1. Protein Tyrosine Kinase/RTK
  2. FLT3
  3. TCS 359

TCS 359 是一种 2-酰基氨基噻吩-3-甲酰胺,是一种有效的选择性 FLT3 抑制剂,IC50 为 42 nM。TCS 359 抑制 MV4-11 细胞增殖,IC50 为 340 nM。

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TCS 359 Chemical Structure

TCS 359 Chemical Structure

CAS No. : 301305-73-7

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10 mM * 1 mL in DMSO ¥660
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5 mg ¥375
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10 mg ¥600
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50 mg ¥1900
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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TCS 359, a 2-acylaminothiophene-3-carboxamide, is a potent and selective FLT3 inhibitor with an IC50 of 42 nM. TCS 359 inhibits MV4-11 cell proliferation with an IC50 of 340 nM[1].

IC50 & Target

IC50: 42 nM (FLT3)[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HL-60 IC50
> 100 μM
Compound: TCS 359
Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
K562 IC50
> 100 μM
Compound: TCS 359
Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
KCL-22 IC50
> 100 μM
Compound: TCS 359
Antiproliferative activity against human KCL-22 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human KCL-22 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
KG-1 IC50
> 100 μM
Compound: TCS 359
Antiproliferative activity against human KG-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human KG-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
KG-1a IC50
> 100 μM
Compound: TCS 359
Antiproliferative activity against human KG-1a cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human KG-1a cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
MOLM-13 IC50
0.31 μM
Compound: TCS 359
Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
MOLT-4 IC50
> 100 μM
Compound: TCS 359
Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
MV4-11 IC50
0.322 μM
Compound: TCS 359
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
NOMO-1 IC50
> 100 μM
Compound: TCS 359
Antiproliferative activity against human NOMO-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human NOMO-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
OCI-AML2 IC50
> 100 μM
Compound: TCS 359
Antiproliferative activity against human OCI-AML2 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human OCI-AML2 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
THP-1 IC50
> 100 μM
Compound: TCS 359
Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
分子量

360.43

Formula

C18H20N2O4S

CAS 号
性状

固体

颜色

White to yellow

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 : 14.29 mg/mL (39.65 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 2.7745 mL 13.8723 mL 27.7446 mL
5 mM 0.5549 mL 2.7745 mL 5.5489 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

动物实验:

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: 1.43 mg/mL (3.97 mM); 悬浊液; 超声助溶

    此方案可获得 1.43 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    1 mL 工作液为例,取 100 μL 14.3 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% Corn Oil

    Solubility: ≥ 1.43 mg/mL (3.97 mM); 澄清溶液

    此方案可获得 ≥ 1.43 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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)。

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

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

纯度: 99.89%

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 2.7745 mL 13.8723 mL 27.7446 mL 69.3616 mL
5 mM 0.5549 mL 2.7745 mL 5.5489 mL 13.8723 mL
10 mM 0.2774 mL 1.3872 mL 2.7745 mL 6.9362 mL
15 mM 0.1850 mL 0.9248 mL 1.8496 mL 4.6241 mL
20 mM 0.1387 mL 0.6936 mL 1.3872 mL 3.4681 mL
25 mM 0.1110 mL 0.5549 mL 1.1098 mL 2.7745 mL
30 mM 0.0925 mL 0.4624 mL 0.9248 mL 2.3121 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:
TCS 359
目录号:
HY-13907
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