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Tandutinib hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tandutinib hydrochloride图片
CAS NO:2438900-70-8
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
MLN518 hydrochloride
CT53518 hydrochloride
产品介绍
Tandutinib hydrochloride (MLN518 hydrochloride) 是一种有效和选择性的FLT3的抑制剂,其IC50为 0.22 μM,并且还抑制c-KitPDGFR,其IC50分别为 0.17 μM 和 0.20 μM。Tandutinib hydrochloride 可用于急性骨髓性白血病,并具有穿越血脑屏障的能力。
生物活性

Tandutinib hydrochloride (MLN518 hydrochloride) is a potent and selective inhibitor of theFLT3with anIC50of 0.22 μM, and also inhibitsc-KitandPDGFRwithIC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib hydrochloride can be used for acute myelogenous leukemia (AML)[1][2]. Tandutinib hydrochloride has the ability to cross the blood-brain barrier[3].

IC50& Target[1]

FLT3

0.22 μM (IC50)

c-Kit

0.17 μM (IC50)

PDGFR

0.2 μM (IC50)

体外研究
(In Vitro)

Tandutinib (0-3 μM; 30 minutes; Ba/F3 cells) treatment inhibits IL-3-independent cell growth and FLT3-ITD autophosphorylation with anIC50of 10-100 nM in Ba/F3 cells expressing different FLT3-ITD mutants[1].
Tandutinib (1 μM; 24-96 hours; Molm-14 and THP-1 AML cells) treatment induces apoptosis in FLT3-ITD-positive AML cells[1].
In human FLT3-ITD-positive AML cell lines, Tandutinib inhibits FLT3-ITD phosphorylation (IC50of ~30 nM). As with Erk2, a constitutively high level of Akt phosphorylation is readily detected and is efficiently blocked by pretreatment of the Molm-14 cells with 100-300 nM Tandutinib[1].
Tandutinib inhibits cell proliferation of the FLT3-ITD-positive Molm-13 and Molm-14 with anIC50of 10 nM. And signaling through the MAP kinase and PI3 kinase pathways[1].

Apoptosis Analysis[1]

Cell Line:Molm-14 and THP-1 AML cells
Concentration:1 μM
Incubation Time:24 hours, 48 hours, 72 hours, 96 hours
Result:Induced apoptosis in FLT3-ITD-positive AML cells.

Western Blot Analysis[1]

Cell Line:Ba/F3 cells
Concentration:0 μM, 0.003 μM, 0.01 μM, 0.03 μM, 0.1 μM, 1 μM and 3 μM
Incubation Time:30 minutes
Result:In Ba/F3 cells expressing different FLT3-ITD mutants, inhibited IL-3-independent cell growth and FLT3-ITD autophosphorylation.
体内研究
(In Vivo)

Tandutinib (60 mg/kg; oral gavage; daily; for 35 days; athymic nude mice) treatment causes a statistically significant increase in survival that was extended on average by 20 days[1].

Animal Model:Athymic nude mice injected with Ba/F3 cells[1]
Dosage:60 mg/kg
Administration:Oral gavage; daily; for 35 days
Result:Caused a statistically significant increase in survival that was extended on average by 20 days.
Clinical Trial
分子量

599.16

性状

Solid

Formula

C31H43ClN6O4

CAS 号

2438900-70-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL(166.90 mM)

H2O : 100 mg/mL(166.90 mM;Need ultrasonic)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.6690 mL8.3450 mL16.6900 mL
5 mM0.3338 mL1.6690 mL3.3380 mL
10 mM0.1669 mL0.8345 mL1.6690 mL
*

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

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

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 100 mg/mL (166.90 mM); Clear solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.17 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.17 mM,饱和度未知) 的澄清溶液。

    以 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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (4.17 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.17 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在本网站选购。