DCH36_06|cas:593273-05-3|西域试剂

DCH36_06,99.22%

产品编号：Bellancom-139108| CAS NO：593273-05-3| 分子式：C₁₈H₁₃ClN₂O₃S| 分子量：372.83

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货号	价格	库存与货期
Bellancom-139108	￥1800.00	杭州北京（现货）
Bellancom-139108	￥3200.00	杭州北京（现货）
Bellancom-139108	￥5300.00	杭州北京（现货）
Bellancom-139108	￥9500.00	杭州北京（现货）

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DCH36_06

产品介绍

DCH36_06 是一种有效的选择性 p300/CBP 抑制剂，对 p300 和 CBP 的 IC₅₀ 分别为 0.6 μM 和 3.2 μM。DCH36_06 介导的 p300/CBP 抑制导致白血病细胞中 H3K18 的低乙酰化。抗肿瘤活性。

生物活性

DCH36_06 is a potent and selective p300/CBP inhibitor with IC₅₀s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity.

体外研究

DCH36_06 (6.7-20 μM; 24-48 hours) treatment arrests cell cycle at G1 phase and induces apotosis in a dose-dependent manner in leukemic cells.
DCH36_06 (5-10 μM; 24 hours) treatment significantly activates the cleavage of pro-caspase 3, pro-caspase 9 and PARP1 at dose-dependent manner.
DCH36_06 shows potent antiproliferative activity against tested leukemia cell lines (CEM, MOLT3, MOLT4, Jurkat, MV4-11, THP-1, RS4; 11, KOPN8, Kasumi-1 and K562 cells) in a dose-dependent manner with IC50 values at single-digit micromolar range.

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

Cell Cycle Analysis

Cell Line:	MV4-11 cells
Concentration:	6.7 μM, 20 μM
Incubation Time:	24 hours, 48 hours
Result:	Dose-dependently arrested cell cycle at G1 phase.

Apoptosis Analysis

Cell Line:	MV4-11 cells
Concentration:	6.7 μM, 20 μM
Incubation Time:	24 hours, 48 hours
Result:	Significantly induced apoptosis.

Western Blot Analysis

Cell Line:	MV4-11 cells
Concentration:	5 μM, 10 μM
Incubation Time:	24 hours
Result:	Significantly activated the cleavage of pro-caspase 3, pro-caspase 9 and PARP1 at dose-dependent manner.

体内研究
(In Vivo)

DCH36_06 (25-50 mg/kg; intraperitoneal injection; every two days; for 20 days) blocks the leukemic xenograft growth in mice.

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

Animal Model:	MV4-11 xenograft nude mice
Dosage:	25 mg/kg, 50 mg/kg
Administration:	Intraperitoneal injection; every two days; for 20 days
Result:	The tumor growth rate showed significant reduction in dose-dependent manner.

体内研究

DCH36_06 (25-50 mg/kg; intraperitoneal injection; every two days; for 20 days) blocks the leukemic xenograft growth in mice.

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

Animal Model:	MV4-11 xenograft nude mice
Dosage:	25 mg/kg, 50 mg/kg
Administration:	Intraperitoneal injection; every two days; for 20 days
Result:	The tumor growth rate showed significant reduction in dose-dependent manner.

体内研究

DCH36_06 (25-50 mg/kg; intraperitoneal injection; every two days; for 20 days) blocks the leukemic xenograft growth in mice.

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

Animal Model:	MV4-11 xenograft nude mice
Dosage:	25 mg/kg, 50 mg/kg
Administration:	Intraperitoneal injection; every two days; for 20 days
Result:	The tumor growth rate showed significant reduction in dose-dependent manner.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (335.27 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6822 mL	13.4109 mL	26.8219 mL
5 mM	0.5364 mL	2.6822 mL	5.3644 mL
10 mM	0.2682 mL	1.3411 mL	2.6822 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。

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 (5.58 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.58 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 (5.58 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (5.58 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