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 NV7MdWZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTBwME[xOFMh|ryP NIfzTHZUSU6JRWK=
LAMA-84 M{niZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnrdplxUUN3ME2wMlE2QTlizszN MUfTRW5ITVJ?
MEG-01 MlH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrudmtiUUN3ME2wMlI{Pjh6IN88US=> MVHTRW5ITVJ?
EM-2 MlzHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoC2TWM2OD1yLkK2OUDPxE1? MnS0V2FPT0WU
TE-15 M3T2NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3nTWM2OD1yLkK3OFEzKM7:TR?= NX\TVFV[W0GQR1XS
NCI-H1648 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTBwMkixNVYh|ryP NWPLbWQ3W0GQR1XS
TE-12 Mm\OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\xWnZKSzVyPUCuN|I3QCEQvF2= MUPTRW5ITVJ?
LB996-RCC MlrzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjNTWM2OD1yLkS0NVk3KM7:TR?= NXHzPHhpW0GQR1XS
K-562 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPjTWM2OD1yLkS0PVY4KM7:TR?= NGfLU3pUSU6JRWK=
D-336MG MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHVTWM2OD1yLkWwN|A1KM7:TR?= M13acnNCVkeHUh?=
NOS-1 NIrNZXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmH5TWM2OD1yLk[wOVI6KM7:TR?= MWfTRW5ITVJ?
EW-24 NIDhXphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjQN|dKSzVyPUCuOlI3QTNizszN NVnUWZdYW0GQR1XS
BV-173 M1X4b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTBwNkWyOFkh|ryP NUDBR4dYW0GQR1XS
NCCIT MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XJWWlEPTB;MD63N|IyQCEQvF2= NW[xemxoW0GQR1XS
NCI-H1436 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmn4TWM2OD1yLke5NFQ6KM7:TR?= MY\TRW5ITVJ?
BB30-HNC MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLWPFVZUUN3ME2wMlg3OjB|IN88US=> NY\NSFdzW0GQR1XS
TE-8 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PvS2lEPTB;MD64O|I4PSEQvF2= NHW4N3VUSU6JRWK=
A704 MlOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vSTmlEPTB;MD64PVIyKM7:TR?= NH3zRlJUSU6JRWK=
TK10 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjVRWFKSzVyPUCuPVA3PjlizszN Mni4V2FPT0WU
KS-1 NYq5WXJvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnUUYxWUUN3ME2xMlE6Pzd7IN88US=> Mny4V2FPT0WU
C2BBe1 NGTmN2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zFU2lEPTB;MT6yNFUxPyEQvF2= MXTTRW5ITVJ?
RXF393 NFHhVW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlWxTWM2OD1zLkK0N|Yh|ryP NHHUWVhUSU6JRWK=
KGN NE\tXXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjNd3p3UUN3ME2xMlI4Pjh5IN88US=> M3zLVnNCVkeHUh?=
NB69 MnLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXPTWM2OD1zLkO3OFk4KM7:TR?= MUPTRW5ITVJ?
TE-11 MmfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTFwNEO0NVgh|ryP MU\TRW5ITVJ?
TE-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jLcWlEPTB;MT60OFExPSEQvF2= NV;JNHh7W0GQR1XS
ST486 M1jRdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PSTGlEPTB;MT60OVg2OiEQvF2= M3XPdHNCVkeHUh?=
HOP-62 NGTsZpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTFwNUCyOFYh|ryP M4XDPHNCVkeHUh?=
EW-16 NYrKUJI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXyzbJFRUUN3ME2xMlU2ODh|IN88US=> MVvTRW5ITVJ?
LB1047-RCC MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEj1PZdKSzVyPUGuOVU1PTNizszN MWnTRW5ITVJ?
TE-10 M{D3TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInYbnRKSzVyPUGuOlYzPTJizszN MXzTRW5ITVJ?
RL95-2 MmfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTFwNk[5NFIh|ryP M{H4fHNCVkeHUh?=
DOHH-2 NU\BXodiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TsW2lEPTB;MT63NVc5OiEQvF2= NVeyTlVnW0GQR1XS
MFH-ino M2jGUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXu2dWw4UUN3ME2xMlc4QDdizszN MkjjV2FPT0WU
GB-1 M37nemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{C5fGlEPTB;MT63PVg{OyEQvF2= M{XlWXNCVkeHUh?=
SK-N-DZ NYP3NnN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TDd2lEPTB;MT64OFY5QCEQvF2= Mor2V2FPT0WU
OS-RC-2 MmLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzUUWdKSzVyPUGuPFg2PzRizszN MmPhV2FPT0WU
SW982 M4XwcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\tUGRQUUN3ME2xMlkzODl|IN88US=> M3TZU3NCVkeHUh?=
KALS-1 MoXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHlTWJEUUN3ME2xMlk5PzJ{IN88US=> MWjTRW5ITVJ?
TGBC24TKB MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTJwMEW5OVgh|ryP M2rrdnNCVkeHUh?=
GI-1 MoHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknPTWM2OD1{LkG2NFg1KM7:TR?= NWr4W2V{W0GQR1XS
SW962 NHLRTGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDLPWpKSzVyPUKuNVcyPzhizszN NUfhfng{W0GQR1XS
SW872 NHTnO3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2D5b2lEPTB;Mj6xPFUxPyEQvF2= MYjTRW5ITVJ?
NCI-H747 NY\qcFZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;zRmlEPTB;Mj6yOVcyPCEQvF2= NEHle29USU6JRWK=
MZ1-PC M2HuS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXaTGFKSzVyPUKuNlk{PTZizszN M{jrVXNCVkeHUh?=
MSTO-211H NFi4OGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTJwM{W3NlMh|ryP MV;TRW5ITVJ?
BL-70 MlzyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojWTWM2OD1{LkS3OFIzKM7:TR?= M{TmWnNCVkeHUh?=
SW954 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnKVXRKSzVyPUKuOVc1ODhizszN NHr2TmxUSU6JRWK=
SNB75 NGjmdWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\yPGlEPTB;Mj62PFU6PCEQvF2= NGXoTmlUSU6JRWK=
IST-SL2 M1niNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\ZTWM2OD1{LkeyN|c6KM7:TR?= NE\LbXFUSU6JRWK=
GCIY M1TJfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWe1bXJ1UUN3ME2yMlg4ODB3IN88US=> M1nzfnNCVkeHUh?=
KU812 NEPaO2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorJTWM2OD1|LkC1Nlk6KM7:TR?= MYDTRW5ITVJ?
LXF-289 NH32cVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M136S2lEPTB;Mz6xNlExQSEQvF2= MXjTRW5ITVJ?
ETK-1 NETIe2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7QTWM2OD1|LkKwO|Y4KM7:TR?= M2jqR3NCVkeHUh?=
SF126 NFSzTlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTNwM{GxO|Qh|ryP NGm4Zm9USU6JRWK=
LC-2-ad NI\2ZZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HlPWlEPTB;Mz61OVch|ryP NVS4TotqW0GQR1XS
KNS-42 NHzNTpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1[2PWlEPTB;Mz62OUDPxE1? NWnCW3I3W0GQR1XS
OVCAR-4 NEXtbnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPhfHJKSzVyPUOuO|M1OzNizszN MlzmV2FPT0WU
PF-382 MmnYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\4TWM2OD1|LkizOlk5KM7:TR?= NVrLPGxMW0GQR1XS
SH-4 NX7E[Fh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fyeWlEPTB;ND6yOVI2QSEQvF2= NEjuSFZUSU6JRWK=
KM12 NIfQWXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fKTWlEPTB;ND6zNlQyPiEQvF2= NFHXdopUSU6JRWK=
NB5 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHQV|VGUUN3ME20MlQyQDZ2IN88US=> NWHvS3cxW0GQR1XS
KURAMOCHI MmTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjzS4J2UUN3ME20MlY2OjV4IN88US=> Ml;EV2FPT0WU
Becker MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPhRnhKSzVyPUSuOlY1OTZizszN M{TNcnNCVkeHUh?=
MV-4-11 Mke5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjOe2JzUUN3ME20MlgyOzR2IN88US=> NES2XZhUSU6JRWK=
KINGS-1 NEPmS2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmH0TWM2OD12LkiyN|c{KM7:TR?= M3y3N3NCVkeHUh?=
LS-123 MlTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4j0OGlEPTB;NT60PVY5PCEQvF2= M{LGe3NCVkeHUh?=
SF268 M3;5Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTVwNkGyOlIh|ryP MU\TRW5ITVJ?
A388 MmX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjRZmxKSzVyPUWuOlM3PjdizszN MYLTRW5ITVJ?
NMC-G1 M3LCNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPFOVBKSzVyPU[uNFE5OTFizszN MW\TRW5ITVJ?
CGTH-W-1 NWLlW41OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Lkb2lEPTB;Nj6wNlA4PSEQvF2= NHTIfGRUSU6JRWK=
ES4 NIHpSJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnv1TWM2OD14LkWzNFc1KM7:TR?= Ml3EV2FPT0WU
SR MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITo[4NKSzVyPU[uOVg5ODdizszN MlXYV2FPT0WU
BB49-HNC M{nNdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TOXmlEPTB;Nj63N|IxPiEQvF2= NWLRNGE1W0GQR1XS
KLE NYTIZYRxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\Rfpk1UUN3ME22Mlc5Ozd5IN88US=> M4XwbnNCVkeHUh?=
HUTU-80 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjEWph3UUN3ME22Mlk5PDZ4IN88US=> MVnTRW5ITVJ?
SNU-C2B NELHTmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjQW|hPUUN3ME23MlgzPzN5IN88US=> MlnGV2FPT0WU
BB65-RCC Mni0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULLO3JiUUN3ME23Mlk1QTB2IN88US=> MUHTRW5ITVJ?
QIMR-WIL NVrLendxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPpOIJKSzVyPUiuOFI5ODhizszN M3L3V3NCVkeHUh?=
GDM-1 MmH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRThwOUeyPVIh|ryP NF7pd2tUSU6JRWK=
LC4-1 NX62c5pMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfHTYk1UUN3ME25MlAxQTFzIN88US=> M3jTdnNCVkeHUh?=
MLMA MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{Lle2lEPTB;OT6xOVAxPiEQvF2= Ml\hV2FPT0WU
EoL-1-cell NVLpTIFpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDheGw1UUN3ME25MlMxOTl{IN88US=> MVfTRW5ITVJ?
BOKU NILK[VNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LSSGlEPTB;OT65OlQ3PiEQvF2= MXrTRW5ITVJ?
EVSA-T M4jhXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLueVBKSzVyPUGwMlY2PjhizszN M2TNOXNCVkeHUh?=
D-283MED NYfvdZBuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\RTZFUUUN3ME2xNE46OTd4IN88US=> MljZV2FPT0WU
NB1 NWrrZplkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEG4W2tKSzVyPUGxMlAzPDJizszN MVLTRW5ITVJ?
RPMI-8402 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXGU5pKSzVyPUGxMlE4QCEQvF2= NU\WeXFZW0GQR1XS
NCI-H1355 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjhWlNvUUN3ME2xNU4yQDB4IN88US=> MVfTRW5ITVJ?
NB7 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2L2UmlEPTB;MUGuN|I6PyEQvF2= MXvTRW5ITVJ?
RPMI-6666 M2jyRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7YUIVKSzVyPUGyMlk2PjdizszN NWrVSldDW0GQR1XS
697 M1vabmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTF|LkK3NFEh|ryP MW\TRW5ITVJ?
CTB-1 MnnQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknDTWM2OD1zMz61PVQ5KM7:TR?= NYjkOW9oW0GQR1XS
VA-ES-BJ NWXlOmE{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojMTWM2OD1zMz65NlM1KM7:TR?= MV3TRW5ITVJ?
BE-13 MnXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUCyd4FWUUN3ME2xOE4{QTF3IN88US=> NF7PVWxUSU6JRWK=
SKM-1 MlS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTF2LkS0PVkh|ryP NXT3cmJ1W0GQR1XS
TE-6 MofpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTF2Lke1PVEh|ryP MV7TRW5ITVJ?
LB771-HNC MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH:5UmNKSzVyPUG0Mlc5QThizszN NFLiVG1USU6JRWK=
ECC4 M4m1Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2raSWlEPTB;MUeuNFI4PyEQvF2= NVr2clFGW0GQR1XS
ES3 NVXnZYlCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGT2OmtKSzVyPUG3MlQ3PTVizszN M{LuRXNCVkeHUh?=
LB647-SCLC M{LqW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDHNoZ6UUN3ME2xO{41QTR7IN88US=> MXzTRW5ITVJ?
NB10 MoDjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlj3TWM2OD1zOD61NlU3KM7:TR?= NEW5fIdUSU6JRWK=
L-540 NWHzZ|FDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTF6LkixNFkh|ryP MnfSV2FPT0WU
NCI-H2126 NXTEO4JuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTF7LkWxJO69VQ>? MlPjV2FPT0WU
HH M2e5Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DQeWlEPTB;MkCuNFA6QSEQvF2= Mkf3V2FPT0WU
MPP-89 NIfvOY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TBfGlEPTB;MkOuNlI5QSEQvF2= MlrYV2FPT0WU
IST-MEL1 MoK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zMdGlEPTB;MkOuPFY2QCEQvF2= Mo\pV2FPT0WU
KP-N-YS NVLuPW43T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3sTWM2OD1{Mz65NlU2KM7:TR?= NW\GTG5QW0GQR1XS
EC-GI-10 NGX2XnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTJ2LkW5PFkh|ryP M3zLNHNCVkeHUh?=
EKVX NE\MO5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTzWHFKSzVyPUK2MlAzODNizszN NH3ROotUSU6JRWK=
TGBC1TKB M3P0NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnGWpRKSzVyPUK2MlQ{PCEQvF2= MkjNV2FPT0WU
Daudi M1nKUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXvXW92UUN3ME2yO{4xPzd|IN88US=> M1PaR3NCVkeHUh?=
ALL-PO Mmr1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTJ5LkC4NUDPxE1? MWPTRW5ITVJ?
NB6 NWDPcGtzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTJ5LkS4PEDPxE1? MoHRV2FPT0WU
ES6 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTJ5LkmxNlMh|ryP MnHxV2FPT0WU
COLO-320-HSR NVT5blMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVO3eWRwUUN3ME2yPE4xOzd|IN88US=> M2PafnNCVkeHUh?=
K5 NFi2WGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTJ6LkGyPFch|ryP M2\VXXNCVkeHUh?=
ES1 M2j4ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfCTWM2OD1{OD63O|c{KM7:TR?= Mmi5V2FPT0WU
LC-1F MmjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfoTWM2OD1{OT63N|Q3KM7:TR?= MXPTRW5ITVJ?
SCLC-21H NX64epcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHxTWM2OD1|MD63N|E4KM7:TR?= NWfMXoU{W0GQR1XS
SK-PN-DW M1G3eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HKVWlEPTB;M{KuOVU6QCEQvF2= NIS3[WFUSU6JRWK=
D-247MG NHjSboZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIC0OFVKSzVyPUOyMlk4PzNizszN NFPue|RUSU6JRWK=
TE-5 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkT0TWM2OD1|Mz6wN|YzKM7:TR?= NYPCVZRTW0GQR1XS
MONO-MAC-6 NHL3Z|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3z6XWlEPTB;M{OuOVA1QCEQvF2= NHfFcZJUSU6JRWK=
LB2518-MEL MoHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\LbolMUUN3ME2zN{44PjZ4IN88US=> NF3ZR5NUSU6JRWK=
LOXIMVI MmnHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPo[2IyUUN3ME2zN{44QTJ6IN88US=> MUHTRW5ITVJ?
NCI-H209 M{T5S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofBTWM2OD1|NT6xOFQh|ryP MWDTRW5ITVJ?
A253 M{Lhe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXiU|BKSzVyPUO1Mlc1OjlizszN M1j4eXNCVkeHUh?=
HCC1599 NGfFWVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTN4LkewOVMh|ryP MWLTRW5ITVJ?
EB-3 Mmj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DLOGlEPTB;M{[uPVUyQCEQvF2= NXjaPWcxW0GQR1XS
GOTO MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfSTWM2OD1|Nz6zNlI1KM7:TR?= NWLCOoFTW0GQR1XS
SW684 NH3XRnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfVTWM2OD12MT64OFk2KM7:TR?= NX7RRnFkW0GQR1XS
DEL NEjsV|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\DSldtUUN3ME20Nk4xPTJ{IN88US=> NVPxb|k3W0GQR1XS
HT-144 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzLTWM2OD12Mj6xOlc3KM7:TR?= MY\TRW5ITVJ?
TE-9 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfBdmg6UUN3ME20N{41PTl4IN88US=> NUnTe2Q5W0GQR1XS
KARPAS-45 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWi2d2d{UUN3ME20OE4{QTJ3IN88US=> MXPTRW5ITVJ?
HAL-01 M{[1bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDhdmJKSzVyPUS0MlUxOzRizszN MVnTRW5ITVJ?
RCC10RGB M3v4V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTR2LkezPVIh|ryP MVLTRW5ITVJ?
CP67-MEL Mn;nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nCNmlEPTB;NEWuOlI1OSEQvF2= MmL1V2FPT0WU
NB17 M2DkS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnz0TWM2OD12NT62OlQ{KM7:TR?= M1LJdXNCVkeHUh?=
SK-UT-1 M4XN[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELFRmJKSzVyPUS1Mlk1PjRizszN NYnJW|VjW0GQR1XS
JiyoyeP-2003 NV\oNGRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPFTJVKSzVyPUS2MlAyOTlizszN M4LKR3NCVkeHUh?=
HCE-4 NWDxbWl{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPNR5ZKSzVyPUS2MlU6PjhizszN M1zFRXNCVkeHUh?=
NCI-H720 NETnXW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHuzS5VKSzVyPUS2Mlc3QDJizszN MmS0V2FPT0WU
KARPAS-422 M2GwXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXoZ4FlUUN3ME20O{4xQDl3IN88US=> MoSwV2FPT0WU
Ramos-2G6-4C10 NH;NboRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fsOmlEPTB;NEeuNVYzOiEQvF2= NEf5cWFUSU6JRWK=
HCE-T NV:2XlNtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1q3PGlEPTB;NEeuOlgzQCEQvF2= M1zyW3NCVkeHUh?=
PSN1 NFHyWXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTR5Lke4NVMh|ryP NXW2VmlqW0GQR1XS

... 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:
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 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

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