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 M2Tkd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDHd3E6UUN3ME2wMlA3OTR|IN88US=> MnT6V2FPT0WU
LAMA-84 NV3QV|dMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTBwMUW5PUDPxE1? NUGzW5ZsW0GQR1XS
MEG-01 NEfG[GpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4roOGlEPTB;MD6yN|Y5QCEQvF2= M3fsbXNCVkeHUh?=
EM-2 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTBwMk[1JO69VQ>? NHTycFRUSU6JRWK=
TE-15 MkfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjX[5pKSzVyPUCuNlc1OTJizszN NFnJSHFUSU6JRWK=
NCI-H1648 NEfXRWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\aZ2NKSzVyPUCuNlgyOTZizszN NFW2dJZUSU6JRWK=
TE-12 MniyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTBwM{K2PEDPxE1? M{[4bHNCVkeHUh?=
LB996-RCC MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIq0d3NKSzVyPUCuOFQyQTZizszN NYLGbVlvW0GQR1XS
K-562 M3niXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETGNYxKSzVyPUCuOFQ6PjdizszN M1\EWXNCVkeHUh?=
D-336MG NXXqSoJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTBwNUCzNFQh|ryP MoTTV2FPT0WU
NOS-1 NFLNNIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M122[GlEPTB;MD62NFUzQSEQvF2= NVLpcmg3W0GQR1XS
EW-24 MkTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTBwNkK2PVMh|ryP Mo\QV2FPT0WU
BV-173 NX[4bml3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3vTWM2OD1yLk[1NlQ6KM7:TR?= M4XvUXNCVkeHUh?=
NCCIT NFf2d2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvEenpKSzVyPUCuO|MzOThizszN M4PMRXNCVkeHUh?=
NCI-H1436 NYKzU3BZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljyTWM2OD1yLke5NFQ6KM7:TR?= M17T[nNCVkeHUh?=
BB30-HNC NFXOVVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;4TWM2OD1yLki2NlA{KM7:TR?= MU\TRW5ITVJ?
TE-8 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIr6doVKSzVyPUCuPFczPzVizszN NWXQcmcyW0GQR1XS
A704 NUL1OJNvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWi5SHNMUUN3ME2wMlg6OjFizszN Moq4V2FPT0WU
TK10 M1rYZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrqe5BKSzVyPUCuPVA3PjlizszN MXHTRW5ITVJ?
KS-1 NX\We5pOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2r5WGlEPTB;MT6xPVc4QSEQvF2= NHPoTY5USU6JRWK=
C2BBe1 M1fqU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnkW243UUN3ME2xMlIxPTB5IN88US=> M1Tx[XNCVkeHUh?=
RXF393 MorOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVO0dJZDUUN3ME2xMlI1OzZizszN NV61O|llW0GQR1XS
KGN MmHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3Xvb2lEPTB;MT6yO|Y5PyEQvF2= NWrEXY51W0GQR1XS
NB69 NYGyfJRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7uTWM2OD1zLkO3OFk4KM7:TR?= MknsV2FPT0WU
TE-11 NU\XV4dKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\6No44UUN3ME2xMlQ{PDF6IN88US=> MVjTRW5ITVJ?
TE-1 MnruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3:wZmlEPTB;MT60OFExPSEQvF2= MmTpV2FPT0WU
ST486 NUnDWmRlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;4VmtPUUN3ME2xMlQ2QDV{IN88US=> NXnv[FR4W0GQR1XS
HOP-62 NIDoRndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DWW2lEPTB;MT61NFI1PiEQvF2= MYPTRW5ITVJ?
EW-16 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzDTWM2OD1zLkW1NFg{KM7:TR?= NFTWfIlUSU6JRWK=
LB1047-RCC NHzDeopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTFwNUW0OVMh|ryP MliyV2FPT0WU
TE-10 MoDGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfJR21[UUN3ME2xMlY3OjV{IN88US=> NXSyb3VlW0GQR1XS
RL95-2 MmnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTFwNk[5NFIh|ryP NWXhZ4RIW0GQR1XS
DOHH-2 NFfoWJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\zS2lEPTB;MT63NVc5OiEQvF2= MWPTRW5ITVJ?
MFH-ino Mmi0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfvSFdLUUN3ME2xMlc4QDdizszN M3rkb3NCVkeHUh?=
GB-1 Mnf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;ZUHZKSzVyPUGuO|k5OzNizszN M4DSR3NCVkeHUh?=
SK-N-DZ NWTWeJZ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4ntZWlEPTB;MT64OFY5QCEQvF2= MmXwV2FPT0WU
OS-RC-2 M3PMXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIq4UppKSzVyPUGuPFg2PzRizszN NEfTdpJUSU6JRWK=
SW982 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTFwOUKwPVMh|ryP MYLTRW5ITVJ?
KALS-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTFwOUi3NlIh|ryP MWXTRW5ITVJ?
TGBC24TKB MonXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjneFU3UUN3ME2yMlA2QTV6IN88US=> MonhV2FPT0WU
GI-1 NVy2PFhlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHVTWM2OD1{LkG2NFg1KM7:TR?= Mk[zV2FPT0WU
SW962 NVXmb4JDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHf2eFRKSzVyPUKuNVcyPzhizszN NU[wOFY3W0GQR1XS
SW872 NI\VN5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTJwMUi1NFch|ryP NU\p[2J1W0GQR1XS
NCI-H747 MoryS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTJwMkW3NVQh|ryP NFzWV2tUSU6JRWK=
MZ1-PC MnLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4SzN2lEPTB;Mj6yPVM2PiEQvF2= MXPTRW5ITVJ?
MSTO-211H M3nufGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTJwM{W3NlMh|ryP MVzTRW5ITVJ?
BL-70 NGLVVY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\5OXJQUUN3ME2yMlQ4PDJ{IN88US=> NXTDOmIzW0GQR1XS
SW954 NWXENXNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnFZWhKSzVyPUKuOVc1ODhizszN NVr5cJA5W0GQR1XS
SNB75 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLITWM2OD1{Lk[4OVk1KM7:TR?= MmLkV2FPT0WU
IST-SL2 M3TQ[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInFbItKSzVyPUKuO|I{PzlizszN MYXTRW5ITVJ?
GCIY NGezN|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2Cxd2lEPTB;Mj64O|AxPSEQvF2= MoHhV2FPT0WU
KU812 M4TrS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLDTWM2OD1|LkC1Nlk6KM7:TR?= MYXTRW5ITVJ?
LXF-289 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH:4Zo5KSzVyPUOuNVIyODlizszN MlnIV2FPT0WU
ETK-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTNwMkC3Olch|ryP MmXZV2FPT0WU
SF126 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXH6e49VUUN3ME2zMlMyOTd2IN88US=> MlXDV2FPT0WU
LC-2-ad NFnQWmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHwd5Q2UUN3ME2zMlU2PyEQvF2= NGrzeYRUSU6JRWK=
KNS-42 MljwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLrc2Q2UUN3ME2zMlY2KM7:TR?= M2e3dnNCVkeHUh?=
OVCAR-4 MnnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHNTWM2OD1|LkezOFM{KM7:TR?= NWrSVmg{W0GQR1XS
PF-382 NWT5[o9tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{P3WmlEPTB;Mz64N|Y6QCEQvF2= M36xW3NCVkeHUh?=
SH-4 M2\kbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HkV2lEPTB;ND6yOVI2QSEQvF2= MYLTRW5ITVJ?
KM12 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLDTWM2OD12LkOyOFE3KM7:TR?= MUnTRW5ITVJ?
NB5 NIqzVoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml65TWM2OD12LkSxPFY1KM7:TR?= NXuyOY9LW0GQR1XS
KURAMOCHI NYS1ToJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFH3TVRKSzVyPUSuOlUzPTZizszN NGXmeWNUSU6JRWK=
Becker MnzqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTRwNk[0NVYh|ryP NWjGXY96W0GQR1XS
MV-4-11 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI[wWXVKSzVyPUSuPFE{PDRizszN NIriU2FUSU6JRWK=
KINGS-1 NXvISXh7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjVTWM2OD12LkiyN|c{KM7:TR?= MlP6V2FPT0WU
LS-123 NXPHUHc2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoG1TWM2OD13LkS5Olg1KM7:TR?= NE\mSWRUSU6JRWK=
SF268 NGLyOJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm[xTWM2OD13Lk[xNlYzKM7:TR?= M1nJ[nNCVkeHUh?=
A388 MnfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUCz[3VXUUN3ME21MlY{PjZ5IN88US=> MVLTRW5ITVJ?
NMC-G1 MoSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7PTWM2OD14LkCxPFEyKM7:TR?= M3Xib3NCVkeHUh?=
CGTH-W-1 NWjSS29jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIO3SZNKSzVyPU[uNFIxPzVizszN MWLTRW5ITVJ?
ES4 M{ftUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXNTWM2OD14LkWzNFc1KM7:TR?= MX\TRW5ITVJ?
SR MnToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTZwNUi4NFch|ryP NUPOSFlLW0GQR1XS
BB49-HNC NUfHWVNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIL1d4NKSzVyPU[uO|MzODZizszN M2S0TXNCVkeHUh?=
KLE M3OzcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjNdnY5UUN3ME22Mlc5Ozd5IN88US=> MWPTRW5ITVJ?
HUTU-80 NITHXlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLwTWM2OD14Lkm4OFY3KM7:TR?= MlPUV2FPT0WU
SNU-C2B NU\KT2dJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\Zb5R7UUN3ME23MlgzPzN5IN88US=> NWW4bow{W0GQR1XS
BB65-RCC M2rFN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nxVmlEPTB;Nz65OFkxPCEQvF2= NV33XFIzW0GQR1XS
QIMR-WIL MnnHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfHNWxtUUN3ME24MlQzQDB6IN88US=> NGD5ZYhUSU6JRWK=
GDM-1 NEjRSmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\3TWM2OD16Lkm3NlkzKM7:TR?= NX3IXGFNW0GQR1XS
LC4-1 NIjkTVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrScld2UUN3ME25MlAxQTFzIN88US=> M4r5XnNCVkeHUh?=
MLMA NEew[WVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LJfGlEPTB;OT6xOVAxPiEQvF2= NV3WeodCW0GQR1XS
EoL-1-cell MlvZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TQd2lEPTB;OT6zNFE6OiEQvF2= M336R3NCVkeHUh?=
BOKU Mke0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DwemlEPTB;OT65OlQ3PiEQvF2= Ml\IV2FPT0WU
EVSA-T Mk[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTFyLk[1Olgh|ryP M3XUUnNCVkeHUh?=
D-283MED M2q5SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTFyLkmxO|Yh|ryP M2DGd3NCVkeHUh?=
NB1 Mn3ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTLd49KSzVyPUGxMlAzPDJizszN M1LyZnNCVkeHUh?=
RPMI-8402 NGCycHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTFzLkG3PEDPxE1? NEjVenVUSU6JRWK=
NCI-H1355 M1rMcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWL5UZAxUUN3ME2xNU4yQDB4IN88US=> NHuxTFFUSU6JRWK=
NB7 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jMRWlEPTB;MUGuN|I6PyEQvF2= NUfEOWxYW0GQR1XS
RPMI-6666 NHvUeGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3PTWM2OD1zMj65OVY4KM7:TR?= MkXZV2FPT0WU
697 M33HZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vQXmlEPTB;MUOuNlcxOSEQvF2= MnHYV2FPT0WU
CTB-1 M{nW[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTF|LkW5OFgh|ryP NVewSpZVW0GQR1XS
VA-ES-BJ MoG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrPbYJGUUN3ME2xN{46OjN2IN88US=> NHTKd4tUSU6JRWK=
BE-13 NFnOOHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXntUGZ{UUN3ME2xOE4{QTF3IN88US=> M3PtcHNCVkeHUh?=
SKM-1 NVXKTWJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTF2LkS0PVkh|ryP NG\m[4RUSU6JRWK=
TE-6 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLDTWM2OD1zND63OVkyKM7:TR?= NHP4N4hUSU6JRWK=
LB771-HNC Mn3YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFf6fJhKSzVyPUG0Mlc5QThizszN NF\VcXNUSU6JRWK=
ECC4 M3K5[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH20ZY1KSzVyPUG3MlAzPzdizszN MmPMV2FPT0WU
ES3 NGLhZmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzmTWM2OD1zNz60OlU2KM7:TR?= MkH3V2FPT0WU
LB647-SCLC NXvEZYZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTF5LkS5OFkh|ryP Mn;GV2FPT0WU
NB10 NF2xPGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzFTWM2OD1zOD61NlU3KM7:TR?= MmLCV2FPT0WU
L-540 NIjyUnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jMXWlEPTB;MUiuPFExQSEQvF2= MXPTRW5ITVJ?
NCI-H2126 NEXZcHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmewTWM2OD1zOT61NUDPxE1? MVfTRW5ITVJ?
HH MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;xcGlEPTB;MkCuNFA6QSEQvF2= NILVVm1USU6JRWK=
MPP-89 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTJ|LkKyPFkh|ryP NHvwbnBUSU6JRWK=
IST-MEL1 MoHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfQTWM2OD1{Mz64OlU5KM7:TR?= M4DB[HNCVkeHUh?=
KP-N-YS NFjMTZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTJ|LkmyOVUh|ryP M{jLdHNCVkeHUh?=
EC-GI-10 MmrXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jqPGlEPTB;MkSuOVk5QSEQvF2= M2L4T3NCVkeHUh?=
EKVX M{PVZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{[4RmlEPTB;Mk[uNFIxOyEQvF2= NYTkXJhCW0GQR1XS
TGBC1TKB NXPHfFdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnn4TWM2OD1{Nj60N|Qh|ryP MnPXV2FPT0WU
Daudi MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjHR3NnUUN3ME2yO{4xPzd|IN88US=> NH7WWVZUSU6JRWK=
ALL-PO NFz1Vm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zwdGlEPTB;MkeuNFgyKM7:TR?= Ml\qV2FPT0WU
NB6 MofqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHFWYl6UUN3ME2yO{41QDhizszN MoXIV2FPT0WU
ES6 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXW1WIZUUUN3ME2yO{46OTJ|IN88US=> MYHTRW5ITVJ?
COLO-320-HSR MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInLVmhKSzVyPUK4MlA{PzNizszN MVHTRW5ITVJ?
K5 NWDBSpd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTJ6LkGyPFch|ryP Mn;UV2FPT0WU
ES1 NYHtZVc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXiTGxUUUN3ME2yPE44Pzd|IN88US=> MUfTRW5ITVJ?
LC-1F M2XYSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rjTGlEPTB;MkmuO|M1PiEQvF2= MkDoV2FPT0WU
SCLC-21H NYraPFFPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HW[GlEPTB;M{CuO|MyPyEQvF2= NXjhSGxyW0GQR1XS
SK-PN-DW NEewRYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TsPGlEPTB;M{KuOVU6QCEQvF2= M{PRUnNCVkeHUh?=
D-247MG MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\tVmVnUUN3ME2zNk46Pzd|IN88US=> NIToe2tUSU6JRWK=
TE-5 NFTOSFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTN|LkCzOlIh|ryP M3LGXXNCVkeHUh?=
MONO-MAC-6 M3\zOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHK[pA5UUN3ME2zN{42ODR6IN88US=> M2TaZnNCVkeHUh?=
LB2518-MEL NFr1NJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTN|Lke2OlYh|ryP MnTOV2FPT0WU
LOXIMVI NVPscXNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\HZW5KSzVyPUOzMlc6OjhizszN NGPsT5pUSU6JRWK=
NCI-H209 MkLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInYTYtKSzVyPUO1MlE1PCEQvF2= M{nONXNCVkeHUh?=
A253 M1PSfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LWdGlEPTB;M{WuO|QzQSEQvF2= NYLO[VFjW0GQR1XS
HCC1599 NGH4Z3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jDVGlEPTB;M{[uO|A2OyEQvF2= MkLHV2FPT0WU
EB-3 MnWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTN4Lkm1NVgh|ryP NVPONJVGW0GQR1XS
GOTO MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrjPI5[UUN3ME2zO{4{OjJ2IN88US=> NU\leVNRW0GQR1XS
SW684 NFH6O5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTRzLki0PVUh|ryP NHfaeFVUSU6JRWK=
DEL M3LqdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWr4dYZPUUN3ME20Nk4xPTJ{IN88US=> MoDyV2FPT0WU
HT-144 NYDPdGVZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTR{LkG2O|Yh|ryP Mn7kV2FPT0WU
TE-9 Ml6zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlv6TWM2OD12Mz60OVk3KM7:TR?= NFXNcG1USU6JRWK=
KARPAS-45 M4fFe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvzTWM2OD12ND6zPVI2KM7:TR?= MW\TRW5ITVJ?
HAL-01 NXfJe211T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MomwTWM2OD12ND61NFM1KM7:TR?= NYqybJIzW0GQR1XS
RCC10RGB NEHpWXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jKcmlEPTB;NESuO|M6OiEQvF2= NUTWV3hUW0GQR1XS
CP67-MEL NVznZ4d1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTR3Lk[yOFEh|ryP MnzDV2FPT0WU
NB17 NFrlfYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkn1TWM2OD12NT62OlQ{KM7:TR?= M1zoR3NCVkeHUh?=
SK-UT-1 MlzPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXoSZRkUUN3ME20OU46PDZ2IN88US=> Ml2wV2FPT0WU
JiyoyeP-2003 Ml;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTR4LkCxNVkh|ryP M1m5WHNCVkeHUh?=
HCE-4 NELQPJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\zTWM2OD12Nj61PVY5KM7:TR?= NXr2PZhKW0GQR1XS
NCI-H720 NXL2fmw6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3nOI5KSzVyPUS2Mlc3QDJizszN MYPTRW5ITVJ?
KARPAS-422 NWTrSXhUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPxcVc{UUN3ME20O{4xQDl3IN88US=> Mn\LV2FPT0WU
Ramos-2G6-4C10 Mnj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDNTWM2OD12Nz6xOlIzKM7:TR?= MXTTRW5ITVJ?
HCE-T MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXaTWM2OD12Nz62PFI5KM7:TR?= NHzzXGVUSU6JRWK=
PSN1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG[wdZBKSzVyPUS3Mlc5OTNizszN M3ezbXNCVkeHUh?=

... 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