691

AP26113

≥98%

1197958-12-5

5mg,10mg,25mg,50mg,100mg

ALK

EGFR

A125664

AZD3463

≥98%

1356962-20-3

5mg,25mg,100mg

ALK

0.75 nM

A128022

ASP3026

≥98%

1097917-15-1

5mg,25mg,100mg

ALK

3.5 nM

P167337

PF-06463922 acetate

98% (HPLC)

1454846-35-5

5mg

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

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

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

N127052

BGJ398 (NVP-BGJ398)

≥98%

872511-34-7

5mg,25mg,10mg

无细胞

FGFR1

0.9 nM

FGFR2

1.4 nM

FGFR3

1 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

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

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

A127209

AZD4547

≥99%

1035270-39-3

5mg,10mg,25mg,50mg,100mg

无细胞

FGFR1

0.2 nM

FGFR2

2.5 nM

FGFR3

1.8 nM

D126182

Danusertib (PHA-739358)

≥98%

827318-97-8

1mg,5mg,10mg,50mg

无细胞

Aurora A

13 nM

Aurora B

79 nM

Aurora C

61 nM

L125518

Lenvatinib (E7080)

≥99%

417716-92-8

5mg,10mg,50mg,100mg

无细胞

VEGFR2/KDR

4.0 nM

VEGFR3/FLT4

5.2 nM

B127317

Brivanib (BMS-540215)

≥98%

649735-46-6

5mg,10mg,50mg

VEGFR2

25 nM

E126318

ENMD-2076

≥99%

934353-76-1

5mg,10mg,50mg

Aurora A

14 nM

Flt3

1.86 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

M129777

MK-2461

≥99%

917879-39-1

1mg,5mg,10mg,50mg

c-Met(WT/mutants)

0.4-2.5 nM

B129764

Brivanib Alaninate (BMS-582664)

≥95%

649735-63-7

10mg,50mg

VEGFR2

25 nM

T129775

Tyrphostin AG 1296

≥99%

146535-11-7

1mg,5mg,25mg

PDGFR

0.3-0.5 μM

Swiss 3T3细胞

FGFR

12.3 μM

c-Kit

1.8 μM

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

F103701

阿魏酸

99%

1135-24-6

5g,10g,25g,50g,100g,250g,500g,1kg

F103702

阿魏酸

分析标准品,≥99.5%（HPLC）

1135-24-6

20mg

O173545

ON-123300

97%

1357470-29-1

5mg,100mg

CDK4

3.9 nM

Ark5/NUAK1

5 nM

PDGFRβ

26 nM

FGFR1

26 nM

RET

9.2 nM

Fyn

11nM

P132694

PD-166866

≥98%(HPLC)

192705-79-6

5mg,25mg,100mg

FGFR1

52.4 nM

B174512

BLU-9931

97%

1538604-68-0

5mg,100mg

FGFR4

3 nM