1. Epigenetics
  2. Histone Demethylase
  3. T-3775440 hydrochloride

T-3775440 hydrochloride 

目录号: HY-103085 纯度: 99.13%
产品使用指南

T-3775440 (hydrochloride) 是一种赖氨酸特异性脱甲基酶1 (LSD1) 的不可逆性抑制剂,其 IC50 值为 2.1 nM。

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T-3775440 hydrochloride Chemical Structure

T-3775440 hydrochloride Chemical Structure

CAS No. : 1422535-52-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3520
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5 mg ¥3200
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10 mg ¥4800
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25 mg ¥10500
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50 mg ¥15000
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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

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

T-3775440 (hydrochloride) is an irreversible lysine-specific histone demethylase (LSD1) inhibitor with an IC50 value of 2.1 nM.

IC50 & Target

IC50: 2.1 nM (LSD1)[1].

体外研究
(In Vitro)

T-3775440 demonstrates irreversible inhibition of recombinant human LSD1, with a kinact/KI value of 1.7×105 (sec−1 M−1). T-3775440 is highly selective for LSD1 relative to other monoamine oxidases (e.g., MAO-A and MAO-B), with an IC50 value of 2.1 nM). T-3775440 blocks the proliferation of several cell lines as quickly as day 3 of treatment. Notably, the granulocyte/macrophage markers CD86 and CD11b are commonly upregulated on both TF-1a and HEL92.1.7 cells in response to T-3775440 treatment, whereas the erythroid markers CD235a and CD71 are downregulated by this treatment. In CMK11-5 cells, CD86 mRNA expression is also clearly upregulated by T-3775440 in a concentration-dependent manner, although only a modest increase in cell surface CD86 expression is observed. T-3775440 treatment disrupts the LSD1-GFI1B association in a concentration-dependent manner. T-3775440 decreases LSD1 binding but not GFI1B binding and increases the level of dimethylated H3K4 at the PI16 locus[1].

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

体内研究
(In Vivo)

T-3775440 upregulates CD86 mRNA expression in tumor xenografts of HEL92.1.7 cells in a dose-dependent manner following the oral administration of single doses ranging from 3 to 30 mg/kg. To investigate target engagement of this compound in tumors, PI16 expression levels is tested as a direct biomarker. As expected, PI16 suppression is dramatically reversed by T-3775440 treatment. In a TF-1a (AEL) tumor xenograft model, T-3775440 exhibits significant antitumor effects, with 15-day T/C values of 15.6% and <0% at doses of 20 and 40 mg/kg, respectively. T-3775440 also exhibits potent antitumor effects in an additional AEL model of HEL 92.1.7 and an AMKL model of CMK11-5, leading to nearly complete tumor growth suppression during the dosing period. It is found that in mice, T-3775440 treatment results in a transient reduction in platelets, followed by a significant rebound; this is considered a mechanism-based adverse effect of LSD1 inhibition. On a dosing schedule comprising 5 days on/2 days off, a statistically significant difference in body weight is observed between vehicle- and T-3775440–treated tumor xenograft model mice at higher doses. However, efficacious T-3775440 doses are tolerated in all subcutaneous tumor xenograft models[1].

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

分子量

346.85

Formula

C18H23ClN4O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen, away from moisture

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

溶解性数据
In Vitro: 

DMSO : ≥ 30.18 mg/mL (87.01 mM)

H2O : 8.33 mg/mL (24.02 mM; ultrasonic and warming and heat to 60°C)

* "≥" 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 2.8831 mL 14.4155 mL 28.8309 mL
5 mM 0.5766 mL 2.8831 mL 5.7662 mL
10 mM 0.2883 mL 1.4415 mL 2.8831 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°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)。-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。

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: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.21 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.21 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
  • 2.

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

    Solubility: ≥ 2.5 mg/mL (7.21 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.21 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 μL 20% 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
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.21 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.21 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    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 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
Cell Assay
[1]

The human leukemia cell lines TF-1a, HEL92.1.7, CMK11-5 and M07e are used. All cells are grown in RPMI1640 plus 10% FBS and maintained in a humidified incubator at 37°C and 5% CO2. To assess cell proliferation and viability in human leukemia cell lines, compounds (e.g T-3775440) are added with different concentrations (T-3775440: 0, 10, 50 nM) at 24 h after cell seeding. After the incubation period, cells are lysed with CellTiter-Glo, and luminescent signals are detected using an ARVO MX1420 microplate reader. For cell-cycle analysis, cells are fixed overnight with 70% ethanol. Fixed cells are stained with propidium iodide and analyzed on a FACSCalibur or FACSVerse flow cytometer[1].

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

Animal Administration
[1]

Mice[1]
Female C.B17/Icr-scid/scid Jcl mice are used and maintained under specific pathogen-free conditions. AML cells (2×106 cells) in Matrigel are inoculated subcutaneously into the left flanks of 6- to 7-week-old mice (day 0). Mice are randomized when the mean tumor volume reached approximately 150 to 350 mm3. Subsequently, mice are administrated with vehicle or T-3775440 single doses ranging from 3 to 30 mg/kg once daily on 5 days on/2 days off schedule for 2 weeks. Twice weekly, tumors are measured with vernier calipers, and tumor volumes are calculated[1].

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

参考文献

纯度: 99.13%

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产品名称:
T-3775440 hydrochloride
目录号:
HY-103085
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