1. Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. Anaplastic lymphoma kinase (ALK) mTOR PARP Caspase
  3. ALK-IN-26

ALK-IN-26 (compound 4a) 是 ALK 抑制剂,对 ALK 酪氨酸激酶的 IC50 值为7.0 μM。ALK-IN-26 有良好的药代动力学特性和血脑屏障通透性。ALK-IN-26 能够引起细胞凋亡、自噬和坏死。ALK-IN-26 能够用于胶质母细胞瘤研究。

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ALK-IN-26 Chemical Structure

ALK-IN-26 Chemical Structure

CAS No. : 2447607-85-2

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ALK-IN-26 is an ALK inhibitor with IC50 value of 7.0 μM for ALK tyrosine kinase. ALK-IN-26 has good pharmacokinetic properties and blood-brain barrier (BBB) permeability. ALK-IN-26 can induce apoptosis, autophagy and necrosis. ALK-IN-26 can be used in glioblastoma studies[1].

体外研究
(In Vitro)

ALK-IN-26 (0.5-2 μM, 24 h) 在 GL216 细胞中能够抑制 ALK 的活性[1]
ALK-IN-26 (0.5-10 μM, 24-72 h) 在 GL216、U87MG、Hela 细胞中能够抑制 GL216、U87MG 的活性,对 Hela 细胞活性的抑制有限[1]
ALK-IN-26 (0.5-2 μM, 24 h) 在 GL216 细胞中能够降低 mTOR 蛋白水平的表达[1]
ALK-IN-26 (0.5-2 μM, 24 h) 在 GL261 和 U87MG 细胞中显著降低 p-ERK1/2 蛋白水平、增强 p-JNK水平,对 p-AKT 和 p-STAT3 蛋白水平几乎不影响[1]
ALK-IN-26 (0.5-2 μM, 24 h) 在 GL261 细胞中能够诱导细胞自噬[1]
ALK-IN-26 (0.5 μM-2 μM, 24-72 h) 在 GL261 细胞中升高了 cleaved-PARP (c-PARP) 和 cleaved-caspase-3 (c-caspase 3) 蛋白水平[1]
ALK-IN-26 (0.5 μM-2 μM, 24-72 h) 在 GL261 细胞中引起凋亡[1]

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

Apoptosis Analysis[1]

Cell Line: GL261
Concentration: 0.5 μM, 1.0 μM, 2.0 μM
Incubation Time: 24 h, 48 h, 72 h
Result: Induced apoptosis of glioblastoma in a concentration- and time-dependent manner, and caused the cells (24.5%) entered the S phase but barely proceeded to the G2/M phase when treated with 1 μM for 72 h.

Cell Viability Assay[1]

Cell Line: GL216, U87MG, Hela
Concentration: 0.5 μM, 1.0 μM, 2.0 μM, 5 μM, 10 μM for GL216 and U87MG cells 5 μM, 10 μM, 20 μM, 40 μM, 80 μM, 160 μM for Hela cells
Incubation Time: 24 h, 48h, 72h
Result: Inhibited the activity of GL216 cells with the inhibition rate of cells at 80% when incubated with 2 μM for 72 h and inhibited U87MG cells viability with a dose- and time-dependent manner, while showed limited inhibition on Hela cells, even at 160 μM, the inhibition rate is less than 50%.
Can inhibit the activity of ALK tyrosine kinase with a dose-dependent manner.

Cell Autophagy Assay[1]

Cell Line: GL261
Concentration: 0.5 μM, 1.0 μM, 2.0 μM
Incubation Time: 24 h
Result: Induced autophagy death in glioblastoma cells.
体内研究
(In Vivo)

ALK-IN-26 (5 mg/kg, i.v., 单剂量) 在雄性 C57BL6/J 小鼠中有药代动力学特性[1]
ALK-IN-26 (20 mg/kg, i.p., 单剂量) 在雄性 C57BL6/J 小鼠中能够穿透血脑屏障[1]

在雄性小鼠 C57BL6/J 的药代动力学分析[1]

Pharmacokinetic property T1/2(h) Tmax(h) Cmax (ng/mL) AUC(0-8) (h*ng/mL) AUC(0-∞) (h*ng/mL) MRT(0-8) (h) MRT(0-∞) (h) V (L/kg) V2 (L/kg) bioavailablity F (%)
i.v.(5mg/kg) 1.13 0.08 1978.21 884.88 924.56 0.63 0.84 4.59 8.89 38.40
i.p.(5mg/kg) 3.55 0.58 117.57 339.79 420.50 2.25 4.60 / / /

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

Animal Model: Male C57BL/6J mice[1]
Dosage: 5 mg/kg
Administration: Intravenous injection (i.v.), Single dose
Result: Could be rapidly absorbed (Tmax = 0.58 h) with an acceptable half-life (T1/2 = 3.55 h) and bioavailability (F = 38.4%).
Animal Model: Male C57BL/6J mice[1]
Dosage: 20mg/kg
Administration: Intraperitoneal injection (i.p.), Single dose
Result: Could enter the body at concentrations up to 2.7μmol/kg (after 2 h administration at 20 mg/kg) and penetrate the blood-brain barrier.
分子量

405.51

Formula

C24H23NO3S

CAS 号
Unlabeled CAS

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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 125 mg/mL (308.25 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4660 mL 12.3302 mL 24.6603 mL
5 mM 0.4932 mL 2.4660 mL 4.9321 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, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 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

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

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, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4660 mL 12.3302 mL 24.6603 mL 61.6508 mL
5 mM 0.4932 mL 2.4660 mL 4.9321 mL 12.3302 mL
10 mM 0.2466 mL 1.2330 mL 2.4660 mL 6.1651 mL
15 mM 0.1644 mL 0.8220 mL 1.6440 mL 4.1101 mL
20 mM 0.1233 mL 0.6165 mL 1.2330 mL 3.0825 mL
25 mM 0.0986 mL 0.4932 mL 0.9864 mL 2.4660 mL
30 mM 0.0822 mL 0.4110 mL 0.8220 mL 2.0550 mL
40 mM 0.0617 mL 0.3083 mL 0.6165 mL 1.5413 mL
50 mM 0.0493 mL 0.2466 mL 0.4932 mL 1.2330 mL
60 mM 0.0411 mL 0.2055 mL 0.4110 mL 1.0275 mL
80 mM 0.0308 mL 0.1541 mL 0.3083 mL 0.7706 mL
100 mM 0.0247 mL 0.1233 mL 0.2466 mL 0.6165 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.

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产品名称:
ALK-IN-26
目录号:
HY-156432
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