1. TGF-beta/Smad Stem Cell/Wnt
  2. TGF-β Receptor TGF-beta/Smad
  3. ALK5-IN-34

ALK5-IN-34 是一种选择性的激活素受体样激酶 (ALK) 抑制剂,具有口服活性。ALK5-IN-34 可以抑制激活素受体样激酶的活性,IC50 值 ≤10 nM。ALK5-IN-34 还具有抑制肿瘤生长的作用,可用于癌症等增殖性疾病的研究。

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ALK5-IN-34 Chemical Structure

ALK5-IN-34 Chemical Structure

CAS No. : 2785430-90-0

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查看 TGF-β Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ALK5-IN-34 is an selective orally active activin receptor-like kinase (ALK) inhibitor. ALK5-IN-34 can inhibit the activity of ALK5-IN-34 with an IC50 value of ≤10 nM. ALK5-IN-34 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer[1].

IC50 & Target[1]

ALK5

<10 nM (IC50)

体外研究
(In Vitro)

ALK5-IN-34 (EX-11) has kinase inhibition of ALK5 with an IC50 value of ≤10 nM[1].
ALK5-IN-34 has kinase selectivity of ALK2/ALK5 with an IC50 value of <100 nM[1].
ALK5-IN-34 shows TGFB-RI inhibition (RD-SMAD receptor activity) with an IC50 value of ≤100 nM[1].
ALK5-IN-34 (1 μM-10 nM) inhibits the expression of TGF-β-mediated alpha-SMA in a full concentration-dependent[1].
ALK5-IN-34 (30, 300 and 3000 nM) suppresses the Treg frequency in a dose dependent manner[1].
ALK5-IN-34 (0-0.1 μM; for 6 days or 7 days) inhibits FOXL2CI34W-driven growth in KGN and COV434 cells with IC50 values of 140 nM and >10 μM, respectively[1].
ALK5-IN-34 (10, 100 and 1000 nM; 2 h) shows a dose-dependent decrease in pSmad2 in KGN cell line[1].
ALK5-IN-34 (30, 300 nM; 24 h) reverses the upregulation of gene expression in dose dependentent[1].
ALK5-IN-34 (30, 300 nM; 24 h) increases HLA class I expression in dose-dependent[1].

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

Cell Viability Assay[1]

Cell Line: KGN and COV434 cell lines
Concentration: 0-0.1 μM
Incubation Time: for 6 days or 7 days
Result: Inhibited FOXL2 CI34W -driven growth.

RT-PCR[1]

Cell Line: Human primary dermal fibroblasts
Concentration: 30, 300 nM
Incubation Time: 24 h
Result: Reversed the upregulation of gene expression with TGFB stimulation.
体内研究
(In Vivo)

ALK5-IN-34 (EX-11) (oral; 10-100 mg/kg) reduces the phopho SMAD2 levels (p-SMAD2) in a dose dependent manner in A549 murine xenograft model[1].
ALK5-IN-34 (oral; 75 mg/kg; 0-24 h) shows reversely correlated between PK and tumor PD (pSMAD2 levels)[1].
ALK5-IN-34 (oral; 150 mg/kg; bid; for 22 days) increases overall survival in ES-2 ovarian cancer mouse xenograft model and can delay progression[1].
ALK5-IN-34 (p.o.; 75, 150 mg/kg; twice a day; for 21days) shows tumor growth inhibition (TGI) and increases the survival when combining with anti-PD-L1/anti-PD-1 in Syngeneic TNBC Model and in Subcutaneous Cloudman S91 melanoma model[1].
ALK5-IN-34 (oral; 300, 1000 mg/kg; bid for 5 days) has good tolerability and safety margin in Tolerability Model[1].

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

Animal Model: A549 murine xenograft model[1]
Dosage: 10, 50, 75 and 100 mg/kg
Administration: oral gavage
Result: Exhibited 92.5% inhibition based upon the average p-SMAD2 levels (75 mg/kg).
Animal Model: EMT6 Syngeneic TNBC Model[1]
Dosage: 75, 150 mg/kg
Administration: p.o., twice a day, for 21days
Result: Resulted significantly tumor growth inhibition (TGI) by 37% at 150 mg/kg.
Result in significant tumor growth inhibition (TGI) with combination of anti-PD-LI and resulted in a significant increase in mean survival by 37%.
Resulted in significant TGI by 34% with combination of anti-PD-1 and resulted in significant increase in mean survival by 26%.
Decreased the intra-tumoral pressure.
Animal Model: Cachexia Model[1]
Dosage: 150 mg/kg
Administration: oral gavage, twice a day for 22 days
Result: Showed reduction in total fluid volume and high whole limb weights.
分子量

413.48

Formula

C23H23N7O

CAS 号
性状

固体

颜色

Light yellow to green yellow

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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (241.85 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 2.4185 mL 12.0925 mL 24.1850 mL
5 mM 0.4837 mL 2.4185 mL 4.8370 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。-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

In Vivo:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 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,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制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

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (6.05 mM); 澄清溶液; 超声助溶

    此方案可获得 2.5 mg/mL的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (6.05 mM); 澄清溶液; 超声助溶

    此方案可获得 2.5 mg/mL的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
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
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
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。-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 2.4185 mL 12.0925 mL 24.1850 mL 60.4624 mL
5 mM 0.4837 mL 2.4185 mL 4.8370 mL 12.0925 mL
10 mM 0.2418 mL 1.2092 mL 2.4185 mL 6.0462 mL
15 mM 0.1612 mL 0.8062 mL 1.6123 mL 4.0308 mL
20 mM 0.1209 mL 0.6046 mL 1.2092 mL 3.0231 mL
25 mM 0.0967 mL 0.4837 mL 0.9674 mL 2.4185 mL
30 mM 0.0806 mL 0.4031 mL 0.8062 mL 2.0154 mL
40 mM 0.0605 mL 0.3023 mL 0.6046 mL 1.5116 mL
50 mM 0.0484 mL 0.2418 mL 0.4837 mL 1.2092 mL
60 mM 0.0403 mL 0.2015 mL 0.4031 mL 1.0077 mL
80 mM 0.0302 mL 0.1512 mL 0.3023 mL 0.7558 mL
100 mM 0.0242 mL 0.1209 mL 0.2418 mL 0.6046 mL
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    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:
ALK5-IN-34
目录号:
HY-151289
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