KGP94|cas:1131456-28-4|西域试剂

KGP94,99.53%

产品编号：Bellancom-118762| CAS NO：1131456-28-4| 分子式：C₁₄H₁₂BrN₃OS| 分子量：350.23

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货号	价格	库存与货期
Bellancom-118762	￥2900.00	杭州北京（现货）
Bellancom-118762	￥4300.00	杭州北京（现货）
Bellancom-118762	￥7700.00	杭州北京（现货）
Bellancom-118762	￥10500.00	杭州北京（现货）

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KGP94

产品介绍

KGP94 是一种特异的 cathepsin L 抑制剂，IC₅₀为 189 nM。KGP94 抑制转移癌的运动性和侵袭性，对人类细胞的毒性低 (GI₅₀=26.9µM)。

生物活性

KGP94 is a selective inhibitor of cathepsin L with an IC₅₀ of 189 nM. KGP94 inhibits migration and invasion of metastatic carcinoma and shows low cytotoxicity (GI₅₀=26.9 µM) against various human cell lines.

体外研究

KGP94 (10 or 20 μM, 24 h) reduces expression of M2 (macrophage) markers (Arginase-1 and CD206) and cells invasion of primary bone marrow-derived macrophages or Raw264.7.
KGP94 (25 μM, 24 h) impairs the incasive capacities of both prostate and breat cancer cells by 53% and 88%, respectively^[4].
KGP94 (25 μM, 24 h) suppresses secreted CTSL activity by 94% and 92% in PC-3ML and MDA-MB-231, repsectively^[4].

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

Cell Invasion Assay^[4]

Cell Line:	PC-3ML, MDA-MB-231
Concentration:	10 μM, 25 μM
Incubation Time:	24 hours
Result:	Attenuated migration and invasion of prostate and breast cancer cells.

体内研究
(In Vivo)

KGP94 (i.p.; 20 mg/kg; once daily for 3 days) exhibits anti-metastatic and anti-bone resorptive efficacy in a prostate cancer bone metastasis model^[5].

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

Animal Model:	NCR nu/nu male mice^[5]
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection; once daily for 3 days
Result:	Reduced 65% in metastatic tumor burden and 58% in tumor angiogenesis, improved survival of bone metastases bearing mice.

体内研究

KGP94 (i.p.; 20 mg/kg; once daily for 3 days) exhibits anti-metastatic and anti-bone resorptive efficacy in a prostate cancer bone metastasis model^[5].

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

Animal Model:	NCR nu/nu male mice^[5]
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection; once daily for 3 days
Result:	Reduced 65% in metastatic tumor burden and 58% in tumor angiogenesis, improved survival of bone metastases bearing mice.

体内研究

KGP94 (i.p.; 20 mg/kg; once daily for 3 days) exhibits anti-metastatic and anti-bone resorptive efficacy in a prostate cancer bone metastasis model^[5].

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

Animal Model:	NCR nu/nu male mice^[5]
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection; once daily for 3 days
Result:	Reduced 65% in metastatic tumor burden and 58% in tumor angiogenesis, improved survival of bone metastases bearing mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (285.53 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8553 mL	14.2763 mL	28.5527 mL
5 mM	0.5711 mL	2.8553 mL	5.7105 mL
10 mM	0.2855 mL	1.4276 mL	2.8553 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: ≥ 2.5 mg/mL (7.14 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.14 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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.14 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.14 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。