GNE-064|cas:1997321-20-6|西域试剂

GNE-064,99.75%

产品编号：Bellancom-149026| CAS NO：1997321-20-6| 分子式：C₁₇H₂₁N₅O₂| 分子量：327.38

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货号	价格	库存与货期
Bellancom-149026	￥3000.00	杭州北京（现货）
Bellancom-149026	￥4800.00	杭州北京（现货）
Bellancom-149026	￥9500.00	杭州北京（现货）
Bellancom-149026	￥14500.00	杭州北京（现货）

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GNE-064

产品介绍

GNE-064 (compound 5) 是一种选择性的，具有口服活性的以及高可溶性的 SMARCA4，SMARCA2 和 PBRM1 bromodomains 5 抑制剂。GNE-064 对 SMARCA4 具有抑制作用，其 IC₅₀ 值为 0.035 μM，对 SMARCA2 也具有抑制作用，其 EC₅₀ 值为 0.10 μM。GNE-064 对 SMARCA4，SMARCA2，PBRM1 bromodomains 5 和 PBRM1 bromodomains 2 的 K_d 值为 0.01，0.016，0.018 以及 0.049 μM。GNE-064 可以作为一种活性分子探针，用于活性分子合成的研究。

生物活性

GNE-064 (compound 5) is a selective, orally active and highly soluble inhibitor of SMARCA4, SMARCA2 and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC₅₀ of 0.035 μM and inhibits SMARCA2 with an EC₅₀ of 0.10 μM. GNE-064 possess K_ds with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of agent synthesis.

体外研究

GNE-064 (0-0.5 μM; 1 h) inhibits SMARCA2 in ZsGreen-SMARCA2 BD-expressing U2OS cells.

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

Cell Viability Assay

Cell Line:	ZsGreen-SMARCA2 BD-expressing U2OS cells
Concentration:	0-0.5 μM
Incubation Time:	1 hour
Result:	Inhibited SMARCA2 in ZsGreen-SMARCA2 BD-expressing U2OS cells with an EC₅₀ of 0.1 μM.

体内研究
(In Vivo)

GNE-064 (compound 5) (0.5 and 1.0 mg/kg; i.v. and p.o. once ) exibits ideal pharmacokinetics value in female CD-1 mice .

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

Animal Model:	Female CD-1 mice
Dosage:	0.5 mg/kg (i.v.) and 1.0 mg/kg (p.o.)
Administration:	Intravenous injection and oral gavage; 0.5 mg/kg and 1.0 mg/kg once
Result:	Showed a low unbound plasma clearance with 16 mL/min/kg, a reasonable half-life of 1.1 h and good oral bioavailability of 59%.

体内研究

GNE-064 (compound 5) (0.5 and 1.0 mg/kg; i.v. and p.o. once ) exibits ideal pharmacokinetics value in female CD-1 mice .

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

Animal Model:	Female CD-1 mice
Dosage:	0.5 mg/kg (i.v.) and 1.0 mg/kg (p.o.)
Administration:	Intravenous injection and oral gavage; 0.5 mg/kg and 1.0 mg/kg once
Result:	Showed a low unbound plasma clearance with 16 mL/min/kg, a reasonable half-life of 1.1 h and good oral bioavailability of 59%.

体内研究

GNE-064 (compound 5) (0.5 and 1.0 mg/kg; i.v. and p.o. once ) exibits ideal pharmacokinetics value in female CD-1 mice .

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

Animal Model:	Female CD-1 mice
Dosage:	0.5 mg/kg (i.v.) and 1.0 mg/kg (p.o.)
Administration:	Intravenous injection and oral gavage; 0.5 mg/kg and 1.0 mg/kg once
Result:	Showed a low unbound plasma clearance with 16 mL/min/kg, a reasonable half-life of 1.1 h and good oral bioavailability of 59%.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 125 mg/mL (381.82 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0546 mL	15.2728 mL	30.5455 mL
5 mM	0.6109 mL	3.0546 mL	6.1091 mL
10 mM	0.3055 mL	1.5273 mL	3.0546 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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式