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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(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)

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IC50Ki 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IC50Ki
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 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 Ki
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

?



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