TRi-1|cas:246020-68-8|西域试剂

TRi-1,99.80%

产品编号：Bellancom-125006| CAS NO：246020-68-8| 分子式：C₁₂H₉ClN₂O₅S| 分子量：328.73

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-125006	￥1800.00	杭州北京（现货）
Bellancom-125006	￥2800.00	杭州北京（现货）
Bellancom-125006	￥6500.00	杭州北京（现货）
Bellancom-125006	￥9500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

TRi-1

产品介绍

TRi-1 是有效的、特异性的、不可逆的胞质硫氧还蛋白还原酶1 (TXNRD1) 的抑制剂，其 IC₅₀ 值为 12 nM。TRi-1 有抗肿瘤活性，且线粒体毒性很小。

生物活性

TRi-1 is a potent, specific and irreversible inhibitor of cytosolic thioredoxin reductase 1 (TXNRD1), with an IC₅₀ of 12 nM. TRi-1 has little mitochondrial toxicity for anticancer therapy.

体外研究

TRi-1 (0.679 and 6.79 μM; 6 h) has no effect on cellular glutathione (GSH) concentrations in FaDu cells, efficiently activates JNK and p38 phosphorylation.
TRi-1 (2 μM) irreversibly inhibit TXNRD1 in an NADPH-dependent manner.
TRi-1 (0.1-10 μM; 0-10 h) increases cellular H₂O₂ production in cultured FaDu cells in a concentration- and time-dependent manner.
TRi-1 (10 nM-100 μM; 48 h) shows cytotoxicity toward cancer cells.

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

Western Blot Analysis

Cell Line:	FaDu cells
Concentration:	0.679 and 6.79 μM
Incubation Time:	6 h
Result:	Efficiently activated JNK and p38 phosphorylation.

Cell Cytotoxicity Assay

Cell Line:	Leukemia, non-small cell lung, CNS, colon, melanoma, ovarian, renal, prostate and breast cancer cells
Concentration:	10 nM-100 μM
Incubation Time:	48 h
Result:	Displayed potency against every cell line tested, with an average growth inhibition to 50% (GI₅₀) of 6.31 μM.

体内研究
(In Vivo)

TRi-1 (10 mg/kg; i.v.; twice a day for 4 days or 5 mg/kg; i.p.; twice a week for 3 weeks) impaires growth and viability of human tumor xenografts and syngeneic mouse tumors.

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

Animal Model:	SCID mice bearing established human FaDu cell xenografts
Dosage:	10 mg/kg
Administration:	Intravenous injection, twice a day for 4 days
Result:	Resulted in decreased tumor growth compared to vehicle controls within four days with no signs of overt toxicity or changes in mouse weight relative to vehicle control.

Animal Model:	PyMT-MMTV mice that spontaneously develop malignant breast cancer tumors
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection, twice a week for 3 weeks
Result:	Impaired tumor growth, significantly reduced tumor volumes.

体内研究

TRi-1 (10 mg/kg; i.v.; twice a day for 4 days or 5 mg/kg; i.p.; twice a week for 3 weeks) impaires growth and viability of human tumor xenografts and syngeneic mouse tumors.

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

Animal Model:	SCID mice bearing established human FaDu cell xenografts
Dosage:	10 mg/kg
Administration:	Intravenous injection, twice a day for 4 days
Result:	Resulted in decreased tumor growth compared to vehicle controls within four days with no signs of overt toxicity or changes in mouse weight relative to vehicle control.

Animal Model:	PyMT-MMTV mice that spontaneously develop malignant breast cancer tumors
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection, twice a week for 3 weeks
Result:	Impaired tumor growth, significantly reduced tumor volumes.

体内研究

TRi-1 (10 mg/kg; i.v.; twice a day for 4 days or 5 mg/kg; i.p.; twice a week for 3 weeks) impaires growth and viability of human tumor xenografts and syngeneic mouse tumors.

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

Animal Model:	SCID mice bearing established human FaDu cell xenografts
Dosage:	10 mg/kg
Administration:	Intravenous injection, twice a day for 4 days
Result:	Resulted in decreased tumor growth compared to vehicle controls within four days with no signs of overt toxicity or changes in mouse weight relative to vehicle control.

Animal Model:	PyMT-MMTV mice that spontaneously develop malignant breast cancer tumors
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection, twice a week for 3 weeks
Result:	Impaired tumor growth, significantly reduced tumor volumes.

性状

Solid

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (190.13 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0420 mL	15.2100 mL	30.4201 mL
5 mM	0.6084 mL	3.0420 mL	6.0840 mL
10 mM	0.3042 mL	1.5210 mL	3.0420 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 (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。

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: ≥ 2.08 mg/mL (6.33 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.33 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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% corn oil
Solubility: ≥ 2.08 mg/mL (6.33 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.33 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。