KJ Pyr 9 - CAS:581073-80-5

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KJ Pyr 9

目录号 : KM11726 CAS No. : 581073-80-5 纯度 : 98%

Data Sheet 产品使用指南

KJ Pyr 9 是 MYC 的抑制剂。体外实验中, KJ Pyr 9 抑制 MYC 的 K_d 值为 6.5±1.0 nM。

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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

KJ Pyr 9 is an inhibitor of MYC with a K_d of 6.5 nM in in vitro assay.

体外研究

KJ Pyr 9 (KJ-Pyr-9) interferes with MYC-MAX complex formation in the cell, as shown in a protein fragment complementation assay. KJ Pyr 9 specifically inhibits MYC-induced oncogenic transformation in cell culture; it has no or only weak effects on the oncogenic activity of several unrelated oncoproteins. KJ Pyr 9 preferentially interferes with the proliferation of MYC-overexpressing human and avian cells and specifically reduces the MYC-driven transcriptional signature. KJ Pyr 9 against three cell lines is tested known to be dependent on increased MYC activity: NCI-H460, MDA-MB-231, and SUM-159PT. The proliferation of all cell lines tested is inhibited, with IC₅₀ values between 5 and 10 μM. Additionally, the proliferation of Burkitt lymphoma cell lines, which show constitutively high expression of c-MYC, is more sensitive to KJ Pyr 9 (IC₅₀ values between 1 and 2.5 μM).

体内研究

To test the in vivo effectiveness of KJ Pyr 9 (KJ-Pyr-9), nude mice receive a xenograft of MDA-MB-231 cells suspended in Matrigel and injected s.c. into the left and right flanks. When the tumors have reached an average volume of 100 mm, mice are treated daily with 10 mg/kg KJ Pyr 9 or vehicle control by i.p. injection for 31 d. Inhibition of tumor growth by KJ Pyr 9 is noted after 8 d of treatment. By day 31, the tumor volume in the KJ Pyr 9-treated animals has not increased significantly. At the conclusion of the experiment the tumors are extracted and weighed. The weight measurements are in agreement with the volume determinations and confirmed the ability of KJ Pyr 9 to halt tumor growth.

分子式

C₂₂H₁₅N₃O₄

分子量

385.37

CAS号

581073-80-5

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 : 125 mg/mL (324.36 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5949 mL	12.9745 mL	25.9491 mL
5 mM	0.5190 mL	2.5949 mL	5.1898 mL
10 mM	0.2595 mL	1.2975 mL	2.5949 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 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (6.49 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.49 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 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。
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.49 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.49 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。
3.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.08 mg/mL (5.40 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (5.40 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 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。