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 MkXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPaTWM2OD1yLkC2NVQ{KM7:TR?= MWfTRW5ITVJ?
LAMA-84 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTBwMUW5PUDPxE1? MkDUV2FPT0WU
MEG-01 M2fvNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTBwMkO2PFgh|ryP NWPpd3c1W0GQR1XS
EM-2 M17H[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlj5TWM2OD1yLkK2OUDPxE1? NYXO[mllW0GQR1XS
TE-15 M4\GO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\ETGlEPTB;MD6yO|QyOiEQvF2= NIHJ[XRUSU6JRWK=
NCI-H1648 MlfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LSSGlEPTB;MD6yPFEyPiEQvF2= NWXNS3A4W0GQR1XS
TE-12 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\X[5Y6UUN3ME2wMlMzPjhizszN MlvyV2FPT0WU
LB996-RCC NUXRfJloT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTBwNESxPVYh|ryP NIDVWIFUSU6JRWK=
K-562 NEjkZ3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnX[FB[UUN3ME2wMlQ1QTZ5IN88US=> NF:2WJVUSU6JRWK=
D-336MG NXftdlJkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnzTWM2OD1yLkWwN|A1KM7:TR?= NV6wc4ZzW0GQR1XS
NOS-1 NIrwPXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTaNYVpUUN3ME2wMlYxPTJ7IN88US=> MlnyV2FPT0WU
EW-24 M4HZUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTBwNkK2PVMh|ryP NV3iUFlUW0GQR1XS
BV-173 MlrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\iN3JqUUN3ME2wMlY2OjR7IN88US=> MnvBV2FPT0WU
NCCIT MkP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2f3dmlEPTB;MD63N|IyQCEQvF2= NYHhblZCW0GQR1XS
NCI-H1436 NVq4XpN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fJbmlEPTB;MD63PVA1QSEQvF2= MVrTRW5ITVJ?
BB30-HNC NGDlZ2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlqyTWM2OD1yLki2NlA{KM7:TR?= NHrtNmxUSU6JRWK=
TE-8 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\vVZVXUUN3ME2wMlg4Ojd3IN88US=> M3PPcXNCVkeHUh?=
A704 MoiwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUKzc3FoUUN3ME2wMlg6OjFizszN NGjqNo1USU6JRWK=
TK10 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPWWI9QUUN3ME2wMlkxPjZ7IN88US=> M{LySXNCVkeHUh?=
KS-1 NX;HbJVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrPTWM2OD1zLkG5O|c6KM7:TR?= NW\JTndsW0GQR1XS
C2BBe1 NGHLfYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLWV3JMUUN3ME2xMlIxPTB5IN88US=> MmCxV2FPT0WU
RXF393 NX\sWIVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTFwMkSzOkDPxE1? NU\ve5oxW0GQR1XS
KGN NEHub3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLtd|BKSzVyPUGuNlc3QDdizszN MXPTRW5ITVJ?
NB69 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HBTmlEPTB;MT6zO|Q6PyEQvF2= MVfTRW5ITVJ?
TE-11 NHfzVlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTFwNEO0NVgh|ryP M1;EOnNCVkeHUh?=
TE-1 NIi4Wm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nsTmlEPTB;MT60OFExPSEQvF2= MnjpV2FPT0WU
ST486 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPZVHpIUUN3ME2xMlQ2QDV{IN88US=> M{faZ3NCVkeHUh?=
HOP-62 MoDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPiS2pKSzVyPUGuOVAzPDZizszN NELtZXJUSU6JRWK=
EW-16 M4O4fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLVWnh[UUN3ME2xMlU2ODh|IN88US=> MoDLV2FPT0WU
LB1047-RCC Mm\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHTPHZJUUN3ME2xMlU2PDV|IN88US=> MmXjV2FPT0WU
TE-10 M{Hoc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEntWppKSzVyPUGuOlYzPTJizszN MXvTRW5ITVJ?
RL95-2 MnTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jh[2lEPTB;MT62OlkxOiEQvF2= MUfTRW5ITVJ?
DOHH-2 MmXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nEO2lEPTB;MT63NVc5OiEQvF2= M4O3VHNCVkeHUh?=
MFH-ino NVvRTpRFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfwO2NKSzVyPUGuO|c5PyEQvF2= M1nM[HNCVkeHUh?=
GB-1 M2ixZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTFwN{m4N|Mh|ryP Mnf1V2FPT0WU
SK-N-DZ NGnYSWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\UTWM2OD1zLki0Olg5KM7:TR?= Mn7MV2FPT0WU
OS-RC-2 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2eyPWlEPTB;MT64PFU4PCEQvF2= NEK3bnhUSU6JRWK=
SW982 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LzUGlEPTB;MT65NlA6OyEQvF2= NHK5coZUSU6JRWK=
KALS-1 M13OWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmf2TWM2OD1zLkm4O|IzKM7:TR?= NVHlSHJQW0GQR1XS
TGBC24TKB MknQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETVNY1KSzVyPUKuNFU6PThizszN Ml7HV2FPT0WU
GI-1 NFm2WmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XoSGlEPTB;Mj6xOlA5PCEQvF2= M2\jOnNCVkeHUh?=
SW962 MkXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jHSWlEPTB;Mj6xO|E4QCEQvF2= MYjTRW5ITVJ?
SW872 Mn:3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2qyPWlEPTB;Mj6xPFUxPyEQvF2= NUDkNlVrW0GQR1XS
NCI-H747 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTJwMkW3NVQh|ryP MkH3V2FPT0WU
MZ1-PC NX7zfIVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XZPGlEPTB;Mj6yPVM2PiEQvF2= M3\mU3NCVkeHUh?=
MSTO-211H MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{j3[2lEPTB;Mj6zOVczOyEQvF2= NXflZW5OW0GQR1XS
BL-70 NIPFcIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjFN5AxUUN3ME2yMlQ4PDJ{IN88US=> NELGVHBUSU6JRWK=
SW954 NH\xeGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3Sy[mlEPTB;Mj61O|QxQCEQvF2= M4X4TXNCVkeHUh?=
SNB75 NUfCXHJ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPGTWM2OD1{Lk[4OVk1KM7:TR?= Ml[wV2FPT0WU
IST-SL2 NUf5PWQ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkD2TWM2OD1{LkeyN|c6KM7:TR?= M1rhdnNCVkeHUh?=
GCIY M1XuSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXrR5k1UUN3ME2yMlg4ODB3IN88US=> NFO2d3NUSU6JRWK=
KU812 M2rKOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfzTWM2OD1|LkC1Nlk6KM7:TR?= NUXBPW1wW0GQR1XS
LXF-289 NIDnfnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV:4cGJ1UUN3ME2zMlEzOTB7IN88US=> NXnPWJp[W0GQR1XS
ETK-1 NW\rTIZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHDTWM2OD1|LkKwO|Y4KM7:TR?= MV7TRW5ITVJ?
SF126 NXfMUow6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTNwM{GxO|Qh|ryP M1nBfnNCVkeHUh?=
LC-2-ad M3ThZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTNwNUW3JO69VQ>? NYjxO5QxW0GQR1XS
KNS-42 NFLGPY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTNwNkWg{txO M{DLVXNCVkeHUh?=
OVCAR-4 NGDyWYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfwTWM2OD1|LkezOFM{KM7:TR?= MUDTRW5ITVJ?
PF-382 NWD3PGZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHTTIpKSzVyPUOuPFM3QThizszN NUfHSG0zW0GQR1XS
SH-4 M2LKVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorLTWM2OD12LkK1NlU6KM7:TR?= M1ezTnNCVkeHUh?=
KM12 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTsPIZCUUN3ME20MlMzPDF4IN88US=> NGTwc5pUSU6JRWK=
NB5 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1m1[WlEPTB;ND60NVg3PCEQvF2= NIjlR3FUSU6JRWK=
KURAMOCHI MkPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LQcWlEPTB;ND62OVI2PiEQvF2= NH3ZcoxUSU6JRWK=
Becker M4TDcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPESFY1UUN3ME20MlY3PDF4IN88US=> M3zvZXNCVkeHUh?=
MV-4-11 NG\QTVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HVXmlEPTB;ND64NVM1PCEQvF2= M2HZU3NCVkeHUh?=
KINGS-1 MkX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XpTWlEPTB;ND64NlM4OyEQvF2= MnS1V2FPT0WU
LS-123 MnrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfaW2lKSzVyPUWuOFk3QDRizszN NVnuRmpZW0GQR1XS
SF268 M1HqOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvkOFFKSzVyPUWuOlEzPjJizszN MojUV2FPT0WU
A388 Mlv6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfoVGdmUUN3ME21MlY{PjZ5IN88US=> NEjodINUSU6JRWK=
NMC-G1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTZwMEG4NVEh|ryP NFfhXJZUSU6JRWK=
CGTH-W-1 NYTvfIdlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVP0fG1ZUUN3ME22MlAzODd3IN88US=> M3vlRnNCVkeHUh?=
ES4 MnPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3KzcWlEPTB;Nj61N|A4PCEQvF2= M4WyXnNCVkeHUh?=
SR MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjpR5FKSzVyPU[uOVg5ODdizszN MXrTRW5ITVJ?
BB49-HNC Mof3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXq3TVN4UUN3ME22Mlc{OjB4IN88US=> M33nfnNCVkeHUh?=
KLE NISz[|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zzOmlEPTB;Nj63PFM4PyEQvF2= NWOzd2VWW0GQR1XS
HUTU-80 MnTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnrdnpPUUN3ME22Mlk5PDZ4IN88US=> NVPKRWRyW0GQR1XS
SNU-C2B M3HGS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjzbpJCUUN3ME23MlgzPzN5IN88US=> NEfxTZFUSU6JRWK=
BB65-RCC M{L1OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTdwOUS5NFQh|ryP NEHES2lUSU6JRWK=
QIMR-WIL M{HicGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TwPGlEPTB;OD60NlgxQCEQvF2= MYLTRW5ITVJ?
GDM-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PPSmlEPTB;OD65O|I6OiEQvF2= MnflV2FPT0WU
LC4-1 M3Tq[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2npc2lEPTB;OT6wNFkyOSEQvF2= NUnOT5NKW0GQR1XS
MLMA NWTkRo5qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jXdGlEPTB;OT6xOVAxPiEQvF2= M4e1T3NCVkeHUh?=
EoL-1-cell MmjjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3MTWM2OD17LkOwNVkzKM7:TR?= MkTjV2FPT0WU
BOKU MkHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGj1bpFKSzVyPUmuPVY1PjZizszN MknqV2FPT0WU
EVSA-T MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTFyLk[1Olgh|ryP MnPDV2FPT0WU
D-283MED MmPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml33TWM2OD1zMD65NVc3KM7:TR?= MoHrV2FPT0WU
NB1 NEiwNJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1j2b2lEPTB;MUGuNFI1OiEQvF2= NVu0RopmW0GQR1XS
RPMI-8402 NFzoeZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnzW2lPUUN3ME2xNU4yPzhizszN NGPCW3NUSU6JRWK=
NCI-H1355 MknqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PUfmlEPTB;MUGuNVgxPiEQvF2= NGnKfotUSU6JRWK=
NB7 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTFzLkOyPVch|ryP MWDTRW5ITVJ?
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LB647-SCLC M4jBdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXxb3JKSzVyPUG3MlQ6PDlizszN MWPTRW5ITVJ?
NB10 MkHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mne0TWM2OD1zOD61NlU3KM7:TR?= MmPBV2FPT0WU
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Daudi Mo\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13pWmlEPTB;MkeuNFc4OyEQvF2= MYnTRW5ITVJ?
ALL-PO NIDSXYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYT5NItIUUN3ME2yO{4xQDFizszN M{PDZXNCVkeHUh?=
NB6 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TaN2lEPTB;MkeuOFg5KM7:TR?= MljGV2FPT0WU
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K5 M{\iVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoD6TWM2OD1{OD6xNlg4KM7:TR?= NH3EZpNUSU6JRWK=
ES1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPBW|l1UUN3ME2yPE44Pzd|IN88US=> M3TFdHNCVkeHUh?=
LC-1F M1rHdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFm2eWZKSzVyPUK5Mlc{PDZizszN NILrWHRUSU6JRWK=
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SK-PN-DW MljsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHxTWM2OD1|Mj61OVk5KM7:TR?= MoPQV2FPT0WU
D-247MG MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETOcGNKSzVyPUOyMlk4PzNizszN M3r5cHNCVkeHUh?=
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MONO-MAC-6 M4PUVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV[4ZYJ2UUN3ME2zN{42ODR6IN88US=> NGnKXnBUSU6JRWK=
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NCI-H209 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTN3LkG0OEDPxE1? MWHTRW5ITVJ?
A253 MkL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjGTWM2OD1|NT63OFI6KM7:TR?= MVLTRW5ITVJ?
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KARPAS-45 Mn3oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTR2LkO5NlUh|ryP MWDTRW5ITVJ?
HAL-01 NEXSXIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPicXZKSzVyPUS0MlUxOzRizszN M1nJcnNCVkeHUh?=
RCC10RGB NInqcJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHS1ZW5KSzVyPUS0Mlc{QTJizszN NFK5WGNUSU6JRWK=
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JiyoyeP-2003 NIqxb4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3z3TGlEPTB;NE[uNFEyQSEQvF2= MWHTRW5ITVJ?
HCE-4 M2LpPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fJcmlEPTB;NE[uOVk3QCEQvF2= NELqUndUSU6JRWK=
NCI-H720 MlPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTR4Lke2PFIh|ryP M1LaTXNCVkeHUh?=
KARPAS-422 NWfBfmxbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[yTWM2OD12Nz6wPFk2KM7:TR?= M3LvTXNCVkeHUh?=
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HCE-T MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTR5Lk[4Nlgh|ryP NE\OcXhUSU6JRWK=
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... 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 从左到右依次加入纯溶剂:
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

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