2. Protein Tyrosine Kinase/RTK Apoptosis
  3. Src Apoptosis
  4. AZM475271

AZM475271  (Synonyms: M475271)

目录号: HY-13561 纯度: 99.89%
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AZM475271 (M475271) 是一种口服有效且具有选择性的 Src 激酶抑制剂。AZM475271 抑制 c-Src 激酶、Lck、c-yes 的磷酸化 (IC50 分别为 0.01、0.03、0.08 μM)。AZM475271 诱导细胞凋亡 (apoptosis)。AZM475271 可在体内外抑制肿瘤细胞增殖和迁移，并降低微血管密度。AZM475271 可使肿瘤细胞对 Gemcitabine (HY-17026) 的细胞毒性作用更敏感。

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AZM475271

AZM475271 Chemical Structure

CAS No. : 476159-98-5

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10 mM * 1 mL in DMSO ￥990
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5 mg ￥900
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10 mg ￥1400
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50 mg ￥4900
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AZM475271 相关抗体

Top Publications Citing Use of Products

查看 Src 亚型特异性产品:

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Lck Fyn Blk Hck Lyn Yes SRC-3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AZM475271 (M475271) is an orally active and selective Src kinase inhibitor. AZM475271 inhibits phosphorylation of c-Src kinase, Lck, c-yes (IC50s = 0.01, 0.03, 0.08 μM, respectively). AZM475271 induces apoptosis. AZM475271 reduces tumor cell proliferation and migration in vitro and in vivo, and reduces microvessel density (MVD). AZM475271 inhibits tumor growth and metastasis. AZM475271 sensitizes tumor cells to the cytotoxic effects of Gemcitabine (HY-17026)[1][2][3][4].

IC50 & Target

Lck

0.03 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 25 μM
Compound: AZM475271
Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay
[PMID: 30562697]
A549 IC50
0.48 μM
Compound: 35, M475271
Inhibition of A549 cell migration by microdroplet migration assay
Inhibition of A549 cell migration by microdroplet migration assay
[PMID: 17064066]
HCT-116 IC50
> 25 μM
Compound: AZM475271
Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay
[PMID: 30562697]
HCT-116 IC50
> 25 μM
Compound: AZM475271
Antiproliferative activity against p53-/- human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against p53-/- human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay
[PMID: 30562697]
MCF7 IC50
> 25 μM
Compound: AZM475271
Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay
[PMID: 30562697]
NHDF IC50
> 25 μM
Compound: AZM475271
Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay
[PMID: 30562697]
Sf9 IC50
5 nM
Compound: 56; AZM475271
Inhibition of human recombinant Src expressed in baculovirus infected Sf9 insect cells assessed as reduction in phosphorylation of polyglutamic acid/tyrosine incubated for 15 mins by ELISA
Inhibition of human recombinant Src expressed in baculovirus infected Sf9 insect cells assessed as reduction in phosphorylation of polyglutamic acid/tyrosine incubated for 15 mins by ELISA
[PMID: 30878832]
体外研究
(In Vitro)

AZM475271 可以抑制 c-Src3T3 (转染成纤维细胞，24 h，IC50 = 0.53 μM)、A549 (IC50 = 0.48 μM) 细胞增殖[1][2]。
AZM475271 (1-20 μM, 48 h) 在 15 μM 以下在体外对 L3.6pl 人胰腺癌细胞无抗增殖作用，但在 20 μM 时诱导细胞死亡[2]。
AZM475271 (5 μM, 12 h) 可诱导 L3.6pl 细胞凋亡，与 Gemcitabine 联合使用可增强凋亡作用[2]。
AZM475271 (0.1-5 μM, 4 h) 可抑制 L3.6pl 细胞迁移[2]。
AZM475271 (1-10 μM, 4 h）在 L3.6pl 细胞系中表现出对 Src 酪氨酸激酶活性的强烈剂量依赖性抑制[2]。
AZM475271有效阻断 TGF-β1 诱导的 Panc-1 细胞趋化作用，并抑制异位表达组成性活性 ALK5T204D 突变体的 Panc-1 细胞的高趋化作用活性。[3]。
AZM475271 (10-100 µM，24-72 h) 可抑制前列腺组织和 WPMY-1 细胞中的 SFK，降低前列腺条带的 α1-肾上腺素能和神经源性收缩[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

AZM475271 相关抗体:

Cell Proliferation Assay[2]

Cell Line: L3.6pl human pancreatic cancer cells
Concentration: 1, 5, 10, 15, 20 μM
Incubation Time: 48 h
Result: Showed no anti-proliferative effect on L3.6pl cells in vitro, although a rapid decrease in cell proliferation was detected at high concentrations (> 20 μM).
Microscopic investigation indicated the rapid inhibition of cell proliferation was caused by reduced cell numbers due to therapy-induced cell death.

Apoptosis Analysis[2]

Cell Line: L3.6pl human pancreatic cancer cells
Concentration: 5 μM
Incubation Time: 12 h
Result: Resulting in apoptosis in 12.6%, 11.0%, and 52.2% of the tumor cells in used alone group, Gemcitabine group and combination group, respectively.

Cell Migration Assay [2]

Cell Line: L3.6pl human pancreatic cancer cells
Concentration: 0.1, 1, 5 μM
Incubation Time: 4 h
Result: Produced significant inhibition of L3.6pl tumor cell migration at 1 and 5μM.

Western Blot Analysis[2]

Cell Line: L3.6pl human pancreatic cancer cells
Concentration: 1, 2.5, 5, 10 μM
Incubation Time: 4 h
Result: Demonstrated strong dose-dependent inhibition of Src tyrosine kinase activity.
Maximum reduction of Src kinase activity was observed with ≥ 5 μM (4.76-fold reduction).
体内研究
(In Vivo)

AZM475271 (50 mg/kg；口服；每日一次，共 32 天) 在注射了 L3.6pl 细胞的无胸腺裸鼠中可缩小肿瘤体积，并且与 Gemcitabine (100 mg/kg；腹腔注射；每周两次，共 32 天) 联用可增强该效果[2]。
AZM475271 (50 mg/kg；口服；单次给药) 在健康裸鼠体内 24 小时内具有生物有效血浆浓度[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Healthy nude mice[2]
Dosage: 50 mg/kg
Administration: Oral gavage (p.o.); once
Result: The plasma concentration was 32.1 μM (14.206 ng/mL), 20 μM (8879 ng/mL), and 11.7 μM (5187 ng/mL) at 2, 6, and 24 hours after p.o..
Animal Model: Athymic nude mice (injected with 1 X 106 viable L3.6pl cells)[2]
Dosage: 50 mg/kg
Administration: Oral gavage (p.o.); once daily for 32 days
Result: The median tumor volume was significantly less than that in control mice.
After combination therapy, primary pancreatic tumor volume was significantly less than that seen with Gemcitabine alone.
The incidence of liver metastasis was markedly reduced.
Did not significantly change animal weight when used alone, but reduced animal weight combined with Gemcitabine.
Has antiproliferative effect alone and in combination with Gemcitabine.
Induce apoptosis in pancreatic carcinoma cells in vivo, maximum apoptotic effect was observed in the combination with Gemcitabine.
Reduced microvessel density (MVD) alone and no significant difference in combination with Gemcitabine.
分子量

442.94

Formula

C23H27ClN4O3
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 42 mg/mL (94.82 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2576 mL 11.2882 mL 22.5764 mL
5 mM 0.4515 mL 2.2576 mL 4.5153 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

AZM475271 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2576 mL 11.2882 mL 22.5764 mL 56.4411 mL
5 mM 0.4515 mL 2.2576 mL 4.5153 mL 11.2882 mL
10 mM 0.2258 mL 1.1288 mL 2.2576 mL 5.6441 mL
15 mM 0.1505 mL 0.7525 mL 1.5051 mL 3.7627 mL
20 mM 0.1129 mL 0.5644 mL 1.1288 mL 2.8221 mL
25 mM 0.0903 mL 0.4515 mL 0.9031 mL 2.2576 mL
30 mM 0.0753 mL 0.3763 mL 0.7525 mL 1.8814 mL
40 mM 0.0564 mL 0.2822 mL 0.5644 mL 1.4110 mL
50 mM 0.0452 mL 0.2258 mL 0.4515 mL 1.1288 mL
60 mM 0.0376 mL 0.1881 mL 0.3763 mL 0.9407 mL
80 mM 0.0282 mL 0.1411 mL 0.2822 mL 0.7055 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZM475271476159-98-5M475271AZM 475271AZM-475271M 475271M-475271SrcApoptosisanti-proliferationmigrationcytotoxickinaseL3.6plInhibitorinhibitorinhibit

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