Saracatinib (AZD0530)

製品コード：S1006 純度：99.99%

Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy. Phase 2/3.

CAS No. 379231-04-6

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
10mg	JPY 22000	国内在庫あり
200mg	JPY 145500	国内在庫あり
1g	JPY 370500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（300）

製品安全説明書

現在のバッチを見る：純度： 99.99%

99.99

Saracatinib (AZD0530)関連製品

関連ターゲット	Lck Fyn Lyn Yes Fgr	もっと見る
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関連化合物ライブラリー	Tyrosine Kinase Inhibitor Library PI3K/Akt Inhibitor Library Angiogenesis Related compound Library HIF-1 Signaling Pathway Compound Library FDA-approved Anticancer Drug Library	もっと見る

シグナル伝達経路

Srcシグナル伝達経路

Src阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
Huh7	Antiviral assay	2.5 uM	5 days	Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control	17360676
Huh7	Antiviral assay	2.5 uM	6 days	Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control	17360676
Vero	Antiviral assay	2.5 uM	4 days	Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control	17360676
Vero	Antiviral assay	2.5 uM	6 days	Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control	17360676
C6/36	Antiviral assay	2.5 uM	4 days	Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control	17360676
C6/36	Antiviral assay	2.5 uM	5 days	Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control	17360676
Vero	Antiviral assay	2.5 uM	5 days	Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control	17360676
Huh7	Antiviral assay	2.5 uM	4 days	Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control	17360676
C6/36	Antiviral assay	2.5 uM	6 days	Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control	17360676
HEK293	Function assay	0.1 to 1 uM	16 hrs	Inhibition of collagen I-induced DDR2 (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting	26191369
HEK293	Function assay	0.1 to 1 uM	16 hrs	Inhibition of collagen I-induced DDR2 I638F mutant (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting	26191369
HEK293	Function assay		1 hr	Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, Ki = 0.0398 μM.	29941193
HEK293	Function assay		1 hr	Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, IC50 = 0.418 μM.	29941193
Rh30	Antiproliferative assay		48 hrs	Antiproliferative activity against human Rh30 cells after 48 hrs by CellTiter-Glo luminescent assay, IC50 = 10.1 μM.	23787099
Vero	Antiviral assay		3 days	Antiviral activity against Dengue virus infected in african green monkey Vero cells administered after viral challenge after 3 days by viral plaque assay	17360676
SH-4	Growth Inhibition Assay			IC50=4.25259 μM	SANGER
PF-382	Growth Inhibition Assay			IC50=3.83698 μM	SANGER
OVCAR-4	Growth Inhibition Assay			IC50=3.73433 μM	SANGER
KNS-42	Growth Inhibition Assay			IC50=3.65 μM	SANGER
LC-2-ad	Growth Inhibition Assay			IC50=3.557 μM	SANGER
SF126	Growth Inhibition Assay			IC50=3.31174 μM	SANGER
ETK-1	Growth Inhibition Assay			IC50=3.20767 μM	SANGER
LXF-289	Growth Inhibition Assay			IC50=3.12109 μM	SANGER
KU812	Growth Inhibition Assay			IC50=3.05299 μM	SANGER
GCIY	Growth Inhibition Assay			IC50=2.87005 μM	SANGER
IST-SL2	Growth Inhibition Assay			IC50=2.72379 μM	SANGER
SNB75	Growth Inhibition Assay			IC50=2.68594 μM	SANGER
SW954	Growth Inhibition Assay			IC50=2.57408 μM	SANGER
BL-70	Growth Inhibition Assay			IC50=2.47422 μM	SANGER
MSTO-211H	Growth Inhibition Assay			IC50=2.35723 μM	SANGER
MZ1-PC	Growth Inhibition Assay			IC50=2.29356 μM	SANGER
NCI-H747	Growth Inhibition Assay			IC50=2.25714 μM	SANGER
SW872	Growth Inhibition Assay			IC50=2.18507 μM	SANGER
SW962	Growth Inhibition Assay			IC50=2.17178 μM	SANGER
GI-1	Growth Inhibition Assay			IC50=2.16084 μM	SANGER
TGBC24TKB	Growth Inhibition Assay			IC50=2.05958 μM	SANGER
KALS-1	Growth Inhibition Assay			IC50=1.98722 μM	SANGER
SW982	Growth Inhibition Assay			IC50=1.92093 μM	SANGER
OS-RC-2	Growth Inhibition Assay			IC50=1.88574 μM	SANGER
SK-N-DZ	Growth Inhibition Assay			IC50=1.84688 μM	SANGER
GB-1	Growth Inhibition Assay			IC50=1.79833 μM	SANGER
MFH-ino	Growth Inhibition Assay			IC50=1.7787 μM	SANGER
DOHH-2	Growth Inhibition Assay			IC50=1.71782 μM	SANGER
RL95-2	Growth Inhibition Assay			IC50=1.66902 μM	SANGER
TE-10	Growth Inhibition Assay			IC50=1.66252 μM	SANGER
LB1047-RCC	Growth Inhibition Assay			IC50=1.55453 μM	SANGER
EW-16	Growth Inhibition Assay			IC50=1.55083 μM	SANGER
HOP-62	Growth Inhibition Assay			IC50=1.50246 μM	SANGER
ST486	Growth Inhibition Assay			IC50=1.45852 μM	SANGER
TE-1	Growth Inhibition Assay			IC50=1.44105 μM	SANGER
TE-11	Growth Inhibition Assay			IC50=1.43418 μM	SANGER
NB69	Growth Inhibition Assay			IC50=1.37497 μM	SANGER
KGN	Growth Inhibition Assay			IC50=1.27687 μM	SANGER
RXF393	Growth Inhibition Assay			IC50=1.2436 μM	SANGER
C2BBe1	Growth Inhibition Assay			IC50=1.20507 μM	SANGER
KS-1	Growth Inhibition Assay			IC50=1.19779 μM	SANGER
TK10	Growth Inhibition Assay			IC50=0.90669 μM	SANGER
A704	Growth Inhibition Assay			IC50=0.8921 μM	SANGER
TE-8	Growth Inhibition Assay			IC50=0.87275 μM	SANGER
BB30-HNC	Growth Inhibition Assay			IC50=0.86203 μM	SANGER
NCI-H1436	Growth Inhibition Assay			IC50=0.79049 μM	SANGER
NCCIT	Growth Inhibition Assay			IC50=0.73218 μM	SANGER
BV-173	Growth Inhibition Assay			IC50=0.65249 μM	SANGER
EW-24	Growth Inhibition Assay			IC50=0.62693 μM	SANGER
NOS-1	Growth Inhibition Assay			IC50=0.60529 μM	SANGER
D-336MG	Growth Inhibition Assay			IC50=0.50304 μM	SANGER
K-562	Growth Inhibition Assay			IC50=0.44967 μM	SANGER
LB996-RCC	Growth Inhibition Assay			IC50=0.44196 μM	SANGER
TE-12	Growth Inhibition Assay			IC50=0.3268 μM	SANGER
NCI-H1648	Growth Inhibition Assay			IC50=0.28116 μM	SANGER
TE-15	Growth Inhibition Assay			IC50=0.27412 μM	SANGER
EM-2	Growth Inhibition Assay			IC50=0.265 μM	SANGER
MEG-01	Growth Inhibition Assay			IC50=0.23688 μM	SANGER
LAMA-84	Growth Inhibition Assay			IC50=0.1599 μM	SANGER
CTV-1	Growth Inhibition Assay			IC50=0.06143 μM	SANGER
KM12	Growth Inhibition Assay			IC50=4.32416 μM	SANGER
NB5	Growth Inhibition Assay			IC50=4.41864 μM	SANGER
KURAMOCHI	Growth Inhibition Assay			IC50=4.65256 μM	SANGER
Becker	Growth Inhibition Assay			IC50=4.66416 μM	SANGER
MV-4-11	Growth Inhibition Assay			IC50=4.81344 μM	SANGER
KINGS-1	Growth Inhibition Assay			IC50=4.82373 μM	SANGER
LS-123	Growth Inhibition Assay			IC50=5.49684 μM	SANGER
SF268	Growth Inhibition Assay			IC50=5.61262 μM	SANGER
A388	Growth Inhibition Assay			IC50=5.63667 μM	SANGER
NMC-G1	Growth Inhibition Assay			IC50=6.01811 μM	SANGER
CGTH-W-1	Growth Inhibition Assay			IC50=6.02075 μM	SANGER
ES4	Growth Inhibition Assay			IC50=6.53074 μM	SANGER
SR	Growth Inhibition Assay			IC50=6.58807 μM	SANGER
BB49-HNC	Growth Inhibition Assay			IC50=6.73206 μM	SANGER
KLE	Growth Inhibition Assay			IC50=6.78377 μM	SANGER
HUTU-80	Growth Inhibition Assay			IC50=6.98466 μM	SANGER
SNU-C2B	Growth Inhibition Assay			IC50=7.82737 μM	SANGER
BB65-RCC	Growth Inhibition Assay			IC50=7.94904 μM	SANGER
QIMR-WIL	Growth Inhibition Assay			IC50=8.42808 μM	SANGER
GDM-1	Growth Inhibition Assay			IC50=8.97292 μM	SANGER
LC4-1	Growth Inhibition Assay			IC50=9.00911 μM	SANGER
MLMA	Growth Inhibition Assay			IC50=9.15006 μM	SANGER
EoL-1-cell	Growth Inhibition Assay			IC50=9.30192 μM	SANGER
BOKU	Growth Inhibition Assay			IC50=9.96466 μM	SANGER
EVSA-T	Growth Inhibition Assay			IC50=10.6568 μM	SANGER
D-283MED	Growth Inhibition Assay			IC50=10.9176 μM	SANGER
NB1	Growth Inhibition Assay			IC50=11.0242 μM	SANGER
RPMI-8402	Growth Inhibition Assay			IC50=11.178 μM	SANGER
NCI-H1355	Growth Inhibition Assay			IC50=11.1806 μM	SANGER
NB7	Growth Inhibition Assay			IC50=11.3297 μM	SANGER
RPMI-6666	Growth Inhibition Assay			IC50=12.9567 μM	SANGER
697	Growth Inhibition Assay			IC50=13.2701 μM	SANGER
CTB-1	Growth Inhibition Assay			IC50=13.5948 μM	SANGER
VA-ES-BJ	Growth Inhibition Assay			IC50=13.9234 μM	SANGER
BE-13	Growth Inhibition Assay			IC50=14.3915 μM	SANGER
SKM-1	Growth Inhibition Assay			IC50=14.4499 μM	SANGER
TE-6	Growth Inhibition Assay			IC50=14.7591 μM	SANGER
LB771-HNC	Growth Inhibition Assay			IC50=14.7898 μM	SANGER
ECC4	Growth Inhibition Assay			IC50=17.0277 μM	SANGER
ES3	Growth Inhibition Assay			IC50=17.4655 μM	SANGER
LB647-SCLC	Growth Inhibition Assay			IC50=17.4949 μM	SANGER
NB10	Growth Inhibition Assay			IC50=18.5256 μM	SANGER
L-540	Growth Inhibition Assay			IC50=18.8109 μM	SANGER
NCI-H2126	Growth Inhibition Assay			IC50=19.51 μM	SANGER
HH	Growth Inhibition Assay			IC50=20.0099 μM	SANGER
MPP-89	Growth Inhibition Assay			IC50=23.2289 μM	SANGER
IST-MEL1	Growth Inhibition Assay			IC50=23.8658 μM	SANGER
KP-N-YS	Growth Inhibition Assay			IC50=23.9255 μM	SANGER
EC-GI-10	Growth Inhibition Assay			IC50=24.5989 μM	SANGER
EKVX	Growth Inhibition Assay			IC50=26.0203 μM	SANGER
TGBC1TKB	Growth Inhibition Assay			IC50=26.434 μM	SANGER
Daudi	Growth Inhibition Assay			IC50=27.0773 μM	SANGER
ALL-PO	Growth Inhibition Assay			IC50=27.081 μM	SANGER
NB6	Growth Inhibition Assay			IC50=27.488 μM	SANGER
ES6	Growth Inhibition Assay			IC50=27.9123 μM	SANGER
COLO-320-HSR	Growth Inhibition Assay			IC50=28.0373 μM	SANGER
K5	Growth Inhibition Assay			IC50=28.1287 μM	SANGER
ES1	Growth Inhibition Assay			IC50=28.7773 μM	SANGER
LC-1F	Growth Inhibition Assay			IC50=29.7346 μM	SANGER
SCLC-21H	Growth Inhibition Assay			IC50=30.7317 μM	SANGER
SK-PN-DW	Growth Inhibition Assay			IC50=32.5598 μM	SANGER
D-247MG	Growth Inhibition Assay			IC50=32.9773 μM	SANGER
TE-5	Growth Inhibition Assay			IC50=33.0362 μM	SANGER
MONO-MAC-6	Growth Inhibition Assay			IC50=33.5048 μM	SANGER
LB2518-MEL	Growth Inhibition Assay			IC50=33.7666 μM	SANGER
LOXIMVI	Growth Inhibition Assay			IC50=33.7928 μM	SANGER
NCI-H209	Growth Inhibition Assay			IC50=35.144 μM	SANGER
A253	Growth Inhibition Assay			IC50=35.7429 μM	SANGER
HCC1599	Growth Inhibition Assay			IC50=36.7053 μM	SANGER
EB-3	Growth Inhibition Assay			IC50=36.9518 μM	SANGER
GOTO	Growth Inhibition Assay			IC50=37.3224 μM	SANGER
SW684	Growth Inhibition Assay			IC50=41.8495 μM	SANGER
DEL	Growth Inhibition Assay			IC50=42.0522 μM	SANGER
HT-144	Growth Inhibition Assay			IC50=42.1676 μM	SANGER
TE-9	Growth Inhibition Assay			IC50=43.4596 μM	SANGER
KARPAS-45	Growth Inhibition Assay			IC50=44.3925 μM	SANGER
HAL-01	Growth Inhibition Assay			IC50=44.5034 μM	SANGER
RCC10RGB	Growth Inhibition Assay			IC50=44.7392 μM	SANGER
CP67-MEL	Growth Inhibition Assay			IC50=45.6241 μM	SANGER
NB17	Growth Inhibition Assay			IC50=45.6643 μM	SANGER
SK-UT-1	Growth Inhibition Assay			IC50=45.9464 μM	SANGER
JiyoyeP-2003	Growth Inhibition Assay			IC50=46.0119 μM	SANGER
HCE-4	Growth Inhibition Assay			IC50=46.5968 μM	SANGER
NCI-H720	Growth Inhibition Assay			IC50=46.7682 μM	SANGER
KARPAS-422	Growth Inhibition Assay			IC50=47.0895 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay			IC50=47.1622 μM	SANGER
HCE-T	Growth Inhibition Assay			IC50=47.6828 μM	SANGER
PSN1	Growth Inhibition Assay			IC50=47.7813 μM	SANGER
NIH3T3	Function assay			Inhibition of human c-Src in NIH3T3 cells, IC50 = 0.0027 μM.	17064066
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
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生物活性

製品説明

特性

The 1st Src inhibitor to show inhibition of the Src pathway in human tumor tissue.

Targets

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)	もっとクリックする
2.7 nM	<4 nM	4 nM	4 nM	5 nM	もっとクリックする

In Vitro
In vitro	Saracatinib also potently inhibits other Src tyrosine kinase family members including c-Yes, Fyn, Lyn, Blk, Fgr, and Lck with IC50 from 4-10 nM. Saracatinib sensitively inhibits Src Y530F NIH 3T3 with IC50 of 80 nM. Saracatinib signiﬁcantly impairs the invasion of HT1080 cells through a 3-dimensional collagen matrix and completely inhibits EGF-induced cell scattering in NBT-II bladder cancer cells. ^[1] Saracatinib potent inhibits Src activation in DU145 and PC3 cells, which through inhibition of Y419 phosphorylation. Saracatinib inhibits the growth of prostate cancer including PC3, DU145, CWR22Rv1 and LNCaP, while Saracatinib shows low activity in LAPC-4, PZ-HPV7 and RWPE-1 cells. Saracatinib induces cell cycle arrest at G1/S but not caspase 3 cleavages. Saracatinib also significantly inhibits DU145 and PC3 migration in the Boyden chamber. ^[2] Saracatinib gives a potent and sustained blockage of AKT and enhances the sensitivity to irradiation in A549 and Calu-6 cells. ^[3] Saracatinib inhibits osteoclast in activity, resorption and formation. Saracatinib also reversibly prevents osteoclast precursor migration. ^[4]
Kinase Assay	Kinase Assay
Kinase Assay	IC50 of tyrosine kinase activity is measured by an enzyme-linked immunosorbent assay (ELISA) with recombinant catalytic domains of a panel of receptor and non-receptor tyrosine kinases (in some cases only part of the catalytic domain is used). Saracatinib dose ranges from 0.001-10 mM. Speciﬁcity assays against a panel of serine/threonine kinases are performed using a ﬁlter capture assay with ³²P. Brieﬂy, multidrop 384 plates containing 0.5 μL Saracatinib or controls (DMSO) alone or pH 3.0 buffer controls) are incubated with 15 μL of enzyme plus peptide/protein substrate for 5 min before the reaction is initiated by the addition of 10 μL of 20 mM Mg-ATP. For all enzymes the ﬁnal concentration is approximated to the Michaelis constant (K_m). Assays are carried out for 30min at room temperature before termination by the addition of 5 μL orthophosphoric acid. After mixing, the well contents are harvested onto a P81 Uniﬁlter plate, using orthophosphoric acid as the wash buffer. Then IC50 is calculated.
細胞実験	細胞株	PC3, DU145, CWR22Rv1, LNCaP, LAPC-4, PZ-HPV7 and RWPE-1 cells
	濃度	62.5 nM - 16 mM
	反応時間	1, 3 and 5 days
	実験の流れ	Cells are seeded at a density of 2× 10³ in 96-well plates and incubated overnight. Then Saracatinib (62.5 nM-16 mM) is added to the cells. After 1, 3 and 5 days, culture medium is removed followed by addition of 0.2 mL DMSO per well and continuous shaking of plates at 200 rotations per minute for 15min. Then IC50 is measured by MTT metho
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	pY576-FAK / pY861-FAK / FAK pY418 Src / Src / pY410 CAS / CAS / Py421 Cortactin / Cortactin p-Akt / p-mTOR / Akt / mTOR / p-S6 / S6 / p-AMPKα / AMPKα		20551056
	Growth inhibition assay	Cell number		24349321

In Vivo
In Vivo	Saracatinib shows great tumor growth inhibition in Src3T3 allografts and a moderate growth delay in Calu-6, MDA-MB-231, AsPc-1 and BT474C xenografts. ^[1] Saracatinib shows great antitumor activity in orthotopic DU145 xenograft mice at a dose of 25mg/kg (orally administered, daily). ^[2]
動物実験	動物モデル	CB17 mice are implanted with DU145 cells.
	投与量	25 mg/kg
	投与経路	Orally administered daily

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT04598919	Active not recruiting	Idiopathic Pulmonary Fibrosis (IPF)	National Jewish Health\|Yale University\|Icahn School of Medicine at Mount Sinai\|AstraZeneca\|National Center for Advancing Translational Sciences (NCATS)\|Baylor University\|International Center for Health Outcomes and Innovation Research	November 12 2020	Phase 1\|Phase 2
NCT04307953	Recruiting	Fibrodysplasia Ossificans Progressiva	Amsterdam UMC location VUmc\|Royal National Orthopaedic Hospital NHS Trust\|Klinikum Garmisch-Patenkirchen\|University of Oxford\|Brigham and Women''s Hospital\|AstraZeneca\|Innovative Medicines Initiative	August 5 2020	Phase 2
NCT02085603	Completed	Cancer	Sheffield Teaching Hospitals NHS Foundation Trust\|AstraZeneca	March 2014	Phase 2
NCT01864655	Completed	Alzheimer''s Disease	Stephen M. Strittmatter\|National Institute of Neurological Disorders and Stroke (NINDS)\|Yale University	July 2013	Phase 1
NCT01000896	Withdrawn	Cancer\|Non Small Cell Lung Cancer\|Epithelial Ovarian Cancer	AstraZeneca	January 2010	Phase 1

参考
[1] Chang YM, Oncogene, 2008, 27(49), 6365-6375. [2] Green TP, et al. Mol Oncol, 2009, 3(3), 248-261. [3] Purnell PR, et al. J Thorac Oncol, 2009, 4(4), 448-454. [4] de Vries TJ, et al. Mol Cancer Res, 2009, 7(4), 476-488. [5] Gwanmesia PM, et al. BMC Cancer, 2009, 13;9:53. [6] Hiscox S, et al. Breast Cancer Res Treat, 2009, 115(1), 57-67. [7] Chen Y, et al. Clin Cancer Res, 2009, 15(10), 3396-3405. + 展開

参考

+ 展開

化学情報

分子量	542.03	化学式	C₂₇H₃₂ClN₅O₅
CAS No.	379231-04-6	SDF	Download Saracatinib (AZD0530) SDFをダウンロードする
Smiles	CN1CCN(CC1)CCOC2=CC3=C(C(=C2)OC4CCOCC4)C(=NC=N3)NC5=C(C=CC6=C5OCO6)Cl
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (184.49 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 100 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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よくある質問（FAQ）

質問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

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