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 MnryS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\jTWM2OD1yLkC2NVQ{KM7:TR?= M1vDW3NCVkeHUh?=
LAMA-84 NIXRbHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zBWGlEPTB;MD6xOVk6KM7:TR?= M{L2WHNCVkeHUh?=
MEG-01 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2ezTGlEPTB;MD6yN|Y5QCEQvF2= NVWxd|lOW0GQR1XS
EM-2 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2L1TGlEPTB;MD6yOlUh|ryP MYjTRW5ITVJ?
TE-15 NGG3UVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LqNmlEPTB;MD6yO|QyOiEQvF2= MkfDV2FPT0WU
NCI-H1648 M{XTNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTBwMkixNVYh|ryP MW\TRW5ITVJ?
TE-12 M2HXXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XTVmlEPTB;MD6zNlY5KM7:TR?= NGjueGFUSU6JRWK=
LB996-RCC MlXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTBwNESxPVYh|ryP MWPTRW5ITVJ?
K-562 NUTMcFdRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTBwNES5Olch|ryP MlLGV2FPT0WU
D-336MG NWP6SnhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HDdWlEPTB;MD61NFMxPCEQvF2= MlO1V2FPT0WU
NOS-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjsZoFyUUN3ME2wMlYxPTJ7IN88US=> M2fy[XNCVkeHUh?=
EW-24 NYHH[29RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHu3W4dKSzVyPUCuOlI3QTNizszN NHHEXFFUSU6JRWK=
BV-173 NYKzOVdmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE[5V4FKSzVyPUCuOlUzPDlizszN NIXj[IhUSU6JRWK=
NCCIT NWH4VGJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPs[4tKSzVyPUCuO|MzOThizszN NEKyXo5USU6JRWK=
NCI-H1436 NHfsPGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jXW2lEPTB;MD63PVA1QSEQvF2= MYnTRW5ITVJ?
BB30-HNC NYSyTVhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHwV3NJUUN3ME2wMlg3OjB|IN88US=> MV7TRW5ITVJ?
TE-8 NFKxWXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUG0Z3JyUUN3ME2wMlg4Ojd3IN88US=> M{LqNXNCVkeHUh?=
A704 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TLNmlEPTB;MD64PVIyKM7:TR?= Mn\uV2FPT0WU
TK10 NVHMV4w1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfYTWM2OD1yLkmwOlY6KM7:TR?= MXPTRW5ITVJ?
KS-1 NGrEVGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37V[2lEPTB;MT6xPVc4QSEQvF2= NEm3WIlUSU6JRWK=
C2BBe1 MkXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTFwMkC1NFch|ryP M2P4R3NCVkeHUh?=
RXF393 M3fvXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrQTWM2OD1zLkK0N|Yh|ryP NXzKPINzW0GQR1XS
KGN MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTFwMke2PFch|ryP Mk[yV2FPT0WU
NB69 M{XiVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTiTWM2OD1zLkO3OFk4KM7:TR?= NYTlN3Q4W0GQR1XS
TE-11 M3TwSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTFwNEO0NVgh|ryP NVvNV5JGW0GQR1XS
TE-1 NX;pZ203T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XSZmlEPTB;MT60OFExPSEQvF2= M3H0ZXNCVkeHUh?=
ST486 M2rJNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;Jb2tiUUN3ME2xMlQ2QDV{IN88US=> M{j4S3NCVkeHUh?=
HOP-62 MknXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPnW283UUN3ME2xMlUxOjR4IN88US=> NVXNdXVpW0GQR1XS
EW-16 M131SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU[3PJBTUUN3ME2xMlU2ODh|IN88US=> M4j6fnNCVkeHUh?=
LB1047-RCC NWPNTFhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HnWWlEPTB;MT61OVQ2OyEQvF2= NX7me|FKW0GQR1XS
TE-10 MnTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPmd5FKSzVyPUGuOlYzPTJizszN M3LYVXNCVkeHUh?=
RL95-2 M3v1eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTFwNk[5NFIh|ryP NIXEeIJUSU6JRWK=
DOHH-2 MmHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnP5TWM2OD1zLkexO|gzKM7:TR?= MmLkV2FPT0WU
MFH-ino M2L3PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXG0fWZNUUN3ME2xMlc4QDdizszN MUjTRW5ITVJ?
GB-1 MnLiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfTTWM2OD1zLke5PFM{KM7:TR?= MkjaV2FPT0WU
SK-N-DZ M{Dacmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzCTWM2OD1zLki0Olg5KM7:TR?= NIrOTlJUSU6JRWK=
OS-RC-2 NHXoZWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjhTWM2OD1zLki4OVc1KM7:TR?= MlrNV2FPT0WU
SW982 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jWPGlEPTB;MT65NlA6OyEQvF2= NVjacVN7W0GQR1XS
KALS-1 NGTiS4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TxSGlEPTB;MT65PFczOiEQvF2= MVjTRW5ITVJ?
TGBC24TKB M362Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mly4TWM2OD1{LkC1PVU5KM7:TR?= NU\NOGZCW0GQR1XS
GI-1 M2fFRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLjTWM2OD1{LkG2NFg1KM7:TR?= NX7XOFZ[W0GQR1XS
SW962 M4fxb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPhR2NKSzVyPUKuNVcyPzhizszN MXXTRW5ITVJ?
SW872 M17NPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTJwMUi1NFch|ryP NWDTbI43W0GQR1XS
NCI-H747 NITWSpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\xTWM2OD1{LkK1O|E1KM7:TR?= MlTrV2FPT0WU
MZ1-PC MlfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFew[|lKSzVyPUKuNlk{PTZizszN MlzrV2FPT0WU
MSTO-211H MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDITWM2OD1{LkO1O|I{KM7:TR?= NFm2VVFUSU6JRWK=
BL-70 M124bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlu2TWM2OD1{LkS3OFIzKM7:TR?= NWHFbHhNW0GQR1XS
SW954 MlHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\oTWM2OD1{LkW3OFA5KM7:TR?= M1LuPHNCVkeHUh?=
SNB75 NF3SVnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\vb5JrUUN3ME2yMlY5PTl2IN88US=> M{fQNnNCVkeHUh?=
IST-SL2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3:3bmlEPTB;Mj63NlM4QSEQvF2= MW\TRW5ITVJ?
GCIY MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTJwOEewNFUh|ryP MnTaV2FPT0WU
KU812 M1X6OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW[3bHpQUUN3ME2zMlA2Ojl7IN88US=> NVnS[pZPW0GQR1XS
LXF-289 M17zemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTNwMUKxNFkh|ryP NVTqR2VQW0GQR1XS
ETK-1 NUGxZ|FuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTNwMkC3Olch|ryP NXnneHRNW0GQR1XS
SF126 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHS5UnZKSzVyPUOuN|EyPzRizszN M{j2fnNCVkeHUh?=
LC-2-ad Mn;0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rmRWlEPTB;Mz61OVch|ryP Mmq3V2FPT0WU
KNS-42 NUjJW|N2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Xq[mlEPTB;Mz62OUDPxE1? MnO1V2FPT0WU
OVCAR-4 NWD4ZYdGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XvNGlEPTB;Mz63N|Q{OyEQvF2= M{C5eXNCVkeHUh?=
PF-382 NGC0O3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlX3TWM2OD1|LkizOlk5KM7:TR?= MnruV2FPT0WU
SH-4 Mn3HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoP1TWM2OD12LkK1NlU6KM7:TR?= NWXnNoRRW0GQR1XS
KM12 MoHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;ITWM2OD12LkOyOFE3KM7:TR?= NGPJOGVUSU6JRWK=
NB5 NWL6NZpMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHIPHpSUUN3ME20MlQyQDZ2IN88US=> M4fuZnNCVkeHUh?=
KURAMOCHI NHLvNlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTSRoREUUN3ME20MlY2OjV4IN88US=> MoP6V2FPT0WU
Becker NHS3WXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rGb2lEPTB;ND62OlQyPiEQvF2= M4L2NnNCVkeHUh?=
MV-4-11 MkTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYH6XXFWUUN3ME20MlgyOzR2IN88US=> M3TvWXNCVkeHUh?=
KINGS-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfoO5NEUUN3ME20MlgzOzd|IN88US=> M4S4VXNCVkeHUh?=
LS-123 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnle5Y2UUN3ME21MlQ6Pjh2IN88US=> M37C[HNCVkeHUh?=
SF268 NFvkTHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4O1TmlEPTB;NT62NVI3OiEQvF2= MmjPV2FPT0WU
A388 M2LhVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHvTWM2OD13Lk[zOlY4KM7:TR?= Mn7xV2FPT0WU
NMC-G1 NIjhTI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWj1[XVOUUN3ME22MlAyQDFzIN88US=> MXjTRW5ITVJ?
CGTH-W-1 NH;ZUHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTZwMEKwO|Uh|ryP Mof6V2FPT0WU
ES4 M4rrTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTafYhOUUN3ME22MlU{ODd2IN88US=> NH72TZJUSU6JRWK=
SR M{fXVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Moj6TWM2OD14LkW4PFA4KM7:TR?= NFrNSJlUSU6JRWK=
BB49-HNC MnnnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTZwN{OyNFYh|ryP NHHvc2NUSU6JRWK=
KLE NWDnNlVOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTZwN{izO|ch|ryP NISxeXBUSU6JRWK=
HUTU-80 Mki1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vwdmlEPTB;Nj65PFQ3PiEQvF2= MWTTRW5ITVJ?
SNU-C2B NGDlVJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TPeWlEPTB;Nz64Nlc{PyEQvF2= M2qzSnNCVkeHUh?=
BB65-RCC M4\0WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\GTWM2OD15Lkm0PVA1KM7:TR?= MoHFV2FPT0WU
QIMR-WIL NVXuTmlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRThwNEK4NFgh|ryP M1TvTnNCVkeHUh?=
GDM-1 NGfybopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlyxTWM2OD16Lkm3NlkzKM7:TR?= MlrFV2FPT0WU
LC4-1 NWPycWtDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[4TWM2OD17LkCwPVEyKM7:TR?= MnHzV2FPT0WU
MLMA M37MVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TiZ2lEPTB;OT6xOVAxPiEQvF2= MV3TRW5ITVJ?
EoL-1-cell NYXObXcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\tTWM2OD17LkOwNVkzKM7:TR?= NI\NcnVUSU6JRWK=
BOKU M3S1O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfWTWM2OD17Lkm2OFY3KM7:TR?= MVnTRW5ITVJ?
EVSA-T M2[wWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1n3emlEPTB;MUCuOlU3QCEQvF2= NYPtNVh{W0GQR1XS
D-283MED NUTqWYhkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7KVYM1UUN3ME2xNE46OTd4IN88US=> NVv4RodrW0GQR1XS
NB1 NYfBcGo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2X4S2lEPTB;MUGuNFI1OiEQvF2= MUfTRW5ITVJ?
RPMI-8402 M{\INGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjoTWM2OD1zMT6xO|gh|ryP Mn;EV2FPT0WU
NCI-H1355 NVu0XVFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlq1TWM2OD1zMT6xPFA3KM7:TR?= NWfse5lwW0GQR1XS
NB7 NFzCZYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTFzLkOyPVch|ryP MUnTRW5ITVJ?
RPMI-6666 NH7LN3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTF{Lkm1Olch|ryP NGrVOZZUSU6JRWK=
697 MnXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIWxdoJKSzVyPUGzMlI4ODFizszN NX[wfW9YW0GQR1XS
CTB-1 NUDqfYxRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnETWM2OD1zMz61PVQ5KM7:TR?= NVLQV2FmW0GQR1XS
VA-ES-BJ MnzDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTF|LkmyN|Qh|ryP NIG0O|ZUSU6JRWK=
BE-13 NEju[VZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTF2LkO5NVUh|ryP NHrWXmpUSU6JRWK=
SKM-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPyTWM2OD1zND60OFk6KM7:TR?= M4HGXHNCVkeHUh?=
TE-6 M1myU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2O0XmlEPTB;MUSuO|U6OSEQvF2= MXnTRW5ITVJ?
LB771-HNC NEDHV|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTF2Lke4PVgh|ryP M4\QXHNCVkeHUh?=
ECC4 NGmwcYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGOz[GdKSzVyPUG3MlAzPzdizszN NYj4U5FKW0GQR1XS
ES3 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTF5LkS2OVUh|ryP MlPaV2FPT0WU
LB647-SCLC M3PQPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NViyUoZOUUN3ME2xO{41QTR7IN88US=> MVLTRW5ITVJ?
NB10 MlmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\yTWM2OD1zOD61NlU3KM7:TR?= M3HqRnNCVkeHUh?=
L-540 NYrXVlhkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTF6LkixNFkh|ryP MmHlV2FPT0WU
NCI-H2126 NYeyVXBPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4D5WWlEPTB;MUmuOVEh|ryP MkHnV2FPT0WU
HH NXvRbFIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\0TWM2OD1{MD6wNFk6KM7:TR?= M2LwRXNCVkeHUh?=
MPP-89 NHLxSnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHlbG1ZUUN3ME2yN{4zOjh7IN88US=> NEXueIpUSU6JRWK=
IST-MEL1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTJ|Lki2OVgh|ryP M1;OeXNCVkeHUh?=
KP-N-YS NW\pVWZHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDpNpozUUN3ME2yN{46OjV3IN88US=> NXm4SnFrW0GQR1XS
EC-GI-10 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTJ2LkW5PFkh|ryP MlfZV2FPT0WU
EKVX M2ThNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fF[2lEPTB;Mk[uNFIxOyEQvF2= MoC0V2FPT0WU
TGBC1TKB NWjkdnc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XuRWlEPTB;Mk[uOFM1KM7:TR?= M4S5XnNCVkeHUh?=
Daudi NVnoUpNuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTJ5LkC3O|Mh|ryP MnLDV2FPT0WU
ALL-PO M1G1XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnuwTWM2OD1{Nz6wPFEh|ryP MVfTRW5ITVJ?
NB6 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTJ5LkS4PEDPxE1? M4jsU3NCVkeHUh?=
ES6 NVq2ZZRFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoS1TWM2OD1{Nz65NVI{KM7:TR?= MnPLV2FPT0WU
COLO-320-HSR MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGD1[|JKSzVyPUK4MlA{PzNizszN MU\TRW5ITVJ?
K5 MojWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjETIJZUUN3ME2yPE4yOjh5IN88US=> MkHCV2FPT0WU
ES1 NEjpZVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnriTWM2OD1{OD63O|c{KM7:TR?= M2P2cnNCVkeHUh?=
LC-1F MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTJ7LkezOFYh|ryP M3rqVHNCVkeHUh?=
SCLC-21H NH33S2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTNyLkezNVch|ryP M3S2OnNCVkeHUh?=
SK-PN-DW MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUX0cYpoUUN3ME2zNk42PTl6IN88US=> NEPQdVZUSU6JRWK=
D-247MG MlvpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LBfGlEPTB;M{KuPVc4OyEQvF2= NYDUVWp3W0GQR1XS
TE-5 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHNPXRKSzVyPUOzMlA{PjJizszN NIPmeFFUSU6JRWK=
MONO-MAC-6 M1Lsc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvkTFFKSzVyPUOzMlUxPDhizszN NUW3c|RrW0GQR1XS
LB2518-MEL NGWxV|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;GbWt4UUN3ME2zN{44PjZ4IN88US=> M1fzVnNCVkeHUh?=
LOXIMVI M2e3bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3i4ZWlEPTB;M{OuO|kzQCEQvF2= MYTTRW5ITVJ?
NCI-H209 M2HNXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mke5TWM2OD1|NT6xOFQh|ryP Mn\BV2FPT0WU
A253 NXzPOVBNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTN3Lke0Nlkh|ryP MVzTRW5ITVJ?
HCC1599 Mn22S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfuNGc6UUN3ME2zOk44ODV|IN88US=> M1vYT3NCVkeHUh?=
EB-3 M2XRTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\UOWo1UUN3ME2zOk46PTF6IN88US=> MUjTRW5ITVJ?
GOTO MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTN5LkOyNlQh|ryP NUf4bVg3W0GQR1XS
SW684 NXnsNGV{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDpPY5KSzVyPUSxMlg1QTVizszN MX7TRW5ITVJ?
DEL MnjOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\ITWM2OD12Mj6wOVIzKM7:TR?= M1fGcHNCVkeHUh?=
HT-144 M3j5OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmP3TWM2OD12Mj6xOlc3KM7:TR?= NIjnTVJUSU6JRWK=
TE-9 NEfKXGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTR|LkS1PVYh|ryP NFXSUGJUSU6JRWK=
KARPAS-45 NHnhXG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjOWZBKSzVyPUS0MlM6OjVizszN NHXEcohUSU6JRWK=
HAL-01 MkHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmX0TWM2OD12ND61NFM1KM7:TR?= NWL6WZBTW0GQR1XS
RCC10RGB NFf5O5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XsRmlEPTB;NESuO|M6OiEQvF2= M3zSNHNCVkeHUh?=
CP67-MEL NFnpVYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTR3Lk[yOFEh|ryP M1LaenNCVkeHUh?=
NB17 M{CySWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTR3Lk[2OFMh|ryP M{jWWXNCVkeHUh?=
SK-UT-1 NGDz[lRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPG[2xKSzVyPUS1Mlk1PjRizszN NWrsbYt7W0GQR1XS
JiyoyeP-2003 M1G1Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1flXGlEPTB;NE[uNFEyQSEQvF2= M{XZOnNCVkeHUh?=
HCE-4 Mn[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rJSGlEPTB;NE[uOVk3QCEQvF2= NUHKbWZWW0GQR1XS
NCI-H720 NX;vUpJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTR4Lke2PFIh|ryP M4jvS3NCVkeHUh?=
KARPAS-422 NE\0PFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;0R5pKSzVyPUS3MlA5QTVizszN M1jSUHNCVkeHUh?=
Ramos-2G6-4C10 MoHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\JR2FNUUN3ME20O{4yPjJ{IN88US=> M3ezPXNCVkeHUh?=
HCE-T M4rPXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfPOGdKSzVyPUS3MlY5OjhizszN NGHJPJdUSU6JRWK=
PSN1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTR5Lke4NVMh|ryP MmX2V2FPT0WU

... 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:
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
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 Not yet recruiting Alcohol Drinking Yale University January 2017 Phase 2
NCT02737202 Recruiting Pulmonary Lymphangioleiomyomatosis Baylor College of Medicine|University of Cincinnati|Brigham and Womens Hospital|Stanford University|Loyola University|University of South Florida|National Institutes of Health (NIH) April 2016 Phase 2
NCT02732587 Active, not recruiting Alcohol Drinking Yale University|National Institute on Alcohol Abuse and Alcoholism (NIAAA) November 2015 Phase 1
NCT02167256 Active, not recruiting Alzheimers Disease Yale University|Alzheimers Therapeutic Research Institute December 2014 Phase 2
NCT02262026 Recruiting Alcoholism Yale University November 2014 Phase 1
NCT02116712 Completed Pulmonary Lymphangioleiomyomatosis Tony Eissa|University of Texas|University of Cincinnati|Baylor College of Medicine August 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

Related Antibodies

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