Saracatinib (AZD0530)

目录号:S1006

Saracatinib (AZD0530) Chemical Structure

Molecular Weight(MW): 542.03

Saracatinib (AZD0530)是一种有效的Src抑制剂,无细胞试验中IC50为2.7 nM,对c-Yes, Fyn, Lyn, Blk, Fgr和Lck也具有活性;但对Abl和EGFR (L858R和L861Q)活性较低。Phase 2/3。

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RMB 746.35 现货
RMB 569.55 现货
RMB 1395.95 现货
RMB 5472.84 现货
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客户购买Selleck的此次产品后发表的文献35篇:

客户使用该产品的8个实验数据:

  • Saracatinib (AZD0530) administration alleviates provocative tumor formation conferred by LHBs exp ression. A and B, cell proliferation assay for Huh7 cells (A) and SK-Hep1 cells (B) after stable LHBs expression under treatment with saracatinib(1 μmol/L). *, P < 0.05.

    Cancer Res 2012 71, 7547-57. Saracatinib (AZD0530) purchased from Selleck.

    C and D, in vivo subcutaneous tumor growth curves (C) and tumor weight quantification of intersected subcutaneous tumor tissues (D) of Huh7 cells after stable LHBs expression under saracatinib treatment (25 mg/kg body weight daily for 4 weeks; n =18). *, P < 0.05. E and F,in vivo subcutaneous tumor growth curves (E) and tumor weight quantification of intersected subcutaneous tumor tissues (F) of SK-Hep1 cells after stable LHBs expression under saracatinib treatment (25 mg/kg body weight daily for 4 weeks; n = 18). *, P < 0.05.

    Cancer Res 2013 71, 7547-57. Saracatinib (AZD0530) purchased from Selleck.

  • cells treated for 1 hour with Src inhibitor AZD0530 (50 mmol/L), or the same volume of dimethyl sulfoxide, before TRAIL treatment (at concentrations described earlier) for 24 hours prior to alamar blue assay.

    Mol Cancer Res 2011 9, 249-258. Saracatinib (AZD0530) purchased from Selleck.

    MCF7 cells were plated in triplicate and treated with vehicle (VEH, DMSO) , AZD0530 (125 nM), AZD7762 (50 nM) or AZD7762 and AZD0530. Cells were isolated 48 h after exposure and subjected to the indicated various cell viability assays. Data for each assay is the mean of all data points from two studies(* p < 0.05 greater than CHK1 inhibitor value).

    Cancer Biol Ther 2011 12(3), 215-28. Saracatinib (AZD0530) purchased from Selleck.

  •  

    The TMZ-induced caveolin-1 modulation is Src-dependent in Hs683 GBM cells Western blot analyses of soluble caveolin-1 expression in Hs683 glioma cells treated with TMZ (100 μM) four times per week (day 1-4) for 7 h/d, the EGFR inhibitor (10 μM) (erlotinib; day 1), the Src inhibitor AZD0530 (10 μM) (day 1), and combination of the inhibitors and TMZ (+TMZ) compared with control untreated cells (Ct). Soluble caveolin-1 expression was measured on day 5.

    Transl Oncol 2011 4, 92-100. Saracatinib (AZD0530) purchased from Selleck.

    J Biomol Screen 2013 18, 54-66. Saracatinib (AZD0530) purchased from Selleck.

  • Example dose response curves of the PLK-1 inhibitor BI-2536. During the large dose response study for each reference compounds 8 dilutions were tested. Curves for IC50 determination for two independent experiments for the PLK1 inhibitor BI-2536 are displayed. This inhibitor is also used to achieve the LC values. IC50 has been determined with 7.48 +/- 0.09 log [M] and 6.75 +/- 0.21 log [M]. Correlating assay performance data are displayed in Suppl. Fig. 5. 

    J Biomol Screen 2013 18, 54-66. Saracatinib (AZD0530) purchased from Selleck.

    IP assay of tyrosine phosphorylation of VDR in the plasmamembrane. Primary human hepatocytes were treated with Veh, 1α, 25(OH)2-VD3 (50nM), LCA-acetate (10 μM), and/or the c-Src inhibitor AZD0530 (AZD) (5 μM) for 6 h.A rabbit anti-VDR antibody was used to immunoprecipitate VDR from cell membrane extracts (300 μg). A mouse anti-phospho-tyrosine was used to detect phosphotyrosines in VDR. A mouse anti-VDR was used to detect immunoprecipitated VDR. Ten % cell extract was set aside as input. Q-PCR assay of the effects of AZD on CYP7A1,CYP27A1, and CYP24A1 mRNA expression in primary human hepatocytes. Primary human hepatocytes were treated with Veh, 1α, 25(OH)2-VD3 (50 nM), LCA-acetate (10 μM), and/or AZD (5 μM) for 16 h. An $, *, or # indicates statistically significant difference, p < 0.05, AZD-treated versus vehicle control, 1α, 25(OH)2-VD3 or LCAacetate-treated versus vehicle control, or 1α, 25(OH)2-VD3 plus AZD or LCA-acetateplus AZD co-treated versus 1α, 25(OH)2-VD3 or LCA-acetate-treated. All the datarepresent one of three separate experiments using primary human hepatocytes from different liver donors (#HH1479, #HH1483, #HH1493, #HH1524, #HH1560, and#HH1567).

     

     

    2010 Dr. Shuxin Han of Kent State University. Saracatinib (AZD0530) purchased from Selleck.

产品安全说明书

Src抑制剂选择性比较

生物活性

产品描述 Saracatinib (AZD0530)是一种有效的Src抑制剂,无细胞试验中IC50为2.7 nM,对c-Yes, Fyn, Lyn, Blk, Fgr和Lck也具有活性;但对Abl和EGFR (L858R和L861Q)活性较低。Phase 2/3。
特性 Saracatinib是第一个作用于人类肿瘤组织Src通路的抑制剂。
靶点
c-Src [2]
(Cell-free assay)
LCK [2]
(Cell-free assay)
c-YES [2]
(Cell-free assay)
EGFR (L861Q) [2]
(Cell-free assay)
Lyn [2]
(Cell-free assay)
2.7 nM <4 nM 4 nM 4 nM 5 nM
体外研究

Saracatinib也有效抑制其他Src酪氨酸激酶家族成员,包括c-Yes, Fyn, Lyn, Blk, Fgr, 和Lck,IC50为4到10 nM。Saracatinib有效抑制SrcY530F突变的NIH 3T3细胞,IC50为80 nM。在NBT-II膀胱癌细胞中,Saracatinib显著阻断HT1080细胞通过立体骨胶原基质的入侵,且完全抑制EGF诱导的细胞分散。[1]Saracatinib作用于DU145和PC3细胞,通过抑制Y419磷酸化而有效抑制Src激活。Saracatinib抑制前列腺癌包括PC3, DU145, CWR22Rv1和 LNCaP的生长,而Saracatinib作用于 LAPC-4, PZ-HPV7和RWPE-1细胞时却显示低活性。Saracatinib使细胞周期停止在G1/S期,但是不使caspase 3断裂。Saracatinib 也明显抑制Boyden 小室的DU145和PC3 移动。[2]Saracatinib有效且持久抑制Akt,且增强A549和Calu-6细胞对放射处理的敏感性。[3]Saracatinib在活性,再吸收,及组成上抑制蚀骨细胞。Saracatinib也可逆阻断蚀骨细胞前体的移动。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CTV-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHO0RllKSzVyPUCuNFYyPDNizszN M3PjU3NCVkeHUh?=
LAMA-84 MlHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHyTWM2OD1yLkG1PVkh|ryP NX\sNYJ{W0GQR1XS
MEG-01 M1PRPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXDZ|FoUUN3ME2wMlI{Pjh6IN88US=> M4\kZXNCVkeHUh?=
EM-2 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;uTWM2OD1yLkK2OUDPxE1? M3HNXXNCVkeHUh?=
TE-15 NH\EXnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\o[JZsUUN3ME2wMlI4PDF{IN88US=> NYnXT5ZrW0GQR1XS
NCI-H1648 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHizS2pKSzVyPUCuNlgyOTZizszN MUHTRW5ITVJ?
TE-12 NVPOTpVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mni4TWM2OD1yLkOyOlgh|ryP M3j6OnNCVkeHUh?=
LB996-RCC MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzRSVlPUUN3ME2wMlQ1OTl4IN88US=> NXXoS5htW0GQR1XS
K-562 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjmVWpsUUN3ME2wMlQ1QTZ5IN88US=> MWTTRW5ITVJ?
D-336MG M4jOU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPETWM2OD1yLkWwN|A1KM7:TR?= M1qwWnNCVkeHUh?=
NOS-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zOdmlEPTB;MD62NFUzQSEQvF2= NULId4t[W0GQR1XS
EW-24 MlzoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2f2RWlEPTB;MD62NlY6OyEQvF2= MV;TRW5ITVJ?
BV-173 Mn;xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTBwNkWyOFkh|ryP MlTXV2FPT0WU
NCCIT MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnEemxKSzVyPUCuO|MzOThizszN MV;TRW5ITVJ?
NCI-H1436 NWXkSHRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGS0N5dKSzVyPUCuO|kxPDlizszN NUmx[IN5W0GQR1XS
BB30-HNC MnHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPOTWM2OD1yLki2NlA{KM7:TR?= NYX4V3pTW0GQR1XS
TE-8 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFviXY9KSzVyPUCuPFczPzVizszN NHO5S|RUSU6JRWK=
A704 NVrMZo1lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVz6N5RzUUN3ME2wMlg6OjFizszN MoryV2FPT0WU
TK10 NHTmTnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTBwOUC2Olkh|ryP NVvKOlIxW0GQR1XS
KS-1 NWXSdXM1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPLeI5KSzVyPUGuNVk4PzlizszN MmXKV2FPT0WU
C2BBe1 M{SxfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzqTWM2OD1zLkKwOVA4KM7:TR?= NUjBeHlPW0GQR1XS
RXF393 NFzEXndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7LTWM2OD1zLkK0N|Yh|ryP NHvzepNUSU6JRWK=
KGN Mne4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTFwMke2PFch|ryP MYPTRW5ITVJ?
NB69 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3CZ3RKSzVyPUGuN|c1QTdizszN NVW0Oo1mW0GQR1XS
TE-11 M1jPVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33NNWlEPTB;MT60N|QyQCEQvF2= NX;ObGt7W0GQR1XS
TE-1 M{fzWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTFwNESxNFUh|ryP MWLTRW5ITVJ?
ST486 M1PzSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTFwNEW4OVIh|ryP M2fxWXNCVkeHUh?=
HOP-62 MlvzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nsdGlEPTB;MT61NFI1PiEQvF2= NVnIT4xYW0GQR1XS
EW-16 NIDpb2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFz3eJZKSzVyPUGuOVUxQDNizszN NUL4XXpoW0GQR1XS
LB1047-RCC MlftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLo[GRKSzVyPUGuOVU1PTNizszN NEXMb4dUSU6JRWK=
TE-10 NWTGS4ZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPBNIpKSzVyPUGuOlYzPTJizszN MljTV2FPT0WU
RL95-2 MnPwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnmV4JKSzVyPUGuOlY6ODJizszN NVK1ZWgxW0GQR1XS
DOHH-2 NGTRdm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;YNZZiUUN3ME2xMlcyPzh{IN88US=> NHGzNplUSU6JRWK=
MFH-ino MkizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorxTWM2OD1zLke3PFch|ryP MYfTRW5ITVJ?
GB-1 NHThNVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4L4OWlEPTB;MT63PVg{OyEQvF2= NEXCRpBUSU6JRWK=
SK-N-DZ MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vsPGlEPTB;MT64OFY5QCEQvF2= MX7TRW5ITVJ?
OS-RC-2 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTFwOEi1O|Qh|ryP NXq5blB{W0GQR1XS
SW982 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF2wdI9KSzVyPUGuPVIxQTNizszN M3fuOHNCVkeHUh?=
KALS-1 MmfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoP6TWM2OD1zLkm4O|IzKM7:TR?= MmK4V2FPT0WU
TGBC24TKB NYWyd5pxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXtUI9KSzVyPUKuNFU6PThizszN NFvndXlUSU6JRWK=
GI-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3QVI56UUN3ME2yMlE3ODh2IN88US=> MYnTRW5ITVJ?
SW962 NXn5TJZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTJwMUexO|gh|ryP MkXmV2FPT0WU
SW872 NXrXT3EzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlGxTWM2OD1{LkG4OVA4KM7:TR?= NYLNdXhwW0GQR1XS
NCI-H747 M4Phbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPvNHlTUUN3ME2yMlI2PzF2IN88US=> NYPRbWdMW0GQR1XS
MZ1-PC MkHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzORVZKSzVyPUKuNlk{PTZizszN NEDncIlUSU6JRWK=
MSTO-211H NV7neGhPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnaTWM2OD1{LkO1O|I{KM7:TR?= MoHLV2FPT0WU
BL-70 NHKzbIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33wPGlEPTB;Mj60O|QzOiEQvF2= NHPkUY1USU6JRWK=
SW954 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nsbmlEPTB;Mj61O|QxQCEQvF2= M37MPHNCVkeHUh?=
SNB75 NHf1UWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVG3eIFHUUN3ME2yMlY5PTl2IN88US=> MlTxV2FPT0WU
IST-SL2 MlTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDSdFltUUN3ME2yMlczOzd7IN88US=> MXLTRW5ITVJ?
GCIY Mm\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULVOXREUUN3ME2yMlg4ODB3IN88US=> MYjTRW5ITVJ?
KU812 M3fZbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnL4TWM2OD1|LkC1Nlk6KM7:TR?= MoL2V2FPT0WU
LXF-289 NEjWbXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjaTWM2OD1|LkGyNVA6KM7:TR?= M1zxTXNCVkeHUh?=
ETK-1 NVftNWxpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{O4e2lEPTB;Mz6yNFc3PyEQvF2= MUjTRW5ITVJ?
SF126 NXTRb2FKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTNwM{GxO|Qh|ryP Mki4V2FPT0WU
LC-2-ad MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTNwNUW3JO69VQ>? NWG2bllWW0GQR1XS
KNS-42 NHXUTVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PUV2lEPTB;Mz62OUDPxE1? NF3nSpFUSU6JRWK=
OVCAR-4 MlLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTNwN{O0N|Mh|ryP NI[zdFRUSU6JRWK=
PF-382 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjvNWh4UUN3ME2zMlg{Pjl6IN88US=> M4nJTXNCVkeHUh?=
SH-4 NVjpTJN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTRwMkWyOVkh|ryP NFzrPZVUSU6JRWK=
KM12 M4DHV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PZOWlEPTB;ND6zNlQyPiEQvF2= NXr5cZR1W0GQR1XS
NB5 Mom3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTRwNEG4OlQh|ryP NIrhbFFUSU6JRWK=
KURAMOCHI NGDIZ25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH23dlhKSzVyPUSuOlUzPTZizszN NYX0T|lXW0GQR1XS
Becker MnjtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknQTWM2OD12Lk[2OFE3KM7:TR?= MojFV2FPT0WU
MV-4-11 M1ey[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTRwOEGzOFQh|ryP NVz0S2VkW0GQR1XS
KINGS-1 MkXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\oTWM2OD12LkiyN|c{KM7:TR?= NF3iN4JUSU6JRWK=
LS-123 MoHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PXdmlEPTB;NT60PVY5PCEQvF2= NXXFOIJDW0GQR1XS
SF268 NF;PeGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHuTWM2OD13Lk[xNlYzKM7:TR?= NWOxVJlZW0GQR1XS
A388 NE\wRYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnmVZhKSzVyPUWuOlM3PjdizszN Mn;xV2FPT0WU
NMC-G1 M4K1Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGi0U29KSzVyPU[uNFE5OTFizszN MX\TRW5ITVJ?
CGTH-W-1 NHm0c5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDnTWM2OD14LkCyNFc2KM7:TR?= M4jh[XNCVkeHUh?=
ES4 MnLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TSO2lEPTB;Nj61N|A4PCEQvF2= M37vfnNCVkeHUh?=
SR MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{L6O2lEPTB;Nj61PFgxPyEQvF2= M1jyZ3NCVkeHUh?=
BB49-HNC MoDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nwSWlEPTB;Nj63N|IxPiEQvF2= MWDTRW5ITVJ?
KLE M1fEcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVn3WGFLUUN3ME22Mlc5Ozd5IN88US=> MXvTRW5ITVJ?
HUTU-80 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPyTWM2OD14Lkm4OFY3KM7:TR?= NF:wWmdUSU6JRWK=
SNU-C2B MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLLUVhKSzVyPUeuPFI4OzdizszN M4LYU3NCVkeHUh?=
BB65-RCC M4i4UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTdwOUS5NFQh|ryP M1zqNnNCVkeHUh?=
QIMR-WIL NHHZOYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXtPWNzUUN3ME24MlQzQDB6IN88US=> M{f6T3NCVkeHUh?=
GDM-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRThwOUeyPVIh|ryP NH71SnRUSU6JRWK=
LC4-1 M{PocWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTlwMEC5NVEh|ryP NUHKNVNGW0GQR1XS
MLMA MkL2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnryTWM2OD17LkG1NFA3KM7:TR?= NGLhOG9USU6JRWK=
EoL-1-cell MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjtTWM2OD17LkOwNVkzKM7:TR?= NEHHXZpUSU6JRWK=
BOKU M372TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTpTWM2OD17Lkm2OFY3KM7:TR?= MX;TRW5ITVJ?
EVSA-T MnjBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTlW4tHUUN3ME2xNE43PTZ6IN88US=> MoLHV2FPT0WU
D-283MED NFvrRmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTFyLkmxO|Yh|ryP NI\xXYhUSU6JRWK=
NB1 Mke2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHS0eGNKSzVyPUGxMlAzPDJizszN NVnjRoo6W0GQR1XS
RPMI-8402 NXfr[4lyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnrd4drUUN3ME2xNU4yPzhizszN MYLTRW5ITVJ?
NCI-H1355 NXHYRnRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXf5SGd1UUN3ME2xNU4yQDB4IN88US=> MVrTRW5ITVJ?
NB7 MnSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYSwRXlLUUN3ME2xNU4{Ojl5IN88US=> MmHlV2FPT0WU
RPMI-6666 MojDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITBbZpKSzVyPUGyMlk2PjdizszN NVvEXnpYW0GQR1XS
697 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrieohUUUN3ME2xN{4zPzBzIN88US=> MUjTRW5ITVJ?
CTB-1 M4fzSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jtUGlEPTB;MUOuOVk1QCEQvF2= NV3sd2hLW0GQR1XS
VA-ES-BJ NHnUOVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPEW4dCUUN3ME2xN{46OjN2IN88US=> NEHqelFUSU6JRWK=
BE-13 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVH3UIl4UUN3ME2xOE4{QTF3IN88US=> NXjxcVNIW0GQR1XS
SKM-1 MnjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rqc2lEPTB;MUSuOFQ6QSEQvF2= MXPTRW5ITVJ?
TE-6 NEfE[G1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHkWYF3UUN3ME2xOE44PTlzIN88US=> NHnKZWFUSU6JRWK=
LB771-HNC M13yTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\KTWM2OD1zND63PFk5KM7:TR?= MnLXV2FPT0WU
ECC4 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXqTWM2OD1zNz6wNlc4KM7:TR?= MlrBV2FPT0WU
ES3 NYjSRWJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;xTWM2OD1zNz60OlU2KM7:TR?= MnPCV2FPT0WU
LB647-SCLC Mn[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorCTWM2OD1zNz60PVQ6KM7:TR?= MYHTRW5ITVJ?
NB10 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTF6LkWyOVYh|ryP NF\nc|lUSU6JRWK=
L-540 M3LiZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTF6LkixNFkh|ryP MXvTRW5ITVJ?
NCI-H2126 M2Wwfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrYTWM2OD1zOT61NUDPxE1? NFey[XRUSU6JRWK=
HH M4nh[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjTTWM2OD1{MD6wNFk6KM7:TR?= M2fze3NCVkeHUh?=
MPP-89 MoX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljWTWM2OD1{Mz6yNlg6KM7:TR?= MkTOV2FPT0WU
IST-MEL1 MmnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfXZYxKSzVyPUKzMlg3PThizszN NHLnenpUSU6JRWK=
KP-N-YS NE[5SZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\JWIdKSzVyPUKzMlkzPTVizszN NEDufIZUSU6JRWK=
EC-GI-10 NGj5WVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrP[5RKSzVyPUK0MlU6QDlizszN MVrTRW5ITVJ?
EKVX MkX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIr4c4dKSzVyPUK2MlAzODNizszN Mmn5V2FPT0WU
TGBC1TKB NXq3XpJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzsUJVuUUN3ME2yOk41OzRizszN MX;TRW5ITVJ?
Daudi MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnxbohKSzVyPUK3MlA4PzNizszN NUfEOolHW0GQR1XS
ALL-PO M1LRS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrZPJVKSzVyPUK3MlA5OSEQvF2= M{PwZnNCVkeHUh?=
NB6 M2TFPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zzO2lEPTB;MkeuOFg5KM7:TR?= M1z1WHNCVkeHUh?=
ES6 Mo\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjJTWM2OD1{Nz65NVI{KM7:TR?= M3nyZnNCVkeHUh?=
COLO-320-HSR NFnMflZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlGwTWM2OD1{OD6wN|c{KM7:TR?= NHfnXZZUSU6JRWK=
K5 M3HVbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTJ6LkGyPFch|ryP NUPXVY1mW0GQR1XS
ES1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mme4TWM2OD1{OD63O|c{KM7:TR?= NV;4ZnZQW0GQR1XS
LC-1F M{X2NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\pVmNqUUN3ME2yPU44OzR4IN88US=> MmL4V2FPT0WU
SCLC-21H MlHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTNyLkezNVch|ryP MXnTRW5ITVJ?
SK-PN-DW MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGD0SlJKSzVyPUOyMlU2QThizszN NVTZTZhQW0GQR1XS
D-247MG NV;zUHE1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDDepN4UUN3ME2zNk46Pzd|IN88US=> NGfjdlNUSU6JRWK=
TE-5 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPrNmVKSzVyPUOzMlA{PjJizszN MoXGV2FPT0WU
MONO-MAC-6 M4XjXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2m4fWlEPTB;M{OuOVA1QCEQvF2= MUXTRW5ITVJ?
LB2518-MEL NInzWIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DycmlEPTB;M{OuO|Y3PiEQvF2= M2m0[XNCVkeHUh?=
LOXIMVI MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTN|Lke5Nlgh|ryP NW\BOmNnW0GQR1XS
NCI-H209 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETCSYNKSzVyPUO1MlE1PCEQvF2= M4DHTnNCVkeHUh?=
A253 M4LsS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\kVHlSUUN3ME2zOU44PDJ7IN88US=> NFjiclJUSU6JRWK=
HCC1599 NEjhWFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoeyTWM2OD1|Nj63NFU{KM7:TR?= NX70dGVtW0GQR1XS
EB-3 M4ryOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2npXWlEPTB;M{[uPVUyQCEQvF2= NYXtZVQ{W0GQR1XS
GOTO MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\4N2lEPTB;M{euN|IzPCEQvF2= MULTRW5ITVJ?
SW684 NG\LSVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXrTWM2OD12MT64OFk2KM7:TR?= M2HUSHNCVkeHUh?=
DEL M2DpcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTR{LkC1NlIh|ryP MX7TRW5ITVJ?
HT-144 NETiVZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjETWM2OD12Mj6xOlc3KM7:TR?= M{\zeHNCVkeHUh?=
TE-9 Mk\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1:3OGlEPTB;NEOuOFU6PiEQvF2= Mn\wV2FPT0WU
KARPAS-45 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDFdoZJUUN3ME20OE4{QTJ3IN88US=> Ml3PV2FPT0WU
HAL-01 M2rYcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\LTWM2OD12ND61NFM1KM7:TR?= NVvGbHlPW0GQR1XS
RCC10RGB MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3qzZmlEPTB;NESuO|M6OiEQvF2= M320TnNCVkeHUh?=
CP67-MEL NIjw[ZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjlTWM2OD12NT62NlQyKM7:TR?= MoPXV2FPT0WU
NB17 NEDOWGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIft[GpKSzVyPUS1MlY3PDNizszN MnywV2FPT0WU
SK-UT-1 MoW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoH6TWM2OD12NT65OFY1KM7:TR?= NE\KbnpUSU6JRWK=
JiyoyeP-2003 M3OwR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7Kb286UUN3ME20Ok4xOTF7IN88US=> MmLoV2FPT0WU
HCE-4 MoK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfK[WRKSzVyPUS2MlU6PjhizszN MmT3V2FPT0WU
NCI-H720 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XPc2lEPTB;NE[uO|Y5OiEQvF2= M3vrWHNCVkeHUh?=
KARPAS-422 NXLQVFZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTR5LkC4PVUh|ryP Mn[0V2FPT0WU
Ramos-2G6-4C10 Mor1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moj6TWM2OD12Nz6xOlIzKM7:TR?= MV7TRW5ITVJ?
HCE-T MnzLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDXTWM2OD12Nz62PFI5KM7:TR?= M3rD[XNCVkeHUh?=
PSN1 NXXCeYppT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGC4c5ZKSzVyPUS3Mlc5OTNizszN MXzTRW5ITVJ?

... Click to View More Cell Line Experimental Data

体内研究 Saracatinib作用于Src3T3异体移植物显示出强的肿瘤生长抑制率,且Saracatinib造成Calu-6, MDA-MB-231, AsPc-1和BT474C移植瘤生长适当延迟。[1]Saracatinib处理常位DU145鼠,按鼠体重,每千克每天口服处理25mg Saracatinib,结果显示出强的抗癌活性。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
+ 展开

激酶实验:

使用受体和非受体酪氨酸激酶的重组催化区,通过酶联免疫吸附法测定酪氨酸激酶活性的IC50值。加入的Saracatinib剂量从0.001到10 mM不等。针对丝氨酸/苏氨酸激酶的特定实验是加32P 的渗透捕捉实验。在加入10 μL 20mM Mg.ATP开始反应前,包含0.5 μL Saracatinib或DMSO(作对照) 或pH 3.0 buffer(作对照)的多支路384孔板加入15 μL酶和肽/蛋白底物温育5分钟。 所有酶的最终浓度都接近米氏常数(Km)。实验在室温下进行30分钟,然后加入5 μL正磷酸终止反应。混合后,孔中的内含物加到P81联合板上,使用正磷酸作为洗涤缓冲液,然后计算IC50值。
细胞实验:[2]
+ 展开
  • Cell lines: PC3, DU145, CWR22Rv1, LNCaP, LAPC-4, PZ-HPV7,和RWPE-1细胞
  • Concentrations: 62.5 nM-16 mM
  • Incubation Time: 1, 3,和5天
  • Method: PC3, DU145, CWR22Rv1, LNCaP, LAPC-4, PZ-HPV7 及RWPE-1细胞按2×103密度接种在96孔板上,温育过夜。加入浓度不等(62.5 nM-16 mM)的Saracatinib。1,3,5天后分离培养基,每孔加入0.2 mL DMSO,按每分钟200轮持续震荡96孔板15分钟。MTT实验测IC50值。
    (Only for Reference)
动物实验:[2]
+ 展开
  • Animal Models: 移植DU145细胞的CB17鼠
  • Formulation: 溶于0.5% 羟丙基甲基纤维素和0.1% Tween-80中
  • Dosages: 25 mg/kg
  • Administration: 每天口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 35 mg/mL warmed (64.57 mM)
Ethanol 31 mg/mL (57.19 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 542.03
化学式

C27H32ClN5O5

CAS号 379231-04-6
稳定性 powder
in solvent
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02955186 Recruiting Alcohol Drinking Yale University May 9 2017 Phase 2
NCT01216176 Completed Breast Cancer Joyce Marie Slingerland|Stanford University|University of Miami October 21 2008 Phase 1|Phase 2
NCT02737202 Recruiting Pulmonary Lymphangioleiomyomatosis Baylor College of Medicine|University of Cincinnati|Brigham and Women''s Hospital|Stanford University|Loyola University|University of South Florida|National Institutes of Health (NIH) April 2016 Phase 2
NCT02732587 Completed Alcohol Drinking Yale University|National Institute on Alcohol Abuse and Alcoholism (NIAAA) November 2015 Phase 1
NCT02167256 Completed Alzheimer''s Disease Yale University|Alzheimer''s Therapeutic Research Institute December 2014 Phase 2
NCT02262026 Recruiting Alcoholism Yale University November 2014 Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    What is the half-life of Saracatinib?

  • 回答:

    Based on the following paper, the half-life of Saracatinib in vivo is around 40hours and it reaches its peak lever around 2-4 hours after dosing: http://clincancerres.aacrjournals.org/content/16/19/4876.long

Src Signaling Pathway Map

Src Inhibitors with Unique Features

相关Src产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID