GSK2643943A|cas:2449301-27-1|西域试剂

GSK2643943A,98.28%

产品编号：Bellancom-111458| CAS NO：2449301-27-1| 分子式：C₁₇H₁₂FN₃| 分子量：277.30

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货号	价格	库存与货期
Bellancom-111458	￥2000.00	杭州北京（现货）
Bellancom-111458	￥3300.00	杭州北京（现货）
Bellancom-111458	￥7000.00	杭州北京（现货）
Bellancom-111458	￥11000.00	杭州北京（现货）
Bellancom-111458	￥19000.00	杭州北京（现货）

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GSK2643943A

产品介绍

GSK2643943A 是一种靶向 USP20 的去泛素化酶 (DUB) 抑制剂。GSK2643943A 对 USP20/Ub-Rho 具有亲和力, 其 IC₅₀ 值为 160 nM。GSK2643943A 具有抗肿瘤作用，可用于口腔鳞状细胞癌 (OSCC) 的研究。

生物活性

GSK2643943A is a deubiquitinating enzyme (DUB) inhibitor targeting USP20. GSK2643943A has affinity with an IC₅₀ of 160 nM for USP20/Ub-Rho. GSK2643943A has anti-tumor efficacy and can be used for the research of oral squamous cell carcinoma (OSCC) .

体外研究

GSK2643943A blocks the USP20-mediated cleavage of protein-ubiquitin bonds.
GSK2643943A (1 μM, 5 μM; overnight) renders SCC9 cells more susceptible to oHSV-1 induced oncolysis.
GSK2643943A (1μM) leds to a notable increase of virus yields in SCC9 with 0.01 MOI T1012G infection.

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

Cell Viability Assay

Cell Line:	SCC9 cells
Concentration:	1 μM, 5 μM (GSK+0.01 MOI T1012) 1 μM (GSK+0.01 MOI/ 1 MOI T1012)
Incubation Time:	overnight
Result:	Displayed a significant drop in viability (R50%) (5 μM GSK+0.01 MOI T1012 infection) and 50% loss of SCC9 viability (1 μM GSK+0.01 MOI T1012 infection) . Remarkably reduced the viability of SCC9 upon exposure to 1 MOI T1012G infection.

Western Blot Analysis

Cell Line:	SCC9 cells
Concentration:	1 μM
Incubation Time:	3h, 9 h and 20 h
Result:	Generally up-regulated the expression of viral proteins at various phases.

RT-PCR

Cell Line:	SCC9 cells
Concentration:	1 μM
Incubation Time:	9 h
Result:	Significantly increased the accumulation of viral ICP8 and VP16 Mrna in SCC9 cells.

体内研究
(In Vivo)

GSK2643943A (5 mg/kg, i.p., daily, for 6 days) potentiates oHSV-1-induced oncolysis in SCC9 tumors.
GSK2643943A (2.5 mg/kg, i.p., daily, for 9 days) plays a regulatory role in oHSV-1 T1012G replication and oncolysis in SCC7 cells.

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

Animal Model:	The subcutaneous xenograft model. (SCC9 or SCC7 cells (8×10⁶ cells or 1×10⁶ cells), 5-week-old, female, BALB/c nude mice or C3H/HeN mice, four groups, n = 6-7, per group)
Dosage:	5 mg/kg
Administration:	GSK2643943A (alone): intraperitoneal administration, daily, for 6 days. GSK2643943A (combination): intraperitoneal administration, daily for 6 days + intratumoral injection with 50 mL of 1×10⁶ PFU T1012G in PBS on day 1, day 4, and day 7.
Result:	Caused a visible drop of tumor volumes and significantly reduced the tumor volumes in mice with combined treatment of GSK2643943A and oHSV-1 T1012G. Increased slightly viral ICP0 and gD mRNA accumulation in SCC9 tumors.

Animal Model:	The SCC7 mouse model.
Dosage:	2.5 mg/kg
Administration:	GSK2643943A (alone): intraperitoneal administration, daily, for 9 days. GSK2643943A (combination): intraperitoneal administration, daily, for 9 days + intratumoral injection, with 50 mL of 1×10⁷ PFU T1012G in PBS on days 1, 4, 7, and 10.
Result:	Caused a visible drop of tumor volumes, significantly reduced in mice with combined treatment of GSK and oHSV-1 T1012G. Increased slightly viral ICP0 and gD mRNA accumulation in SCC7 tumors.

体内研究

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

Animal Model:	The subcutaneous xenograft model. (SCC9 or SCC7 cells (8×10⁶ cells or 1×10⁶ cells), 5-week-old, female, BALB/c nude mice or C3H/HeN mice, four groups, n = 6-7, per group)
Dosage:	5 mg/kg
Administration:	GSK2643943A (alone): intraperitoneal administration, daily, for 6 days. GSK2643943A (combination): intraperitoneal administration, daily for 6 days + intratumoral injection with 50 mL of 1×10⁶ PFU T1012G in PBS on day 1, day 4, and day 7.
Result:	Caused a visible drop of tumor volumes and significantly reduced the tumor volumes in mice with combined treatment of GSK2643943A and oHSV-1 T1012G. Increased slightly viral ICP0 and gD mRNA accumulation in SCC9 tumors.

Animal Model:	The SCC7 mouse model.
Dosage:	2.5 mg/kg
Administration:	GSK2643943A (alone): intraperitoneal administration, daily, for 9 days. GSK2643943A (combination): intraperitoneal administration, daily, for 9 days + intratumoral injection, with 50 mL of 1×10⁷ PFU T1012G in PBS on days 1, 4, 7, and 10.
Result:	Caused a visible drop of tumor volumes, significantly reduced in mice with combined treatment of GSK and oHSV-1 T1012G. Increased slightly viral ICP0 and gD mRNA accumulation in SCC7 tumors.

体内研究

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

Animal Model:	The subcutaneous xenograft model. (SCC9 or SCC7 cells (8×10⁶ cells or 1×10⁶ cells), 5-week-old, female, BALB/c nude mice or C3H/HeN mice, four groups, n = 6-7, per group)
Dosage:	5 mg/kg
Administration:	GSK2643943A (alone): intraperitoneal administration, daily, for 6 days. GSK2643943A (combination): intraperitoneal administration, daily for 6 days + intratumoral injection with 50 mL of 1×10⁶ PFU T1012G in PBS on day 1, day 4, and day 7.
Result:	Caused a visible drop of tumor volumes and significantly reduced the tumor volumes in mice with combined treatment of GSK2643943A and oHSV-1 T1012G. Increased slightly viral ICP0 and gD mRNA accumulation in SCC9 tumors.

Animal Model:	The SCC7 mouse model.
Dosage:	2.5 mg/kg
Administration:	GSK2643943A (alone): intraperitoneal administration, daily, for 9 days. GSK2643943A (combination): intraperitoneal administration, daily, for 9 days + intratumoral injection, with 50 mL of 1×10⁷ PFU T1012G in PBS on days 1, 4, 7, and 10.
Result:	Caused a visible drop of tumor volumes, significantly reduced in mice with combined treatment of GSK and oHSV-1 T1012G. Increased slightly viral ICP0 and gD mRNA accumulation in SCC7 tumors.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 125 mg/mL (450.78 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	3.6062 mL	18.0310 mL	36.0620 mL
5 mM	0.7212 mL	3.6062 mL	7.2124 mL
10 mM	0.3606 mL	1.8031 mL	3.6062 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: ≥ 2.08 mg/mL (7.50 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (7.50 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: 2.08 mg/mL (7.50 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (7.50 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 20.8 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