NCT-503

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NCT-503

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。

CAS NO:

1916571-90-8

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 aphosphoglycerate dehydrogenase(PHGDH) inhibitor with anIC₅₀of 2.5 μM.

IC₅₀& Target

IC50: 2.5 μM (PHGDH)^[1]

体外研究
(In Vitro)

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 EC₅₀for MDA-MB-231 cells, and no toxicity towards other PHGDH-independent cell lines^[1].

体内研究
(In Vivo)

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^[1].

分子量

408.48

性状

Solid

Formula

C₂₀H₂₃F₃N₄S

CAS 号

1916571-90-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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℃)

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℃, 6 months; -20℃, 1 month。-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： 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

*以上所有助溶剂都可在本网站选购。