BAY-3827 - CAS:2377576-35-5

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BAY-3827

目录号 : KP12714 CAS No. : 2377576-35-5

Data Sheet 产品使用指南

BAY-3827 是强效的、选择性的 AMPK 抑制剂，IC₅₀ 值为 1.4 nM (10 µM ATP) 和 15 nM (2 mM ATP)。BAY-3827 对其他 331 种被测激酶的选择性超过 500 倍相比于 AMPK。AMPK 抑制乙酰 CoA 羧化酶 1 的磷酸化，并在雄激素依赖的前列腺癌细胞株中显示出强效的抗增殖活性。

规格	价格	是否有货	数量
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock

加入购物车大包装询价

Other Forms of Rapamycin:

BAY-3827 In-stock
XMD-17-51 In-stock
N,N-Didesethyl Sunitinib Hydrochloride In-stock
XMD-17-51 Trifluoroacetate In-stock
Ligupurpuroside A In-stock

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生物活性

BAY-3827 is a potent and selective AMPK inhibitor with IC₅₀ values of 1.4 nM at low (10 µM ATP concentration) and 15 nM at high (2 mM ATP concentration). BAY-3827 shows over 500-fold selectivity for most of the 331 kinases. BAY-3827 prevents phosphorylation of acetyl-CoA carboxylase 1 and shows strongest anti-proliferative activity in androgen-dependent prostate cancer cell lines.

体外研究

BAY-3827 (0-200 μM) inhibits AMPK kinase activity with IC50 values of 1.4 nM and 15 nM, respectively, under low (10 μM) and high (2 mM) ATP conditions. BAY-3827 (0-200 μM) inhibited the activity of Aurora A, Flt3, c-Met, and Rsk4 under 10 μM ATP conditions, with IC50 values of 1324 nM, 124 nM, 788 nM, and 36 nM, respectively. BAY-3827 (overnight) significantly reduced the phosphorylation of ACC1 Ser79 in LNCaP and VCaP cells, with weaker effects in IMR-32 and Colo320 cells [1].
BAY-3827 (0-10 nM; 6 days) showed significant inhibitory effects on LNCaP and VCaP cells [1].
BAY-3827 (1 and 5 μM; Inhibiting LIPE gene expression at 24 and 48 hours, reducing the expression of serine/threonine kinase AKT3, and blocking the expression of several genes in the mitochondrial carnitine palmitoyltransferase (CPT) family involved in acylcarnitine formation in VCaP cells [1].
BAY-3827 (5 μM; 2-4 days) significantly increased lipid droplet formation in VCaP cells compared to androgen treatment alone [1].

Cell Proliferation Assay

Cell Line:	LNCaP, VCaP, 22Rv1, C4-2B, PC-3 and DU-145 prostate cancer cell lines
Concentration:	0-10 nM
Incubation Time:	6 d
Result:	Showed strong inhibitory effects for LNCaP and VCaP cells, two prostate cancer cell lines with IC₅₀ values of 0.28 and 1.71 nM, respectily. Inhibited proliferation of 22Rv1 cells with an IC₅₀ value of 5.55 nM.

分子式

C₂₇H₂₅FN₆O

分子量

468.53

CAS号

2377576-35-5

中文名称

BAY-3827

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO: 25 mg/mL (53.36 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	2.1343 mL	10.6717 mL	21.3434 mL
5 mM	0.4269 mL	2.1343 mL	4.2687 mL
10 mM	0.2134 mL	1.0672 mL	2.1343 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。