NCT-503|cas:1916571-90-8|西域试剂

NCT-503,99.55%

产品编号：Bellancom-101966| CAS NO：1916571-90-8| 分子式：C₂₀H₂₃F₃N₄S| 分子量：408.48

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货号	价格	库存与货期
Bellancom-101966	￥660.00	杭州北京（现货）
Bellancom-101966	￥1000.00	杭州北京（现货）
Bellancom-101966	￥1950.00	杭州北京（现货）
Bellancom-101966	￥3100.00	杭州北京（现货）
Bellancom-101966	￥4750.00	杭州北京（现货）

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NCT-503

产品介绍

NCT-503磷酸甘油酸脱氢酶 (PHGDH) 抑制剂，IC₅₀ 值为2.5 µM。

生物活性

NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC₅₀ of 2.5 µM.

体外研究

Human phosphoglycerate dehydrogenase (PHGDH) catalyzes the first, rate-limiting step in the canonical glucose-derived serine synthesis pathway. NCT-503, a PHGDH inhibitor, inhibits serine synthesis from 3-phosphoglycerate in cells (IC₅₀=2.5 µM). NCT-503 is inactive against a panel of other dehydrogenases and shows minimal cross-reactivity in a panel of 168 GPCRs. Competition studies of NCT-503 against 3-phosphoglycerate (3-PG) and the co-substrate NAD⁺ reveal a non-competitive mode of inhibition with respect to both 3-PG and NAD⁺. NCT-503 has EC₅₀s of 8–16 µM for the PHGDH-dependent cell lines, a 6- to 10-fold higher EC₅₀ for MDA-MB-231 cells, and no toxicity towards other PHGDH-independent cell lines.

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

体内研究

NCT-503 exhibits favorable absorption, distribution, metabolism and excretion (ADME) properties. NCT-503 has good exposure, half-life (2.5 hr) and C_max (20 µM in plasma) following intraperitoneal administration with significant partitioning into the liver and brain. NCT-503 treatment reduces the growth and weight of PHGDH-dependent MDA-MB-468 xenografts but does not affect the growth or weight of PHGDH-independent MDA-MB-231 xenografts.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (122.41 mM; Need ultrasonic)

Ethanol : 13.33 mg/mL (32.63 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	2.4481 mL	12.2405 mL	24.4810 mL
5 mM	0.4896 mL	2.4481 mL	4.8962 mL
10 mM	0.2448 mL	1.2241 mL	2.4481 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。-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： 50% PEG300 50% saline
Solubility: 10 mg/mL (24.48 mM); Suspended 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 (6.12 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.12 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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% corn oil
Solubility: ≥ 2.5 mg/mL (6.12 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.12 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。
4.

请依序添加每种溶剂： 0.5% methylcellulose 0.2% Tween 80
Solubility: 2 mg/mL (4.90 mM); Suspended solution; Need ultrasonic