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/ Saracatinib/塞卡替尼

Saracatinib/塞卡替尼 {[allProObj[0].p_purity_real_show]}

货号：A154045 同义名： AZD0530

Saracatinib（AZD0530）是一种高效的Src家族抑制剂，对c-Src、Lck、c-YES、Lyn、Fyn、Fgr和Blk的IC50范围为2.7至11 nM，显示出对其他酪氨酸激酶的高选择性。

Saracatinib/塞卡替尼 化学结构 CAS号：379231-04-6
Saracatinib/塞卡替尼 化学结构
CAS号：379231-04-6
Saracatinib/塞卡替尼 3D分子结构
CAS号：379231-04-6
Saracatinib/塞卡替尼 化学结构 CAS号：379231-04-6
Saracatinib/塞卡替尼 3D分子结构 CAS号：379231-04-6
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Saracatinib/塞卡替尼 纯度/质量文件 产品仅供科研

货号：A154045 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
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• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >
产品名称 ALK1 ↓ ALK2 ↓ ALK3 ↓ ALK4 ↓ ALK6 ↓ Smad3 ↓ TGF-β ↓ TGFβRI/ALK5 ↓ TGFβRII ↓ 其他靶点 纯度
LDN193189 ++++

ALK1, IC50: 0.8 nM

 		++++

ALK2, IC50: 0.8 nM

 		+++

ALK3, IC50: 5.3 nM

 		+++

ALK6, IC50: 16.7 nM

 		99%+
LDN-212854 ++++

ALK1, IC50: 2.4 nM

 		++++

ALK2, IC50: 1.3 nM

 		+

ALK3, IC50: 85.8 nM

 		+

ALK4, IC50: 2133 nM

 		+

ALK5, IC50: 9276 nM

 		99%+
ML347 ++

ALK1, IC50: 46 nM

 		++

ALK2, IC50: 32 nM

 		98%
K02288 ++++

ALK1, IC50: 1.8 nM

 		++++

ALK2, IC50: 1.1 nM

 		++

ALK3, IC50: 34.4 nM

 		+++

ALK6, IC50: 6.4 nM

 		99%+
LDN-193189 2HCl ++++

ALK1, IC50: 0.8 nM

 		++++

ALK2, IC50: 0.8 nM

 		+++

ALK3, IC50: 5.3 nM

 		+++

ALK6, IC50: 16.7 nM

 		99%
LDN-214117 ++

ALK2, IC50: 24 nM

 		98%
DMH-1 +

ALK2, IC50: 107.9 nM

 		99%+
SB-505124 +

ALK4, IC50: 129 nM

 		++

ALK5, IC50: 47 nM

 		99%+
Vactosertib +++

ALK4, IC50: 13 nM

 		+++

ALK5, IC50: 11 nM

 		99%+
Alantolactone ✔ 98%
(E/Z)-SIS3 free base ✔ 97%
Pirfenidone ✔ 98%
Hesperetin ✔ 97%
RepSox ++++

TGFβR1(ALK5), IC50: 4 nM

 		98%
GW788388 +++

ALK5, IC50: 18 nM

 		98%
LY364947 ++

TGFβRI, IC50: 59 nM

 		+

TGFβRII, IC50: 0.4 μM

 		98%
SD-208 ++

TGF-βRI (ALK5), IC50: 48 nM

 		99%
SB-525334 +++

TGFβR1(ALK5), IC50: 14.3 nM

 		99%+
LY2109761 ++

TβRI, Ki: 38 nM

 		+

TβRII, Ki: 300 nM

 		99%+
Galunisertib ++

TβRI, IC50: 56 nM

 		98%
SB 431542 +

ALK5, IC50: 94 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
产品名称 Abl ↓ Bcr-Abl ↓ 其他靶点 纯度
NVP-BHG 712 +

c-Abl, IC50: 1.667 μM

 		99%+
KW-2449 +++

Abl (T315I), IC50: 4 nM

Abl, IC50: 14 nM

 		FLT3 99%+
Ponatinib ++++

Abl, IC50: 0.37 nM

 		98%
AT9283 99%+
Imatinib Mesylate +

v-Abl, IC50: 600 nM

 		c-Kit,PDGFR 99%
Danusertib ++

Abl, IC50: 25 nM

 		RET 99%+
Rebastinib ++++

u-Abl1 (T315I), IC50: 5 nM

p-Abl1 (native), IC50: 0.75 nM

 		Tie-2,FLT3 99%+
PP121 ++

Abl, IC50: 18 nM

 		VEGFR,PDGFR 99%+
GNF-7 +++

E255V, IC50: 122 nM

M351T, IC50: 133 nM

 		99%+
Olverembatinib dimesylate ++++

Abl (G250E), IC50: 0.35 nM

Abl, IC50: 0.34 nM

 		98%
Dasatinib monohydrate ++++

Abl , IC50: 0.6 nM

 		Src 98%
Dasatinib ++++

Abl, IC50: 0.6 nM

 		Src 98%
Bafetinib +++

Abl, IC50: 5.8 nM

 		98+%
GNF-2 +

Bcr-Abl (SUP-B15 cell line), IC50: 268 nM

Bcr-Abl (K562 cell line), IC50: 273 nM

 		98%+
Degrasyn +

Bcr-Abl, IC50: 1.8 μM

 		DUB/Deubiquitinase 99+%
GNF-5 ++

Bcr-Abl, IC50: 220 nM

 		99%
Radotinib ++

BCR-ABL1, IC50: 34 nM

 		98+%
PD173955 Src 99%+
Nilotinib ++

Bcr-Abl, IC50: <30 nM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
产品名称 Fyn ↓ Lck ↓ Lyn ↓ Src ↓ Yes ↓ 其他靶点 纯度
Saracatinib ++

Fyn, IC50: 10 nM

 		++++

LCK, IC50: <4 nM

 		+++

Lyn, IC50: 5 nM

 		++++

c-Src, IC50: 2.7 nM

 		99%+
SU6656 +

Fyn, IC50: 170 nM

 		+

Lyn, IC50: 130 nM

 		+

Src, IC50: 280 nM

 		++

YES, IC50: 20 nM

 		98%
PP1 +++

Fyn, IC50: 6 nM

 		+++

LCK, IC50: 5 nM

 		EGFR 99%+
PP2 +++

Fyn, IC50: 5 nM

 		++++

LCK, IC50: 4 nM

 		98%
WH-4-023 ++++

Lck, IC50: 2 nM

 		+++

Src, IC50: 6 nM

 		99%+
NVP-BHG 712 +

c-Src, IC50: 1.266 μM

 		99%+
CCT196969 ++

LCK, IC50: 0.02 μM

 		+

Src, IC50: 0.03 μM

 		98%
MNS +

Src, IC50: 29.3 μM

 		Syk,p97 98%
Tirbanibulin ++

Src (HuH7), GI50: 13 nM

Src (Hep 3B), GI50: 26 nM

 		99%+
PP121 ++

Src, IC50: 14 nM

 		VEGFR,PDGFR 99%+
Bosutinib ++++

Src, IC50: 1.2 nM

 		99%
Dasatinib monohydrate ++++

Src, IC50: 0.8 nM

 		98%
Quercetin ✔ Sirtuin,PKC 95%
Dasatinib ++++

Src, IC50: 0.8 nM

 		98%
Repotrectinib +++

Src, IC50: 5.3 nM

 		99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Saracatinib/塞卡替尼 生物活性

靶点

  • EGFR/ErbB1

    EGFR (L861Q), IC50:4 nM

    EGFR, IC50:5 nM

  • Fyn

    Fyn, IC50:10 nM

  • Src

    c-Src, IC50:2.7 nM

  • Lck

    LCK, IC50:<4 nM

  • Lyn

    Lyn, IC50:5 nM
描述 Saracatinib is a potent Src inhibitor with IC50 of 2.7 nM, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck and is less active for Abl and EGFR (L858R and L861Q).

Saracatinib/塞卡替尼 细胞实验

Cell Line
Concentration Treated Time Description References
DS fibroblasts 2 μM 24 h lowering pY682APP-βCTF levels and rescuing v-ATPase deficits Sci Adv. 2023 Jul 28;9(30):eadg1925.
SK-Hep-1 cells 1 mM 6 h Inhibits YAP-induced tumor cell migration Cell Death Dis. 2021 Dec 3;12(12):1126.
PLC5 cells 20 µM 24 h To investigate the effect of Saracatinib on STAT3 phosphorylation in PLC5 cells, results showed that Saracatinib decreased STAT3 phosphorylation. J Transl Med. 2021 Apr 1;19(1):138.
PLC/PRF/5 cells 1 mM 6 h To test the inhibitory effect of Saracatinib on YAP-induced HCC cell migration Cell Death Dis. 2021 Dec 3;12(12):1126.
CRC cell lines 0.0625–2 µM 72 h To evaluate the antiproliferative effects of Saracatinib on CRC cell lines, LS180, H508, and LS174T cell lines were sensitive to Saracatinib with an IC50 of 0.5 µM. Clin Cancer Res. 2010 Aug 15;16(16):4165-77.
SW620, SW480, H508, LS174T 1 µM 48 h To evaluate the effects of Saracatinib on the cell cycle, H508 and LS174T cell lines showed G1 cell cycle arrest after 48 h. Clin Cancer Res. 2010 Aug 15;16(16):4165-77.

Saracatinib/塞卡替尼 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Operant conditioning-induced habitual responding for ethanol Intraperitoneal injection 5 mg/kg Single administration, 2h or 30 min prior to testing To evaluate the effects of saracatinib on habitual ethanol-seeking and consumption in mice. Results showed that saracatinib did not significantly alter habitual ethanol-seeking or consumption at either the 2-h or 30-min pretreatment time points. Front Psychiatry. 2021 Aug 31;12:709559
Mice Ts2 mouse model Oral 5 mg/kg Twice daily for 4 weeks Decreasing pY682APP-βCTF levels and restoring v-ATPase function Sci Adv. 2023 Jul 28;9(30):eadg1925.
Mice A549 xenograft model Oral 50 mg/kg Once daily for two weeks To evaluate the effect of Saracatinib in combination with Tazemetostat and MK-2206 on tumor growth, the results showed that the combination significantly reduced tumor weight Nat Commun. 2021 Dec 3;12(1):6941.
Nude mice CRC cell line xenograft model Oral gavage 50 mg/kg Daily for 28 days To evaluate the antitumor effects of Saracatinib in a CRC xenograft model, LS180 and LS174T cell lines were sensitive to Saracatinib with significant tumor growth reduction. Clin Cancer Res. 2010 Aug 15;16(16):4165-77.

Saracatinib/塞卡替尼 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01144481 - Completed - Canada, Ontario ... 展开 >> University Health Network Toronto, Ontario, Canada, M5G 2C4 收起 <<
NCT00265876 Pancreatic Cancer Phase 1 Phase 2 Completed - Canada, British Columbia ... 展开 >> BCCA - Vancouver Cancer Centre Vancouver, British Columbia, Canada, V5Z 4E6 Canada, Ontario Ottawa Health Research Institute - General Division Ottawa, Ontario, Canada, K1H 8L6 Algoma District Cancer Program Sault Ste. Marie, Ontario, Canada, P6B 0A8 Univ. Health Network-Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 收起 <<
NCT01000896 Cancer Non Sm... 展开 >>all Cell Lung Cancer Epithelial Ovarian Cancer 收起 << Phase 1 Withdrawn(AstraZeneca has disc... 展开 >>ontinued the development of AZD0530. No new AstraZeneca-sponsored clinical studies will be initiated..) 收起 << March 2011 Japan ... 展开 >> Research Site Matsuyama, Ehime, Japan Research Site Fukuoka, Japan 收起 <<

Saracatinib/塞卡替尼 参考文献

[1]Green TP, Fennell M, et al. Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530. Mol Oncol. 2009 Jun;3(3):248-61.

[2]Chang YM, Bai L, et al. Src family kinase oncogenic potential and pathways in prostate cancer as revealed by AZD0530. Oncogene. 2008 Oct 23;27(49):6365-75.

Saracatinib/塞卡替尼 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.84mL

0.37mL

0.18mL

9.22mL

1.84mL

0.92mL

18.45mL

3.69mL

1.84mL

Saracatinib/塞卡替尼 技术信息

CAS号379231-04-6
分子式C27H32ClN5O5
分子量 542.03
SMILES Code CN1CCN(CC1)CCOC2=CC(OC3CCOCC3)=C4C(N=CN=C4NC5=C(C=CC6=C5OCO6)Cl)=C2
MDL No. MFCD09832698
别名 AZD0530
运输蓝冰
InChI Key OUKYUETWWIPKQR-UHFFFAOYSA-N
Pubchem ID 10302451
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, 2-8°C
溶解方案

DMSO: 50 mg/mL(92.25 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: Saracatinib | 379231-04-6 | AZD0530 | AZD 0530 | AZD-0530 | Src Inhibitor | Protein Tyrosine Kinase/RTK | Autophagy | Src | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Saracatinib/塞卡替尼 纯度/质量文件 | Saracatinib/塞卡替尼 亚型比较 | Saracatinib/塞卡替尼 生物活性 | Saracatinib/塞卡替尼 临床数据 | Saracatinib/塞卡替尼 参考文献 | Saracatinib/塞卡替尼 实验方案 | Saracatinib/塞卡替尼 技术信息

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