Pulrodemstat benzenesulfonate - CAS:2097523-60-7

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Pulrodemstat benzenesulfonate (Synonyms:CC-90011 benzenesulfonate; LSD1-IN-7 benzenesulfonate)

目录号 : KM4762 CAS No. : 2097523-60-7 纯度 : 97%

Data Sheet 产品使用指南

CC-90011 benzenesulfonate 是一种有效的，选择性的，可逆的和具有口服活性的赖氨酸特异性脱甲基酶-1 (LSD1) 抑制剂，IC₅₀ 为 0.25 nM。CC-90011 benzenesulfonate 对 LSD2，MOA-A 和 MAO-B 的酶抑制作用较小。CC-90011 benzenesulfonate 诱导急性髓细胞性白血病 (AML)和小细胞肺癌 (SCLC) 细胞分化，并具有有效的抗癌活性。

规格	价格	是否有货
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10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

CC-90011 benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC₅₀ of 0.25 nM. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.

体外研究

CC-90011 (Compound 11) shows potent induction of on-target cellular differentiation marker CD11b in THP-1 cell line with an EC₅₀ of 7 nM, antiproliferative activity in AML kasumi-1 cells with an EC₅₀ of 2 nM.
Suppression of GRP is observed with treatment of CC-90011 (4 days) in a dose-dependent manner and at pharmacologically useful concentrations (EC₅₀=3 nM, H209 and 4 nM, H1417). CC-90011 (12 days) treatment of SCLC cells results in potent antiproliferative activity (EC₅₀=6 nM, H1417) that correlated with GRP suppression.

体内研究

CC-90011 (5 mg/kg; oral administration; daily; for 30 days; for 30 days) treatment inhibits tumor growth in patient-derived xenograft SCLC models.
CC-90011 (once a day; for 4 days) treatment results in robust downregulation of GRP mRNA levels at 2.5 mg/kg and maximum suppression of GRP at 5 mg/kg in a SCLC human tumor xenograft (H1417) mice.
After i.v. administration, CC-90011 (Compound 11; 5 mg/kg) has systemic clearance of 32.4 mL/min/kg, elimination half-life of 2 h, and a high volume of distribution of 7.5 L/kg. CC-90011 (Compound 11; 5 mg/kg) is readily absorbed after oral administration with an AUC_0-24h of 1.8 μM·h, C/sub>max of 0.36 μM, and oral bioavailability of 32%.

Animal Model:	BALB/c nude mice bearing small cell lung carcinoma (SCLC)
Dosage:	5 mg/kg
Administration:	Oral administration; daily; for 30 days
Result:	Showed a tumor growth inhibition (TGI) of 78% at 5 mg/kg with no body weight loss.

分子式

C₃₀H₂₉F₂N₅O₅S

分子量

609.64

CAS号

2097523-60-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (102.52 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6403 mL	8.2016 mL	16.4031 mL
5 mM	0.3281 mL	1.6403 mL	3.2806 mL
10 mM	0.1640 mL	0.8202 mL	1.6403 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 (3.41 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.41 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。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.41 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.41 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。