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)

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文献中Selleckの製品使用例（300）

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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

阻害剤	Citation	IGF-1R	Insulin Receptor	その他
Linsitinib (OSI-906)	199	++	++	IRR
NVP-AEW541	64	+	++	FLT3,Tek,FLT1
GSK1904529A	26	+++	+++
NVP-ADW742	22	+
BMS-536924	25	++	++	FAK,MEK,LCK
AG-1024	27	+	+
GSK1838705A	18	++++	++++	ALK
BMS-754807	51	++++	++++	TrkB,Met,TrkA
PQ 401	3	+
Ginsenoside Rg5	0	++
XL228	0	++++		ABL T315I,LYN,Aurora A
Picropodophyllin (PPP)	43	++++
AZD3463	7	✔		ALK
S961	1		✔
Nordihydroguaiaretic acid (NDGA)	0	✔		p300,HER2,lipoxygenase

1. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation. 2. "✔" indicates inhibitory effect, but without specific value.

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
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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

Clear solution

5% DMSO 1 95% Corn oil

1.65mg/ml (3.04mM)

Taking the 1 mL working solution as an example, add 50 μL of 33 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

Clear solution

5%DMSO 1 40%PEG300 Click to order 2 5%Tween 80 Click to order 3 50%ddH2O

5.0mg/ml (9.22mM)

Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

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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