Ivaltinostat formic CG-200745 formic|西域试剂

Ivaltinostat formic CG-200745 formic,99.36%

产品编号：Bellancom-16138A| 分子式：C₂₅H₃₅N₃O₆| 分子量：473.56

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-16138A		￥9900.00	杭州北京（现货）
Bellancom-16138A		￥16000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Ivaltinostat formic CG-200745 formic

产品介绍

Ivaltinostat (CG-200745) formic 是一种口服有效的泛 HDAC 抑制剂，具有异羟肟酸部分，可在催化袋底部结合锌。Ivaltinostat formic 抑制组蛋白 H3 和微管蛋白的脱乙酰作用。Ivaltinostat formic 诱导 p53 的积累，促进 p53 依赖性反式激活，并增强 MDM2 和 p21 (Waf1/Cip1) 蛋白的表达。Ivaltinostat formic 可增强 Gemcitabine 耐药细胞对 Gemcitabine (HY-16138) 和 5-Fluorouracil (5-FU; HY-90006) 的敏感性。Ivaltinostat formic 诱导凋亡并具有抗肿瘤作用。

生物活性

Ivaltinostat (CG-200745) formic is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat formic inhibits deacetylation of histone H3 and tubulin. Ivaltinostat formic induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat formic enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine (HY-16138) and 5-Fluorouracil (5-FU; HY-90006). Ivaltinostat formic induces apoptosis and has anti-tumour effects.

体外研究

Ivaltinostat (CG-200745; 0.01-100 μM; 48 hours) formic inhibits growth of prostate cancer cells (LNCaP, DU145 and PC3 cells). Ivaltinostat (1, 10 μM; 24, 48 hours) formic increases sub-G1 population, and activates caspase-9, -3 and -8.
Ivaltinostat (0.001-100 μM; for 72 hours) inhibits proliferation of cholangiocarcinoma cells (IC₅₀s of 0.63, 0.93, and 1.80 μM for SNU-1196, SNU-1196/GR, SNU-308 cells, respectively).
Ivaltinostat (0-10 μM; 48 hours) formic reduces the Calu6 cells proliferation to 40% of untreated cells^[4].
Ivaltinostat (3 μM; 1-24 hours) formic significantly increases Calu6 cells proportion in G2/M phase (69%)^[4].
Ivaltinostat (0-10 μM; 1-24 hours) formic treatment with low concentration significantly increases the acetylation of histone H3 and H4 in Calu6 cells at various sites in a time-dependent manner up to 24 hours after treatment^[4].

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

Cell Proliferation Assay^[4]

Cell Line:	Calu6 cells
Concentration:	0-10 μM
Incubation Time:	48 hours
Result:	Reduced the cell proliferation to 40% of untreated cells.

Cell Cycle Analysis^[4]

Cell Line:	Calu6 cells
Concentration:	3 μM
Incubation Time:	1, 8, 12, 24 hours
Result:	Increased significantly cell proportion in G2/M phase (69%).

Western Blot Analysis^[4]

Cell Line:	Calu6 cells
Concentration:	3 μM
Incubation Time:	1, 4, 8, 12, 24 hours
Result:	Increased the acetylation of histone H3 and H4 at various sites in a time-dependent manner.

体内研究
(In Vivo)

Ivaltinostat (CG-200745; p.o.; 30 mg/kg/day; for 7 days) formic attenuates oxidative stress, inflammatory cytokines, and adhesion molecules in UUO kidneys^[5].

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

Animal Model:	Male 8-week-old C57BL/6 J mice weighing 20~22 g of unilateral ureteral obstruction (UUO)^[5]
Dosage:	30 mg/kg
Administration:	PO; daily; for 7 days
Result:	Attenuated oxidative stress, inflammatory cytokines and adhesion molecules in UUO kidneys.

体内研究

Ivaltinostat (CG-200745; p.o.; 30 mg/kg/day; for 7 days) formic attenuates oxidative stress, inflammatory cytokines, and adhesion molecules in UUO kidneys^[5].

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

Animal Model:	Male 8-week-old C57BL/6 J mice weighing 20~22 g of unilateral ureteral obstruction (UUO)^[5]
Dosage:	30 mg/kg
Administration:	PO; daily; for 7 days
Result:	Attenuated oxidative stress, inflammatory cytokines and adhesion molecules in UUO kidneys.

体内研究

Ivaltinostat (CG-200745; p.o.; 30 mg/kg/day; for 7 days) formic attenuates oxidative stress, inflammatory cytokines, and adhesion molecules in UUO kidneys^[5].

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

Animal Model:	Male 8-week-old C57BL/6 J mice weighing 20~22 g of unilateral ureteral obstruction (UUO)^[5]
Dosage:	30 mg/kg
Administration:	PO; daily; for 7 days
Result:	Attenuated oxidative stress, inflammatory cytokines and adhesion molecules in UUO kidneys.

性状

Oil

溶解性数据

In Vitro:

H₂O : 50 mg/mL (105.58 mM; Need ultrasonic)

DMSO : 50 mg/mL (105.58 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1117 mL	10.5583 mL	21.1166 mL
5 mM	0.4223 mL	2.1117 mL	4.2233 mL
10 mM	0.2112 mL	1.0558 mL	2.1117 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 (sealed storage, away from moisture)。-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： PBS
Solubility: 50 mg/mL (105.58 mM); Clear 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 (5.28 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.28 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
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.28 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
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.28 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。