RSM-932A TCD-717|cas:850807-63-5|西域试剂

RSM-932A TCD-717,99.60%

产品编号：Bellancom-101144| CAS NO：850807-63-5| 分子式：C₄₆H₃₈Br₂Cl₂N₄| 分子量：877.53

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-101144	￥1800.00	杭州北京（现货）
Bellancom-101144	￥3000.00	杭州北京（现货）
Bellancom-101144	￥6500.00	杭州北京（现货）
Bellancom-101144	￥9500.00	杭州北京（现货）
Bellancom-101144	￥13500.00	杭州北京（现货）

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RSM-932A TCD-717

产品介绍

RSM-932A (TCD-717) 是一种特异性 ChoKα 抑制剂，对人重组 ChoKα 和 ChoKβ 酶的 IC₅₀ 分别为 1 和 33 μM。RSM-932A 是针对 ChoKα 的“人类首创”化合物。RSM-932A 具有有效的体外抗肿瘤增殖和体内抗肿瘤活性，且显示低毒性^{[ 3]}。

生物活性

RSM-932A (TCD-717) is a specific ChoKα inhibitor with IC₅₀s of 1 and 33 μM for human recombinant ChoKα and ChoKβ enzymes, respectively. RSM-932A acts as the “first in humans” compound targeting ChoKα. RSM-932A is potent in vitro anti-proliferative and in vivo anti-tumoral activity against human xenografts in mice, showing high efficacy with low toxicity profiles.

体外研究

RSM-932A has a potent anti-proliferative activity against most tumor-derived cell lines tested, including those derived from breast, lung, colon, bladder, liver, ovary, bone, cervix, kidney, pancreas, melanoma, and brain tumors, with IC₅₀s of 1.3-7.1 μM for 72 hours.
RSM-932A (TCD-717; 2-4 µM; for 24 hours) promotes cell death of colon cancer cells.
RSM-932A (2-10 µM) exhibits a dosage-dependent decrease in the levels of thymidylate synthase (TS) and thymidine kinase (TK1) proteins proteins.
RSM-932A inhibits Streptococcus pneumoniae choline kinase (sChoK) with IC₅₀ of 0.5 μM in LDH/PK and colorimetric enzymatic assays.
The minimum inhibitory concentration (MIC) of RSM-932A for S. pneumoniae is 0.4 μM, and the minimum lethal concentration (MLC) is 1.6 μM.
RSM-932A is a comparatively potent inhibitor with the IC₅₀ of 1.75 μM in a steady-state reaction in which the concentration of Choline is equivalent to its K_m^[4].

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

Cell Proliferation Assay

Cell Line:	DLD-1, HT29, SW620 and HCT116 CRC cell lines and the non-tumourigenic CCD-841 cell line
Concentration:	2, 3, 4 µM
Incubation Time:	24 hours
Result:	Triggered to cell death.

Western Blot Analysis

Cell Line:	DLD-1, HT29 and SW620 cell lines
Concentration:	2, 4, 6, 8, 10 uM
Incubation Time:	24 hours
Result:	A dosage-dependent decrease in the levels of thymidylate synthase (TS) and thymidine kinase (TK1) proteins.

体内研究
(In Vivo)

RSM-932A exhibits a potent in vivo anticancer activity, and lack of toxicity at the effective doses.

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

Animal Model:	Athymic nu/nu mice, CD1 nude mice, and BALB/c nude (six-week-old) bearing human tumor xenografts (colon adenocarcinoma HT29, non-small cell lung cancer (NSCLC) H-460, breast adenocarcinoma MDA-MB-231)
Dosage:	7.5 mg/kg, 6 mg/kg, 5 mg/kg, 3 mg/kg, 1 mg/kg, 0.3 mg/kg
Administration:	Administration routes (intraperitoneal or intravenous), treatment schedule (5 consecutive days, 3 days per week, 2 days per week, 1 day per week)
Result:	The LD₅₀ was 10.9 mg/kg in mice. The effective dose used in the in vivo experiments was 7.5 mg/kg.

体内研究

RSM-932A exhibits a potent in vivo anticancer activity, and lack of toxicity at the effective doses.

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

Animal Model:	Athymic nu/nu mice, CD1 nude mice, and BALB/c nude (six-week-old) bearing human tumor xenografts (colon adenocarcinoma HT29, non-small cell lung cancer (NSCLC) H-460, breast adenocarcinoma MDA-MB-231)
Dosage:	7.5 mg/kg, 6 mg/kg, 5 mg/kg, 3 mg/kg, 1 mg/kg, 0.3 mg/kg
Administration:	Administration routes (intraperitoneal or intravenous), treatment schedule (5 consecutive days, 3 days per week, 2 days per week, 1 day per week)
Result:	The LD₅₀ was 10.9 mg/kg in mice. The effective dose used in the in vivo experiments was 7.5 mg/kg.

体内研究

RSM-932A exhibits a potent in vivo anticancer activity, and lack of toxicity at the effective doses.

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

Animal Model:	Athymic nu/nu mice, CD1 nude mice, and BALB/c nude (six-week-old) bearing human tumor xenografts (colon adenocarcinoma HT29, non-small cell lung cancer (NSCLC) H-460, breast adenocarcinoma MDA-MB-231)
Dosage:	7.5 mg/kg, 6 mg/kg, 5 mg/kg, 3 mg/kg, 1 mg/kg, 0.3 mg/kg
Administration:	Administration routes (intraperitoneal or intravenous), treatment schedule (5 consecutive days, 3 days per week, 2 days per week, 1 day per week)
Result:	The LD₅₀ was 10.9 mg/kg in mice. The effective dose used in the in vivo experiments was 7.5 mg/kg.

性状

Solid

溶解性数据

In Vitro:

DMSO : 16.67 mg/mL (19.00 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.1396 mL	5.6978 mL	11.3956 mL
5 mM	0.2279 mL	1.1396 mL	2.2791 mL
10 mM	0.1140 mL	0.5698 mL	1.1396 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 (sealed storage, away from moisture and 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 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.67 mg/mL (1.90 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (1.90 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 16.7 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