CPI-1612 - CAS:2374971-81-8

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CPI-1612

目录号 : KM7996 CAS No. : 2374971-81-8

Data Sheet 产品使用指南

CPI-1612 是一种高效的具有口服活性的 EP300/CBP 组蛋白乙酰转移酶 (HAT) 抑制剂，对于 EP300 HAT 的 IC₅₀ 值为 8.1 nM。CPI-1612 具有抗癌活性。

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10mg		In-stock
25mg		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

CPI-1612 is a highly potent, orally active EP300/CBP histone acetyltransferase (HAT) inhibitor with an IC₅₀ of 8.1 nM for EP300 HAT. CPI-1612 has an anticancer activity.

体外研究

CPI-1612 inhibits full length EP300 and full length CBP with IC₅₀ values <0.5 nM and 2.9 nM, respectively.
CPI-1612 inhibits H3K18Ac MSD (H3K18 = histone 3 lysine 18, MSD = meso scale discovery) and JEKO-1 cell proliferation with with IC₅₀ values 14 nM and <7.9 nM, respectively.
CPI-1612 (compound 17) shows weak activity in a hERG binding assay (IC₅₀ = 10.4 μM) and displayed moderate inhibition of CYP2C8 (IC₅₀ = 1.9 μM) and CYP2C19 (IC₅₀ = 2.7 μM).

体内研究

CPI-1612 (compound 17; 0.5 mg/kg; oral administration; twice a day; for 4 weeks) treatment shows 67% tumor growth inhibition (TGI) with concomitant reduction of H3K27Ac in plasma and reduction of H3K18Ac in the tumor.
While the oral exposure of CPI-1612 (compound 17) in dogs (0.5 mg/kg IV; 1.0 mg/kg PO; clearance = 0.42 L/h/kg, V_ss = 3.7 L/kg, T_1/2 = 5.5 h, F% = 71; AUC/dose = 1691 h·mg/mL) and mice (1 mg/kg IV; 5 mg/kg PO; clearance = 3.8 L/h/kg, V_ss = 2.0 L/kg, T_1/2 = 0.98 h, F% = 79; AUC/dose = 211 h·mg/mL) is good, the exposure in rats is limited by poor bioavailability (1.0 mg/kg IV; 5.0 mg/kg PO; clearance = 2.6 L/h/kg, V_ss = 1.8 L/kg, T_1/2 = 1.2 h, F% = 9; AUC/dose = 35.6 h·mg/mL).
A single dose of CPI-1612 is administered orally to CD-1 mice and brain and plasma exposures of CPI-1612 are measured at 0.25, 0.5, 1.0, 2.0, 4.0, and 8.0 h. CPI-1612 is highly brain-penetrant, showing a brain-to-plasma ratio of 0.35 after a single oral dose.

Animal Model:	C57B6 mice injected with JEKO-1 cells
Dosage:	0.5 mg/kg
Administration:	Oral administration; twice a day; for 4 weeks
Result:	Showed 67% tumor growth inhibition (TGI) at a dose of 0.5 mg/kg.

分子式

C₂₇H₂₆N₆O

分子量

450.53

CAS号

2374971-81-8

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 : 100 mg/mL (221.96 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2196 mL	11.0980 mL	22.1961 mL
5 mM	0.4439 mL	2.2196 mL	4.4392 mL
10 mM	0.2220 mL	1.1098 mL	2.2196 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: 5 mg/mL (11.10 mM); Suspended solution; Need ultrasonic

此方案可获得 5 mg/mL (11.10 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 50.0 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。
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 5 mg/mL (11.10 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (11.10 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 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。