A-366|cas:1527503-11-2|西域试剂

A-366,98.02%

产品编号：Bellancom-12583| CAS NO：1527503-11-2| 分子式：C₁₉H₂₇N₃O₂| 分子量：329.44

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货号	价格	库存与货期
Bellancom-12583	￥750.00	杭州北京（现货）
Bellancom-12583	￥1000.00	杭州北京（现货）
Bellancom-12583	￥4000.00	杭州北京（现货）

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A-366

产品介绍

A-366 是一种高效、高选择性的肽竞争性组蛋白甲基转移酶 G9a 抑制剂，对 G9a 和 GLP 的 IC₅₀ 分别为 3.3 和 38 nM。A-366 比其他 21 种甲基转移酶具有 1000 倍以上的选择性。A-366 是一种有效的 Spindlin1-H3K4me3 相互作用的抑制剂 (IC₅₀=182.6 nM)。A-366 对人 H3R (K_i=17 nM) 表现出很高的亲和力，并且在组胺能和多巴胺能受体家族的亚群间表现出亚型选择性。

生物活性

A-366 is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC₅₀s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC₅₀=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (K_i=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families^[4].

体外研究

A-366 (0.01-10 μM; 14 days) induces differentiation and affects viability in MV4;11 cells^[4].
A-366 (0.3-3 μM; 72 hours) reduces the total levels of H3K9me2 in a time and concentration dependent manner with a cellular EC50 of ~300 nM in PC-3 prostate adenocarcinoma cells. A-366 (0.01-10 μM; 4 days; HL-60 cells) results in a dose-dependent differentiation and a corresponding decrease in proliferation. DNA content analysis of A-366-treated HL-60 cells showed an accumulation of cells in G1 consistent with cytostasis^[4].

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

Cell Viability Assay^[4]

Cell Line:	MV4;11 cells
Concentration:	0.01-10 μM
Incubation Time:	14 days
Result:	Resulted in inhibited proliferation and a decrease in viability corresponding to the dose response observed for CD11b staining.

体内研究
(In Vivo)

A-366 (30 mg/kg; osmotic mini-pump; daily for 14 days) treatment of MV4;11 xenografts elicits growth inhibition^[4].

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

Animal Model:	6-8 week old SCID-beige female mice (MV4;11 xenografts)^[4]
Dosage:	30 mg/kg
Administration:	By osmotic mini-pump; daily for 14 days
Result:	A modest 45% tumor growth inhibition resulting from A-366 treatment in this model.

体内研究

A-366 (30 mg/kg; osmotic mini-pump; daily for 14 days) treatment of MV4;11 xenografts elicits growth inhibition^[4].

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

Animal Model:	6-8 week old SCID-beige female mice (MV4;11 xenografts)^[4]
Dosage:	30 mg/kg
Administration:	By osmotic mini-pump; daily for 14 days
Result:	A modest 45% tumor growth inhibition resulting from A-366 treatment in this model.

体内研究

A-366 (30 mg/kg; osmotic mini-pump; daily for 14 days) treatment of MV4;11 xenografts elicits growth inhibition^[4].

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

Animal Model:	6-8 week old SCID-beige female mice (MV4;11 xenografts)^[4]
Dosage:	30 mg/kg
Administration:	By osmotic mini-pump; daily for 14 days
Result:	A modest 45% tumor growth inhibition resulting from A-366 treatment in this model.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (151.77 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0355 mL	15.1773 mL	30.3545 mL
5 mM	0.6071 mL	3.0355 mL	6.0709 mL
10 mM	0.3035 mL	1.5177 mL	3.0355 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： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (7.59 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.59 mM，饱和度未知) 的澄清溶液。
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
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (7.59 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.59 mM，饱和度未知) 的澄清溶液。
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 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