HXR9 hydrochloride|西域试剂

HXR9 hydrochloride,99.50%

产品编号：Bellancom-P3245A| 分子式：C₁₁₉H₁₉₄ClN₅₃O₂₀S| 分子量：2754.67

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货号	价格	库存与货期
Bellancom-P3245A	￥1600.00	杭州北京（现货）
Bellancom-P3245A	￥3700.00	杭州北京（现货）
Bellancom-P3245A	￥5900.00	杭州北京（现货）

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HXR9 hydrochloride

产品介绍

HXR9 hydrochloride 是一种细胞渗透性肽，是 HOX/PBX 相互作用 (HOX/PBX interaction) 的竞争性拮抗剂。HXR9 hydrochloride 拮抗 HOX 与第二转录因子 (PBX) 之间的相互作用，PBX 与旁系同源基因组 1 至 8 中的 HOX 蛋白结合。HXR9 hydrochloride 选择性地减少细胞增殖并促进 HOXA/PBX3 基因高水平表达的细胞，例如 MLL 重排的白血病细胞中的细胞凋亡 (apoptosis)。

生物活性

HXR9 hydrochloride is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 hydrochloride antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 hydrochloride selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells.

体外研究

HXR9 hydrochloride (60μM; 4 hours) blocks the interaction between PBX and HOX.
HXR9 hydrochloride (60μM; 2 hours) triggers apoptosis in B16 and primary melanoma cells.
HXR9 hydrochloride (60μM; 2 hours) causes specific transcriptional changes.
HXR9 hydrochloride (B16 cells) shows antiproliferative activity with an IC₅₀ of 20μM.

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

Western Blot Analysis

Cell Line:	murine B16melanoma cells
Concentration:	60 μM
Incubation Time:	4 hours
Result:	Blocked the binding of HOXD9 to PBX.

Apoptosis Analysis

Cell Line:	B16 cells
Concentration:	60 μM
Incubation Time:	2 hours
Result:	A significant proportion of cells were in late phases of apoptosis.

RT-PCR

Cell Line:	B16F10cells
Concentration:	60 μM
Incubation Time:	2 hours
Result:	Fos, Jun, Dusp1, and Atf1，were allsignificantly up-regulate.

体内研究
(In Vivo)

HXR9 hydrochloride (10 mg/kg; i.v. via the tail vein; twice weekly) blocks tumor growth.
HXR9 hydrochloride (Initial dose of 100 mg/kg (subsequent dosing of 10 mg/kg twice weekly); Intraperitoneal; twice weekly for 18 days) blocks A549 tumour growth in vivo.

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

Animal Model:	C57black/6 mice (bearing B16 cells)
Dosage:	10 mg/kg
Administration:	I.v. via the tail vein; twice weekly (~30 days)
Result:	Tumors showed a significant degree of growth retardation.

Animal Model:	Athymic nude mice (bearing A549 cells)
Dosage:	Initial dose of 100 mg/kg (subsequent dosing of 10 mg/kg twice weekly)
Administration:	Intraperitoneal; twice weekly for 18 days
Result:	The tumours of HXR9-treated mice were considerably smaller than those of the control groups.

体内研究

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

Animal Model:	C57black/6 mice (bearing B16 cells)
Dosage:	10 mg/kg
Administration:	I.v. via the tail vein; twice weekly (~30 days)
Result:	Tumors showed a significant degree of growth retardation.

Animal Model:	Athymic nude mice (bearing A549 cells)
Dosage:	Initial dose of 100 mg/kg (subsequent dosing of 10 mg/kg twice weekly)
Administration:	Intraperitoneal; twice weekly for 18 days
Result:	The tumours of HXR9-treated mice were considerably smaller than those of the control groups.

体内研究

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

Animal Model:	C57black/6 mice (bearing B16 cells)
Dosage:	10 mg/kg
Administration:	I.v. via the tail vein; twice weekly (~30 days)
Result:	Tumors showed a significant degree of growth retardation.

Animal Model:	Athymic nude mice (bearing A549 cells)
Dosage:	Initial dose of 100 mg/kg (subsequent dosing of 10 mg/kg twice weekly)
Administration:	Intraperitoneal; twice weekly for 18 days
Result:	The tumours of HXR9-treated mice were considerably smaller than those of the control groups.

性状

Solid

溶解性数据

In Vitro:

H₂O : 50 mg/mL (18.15 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.3630 mL	1.8151 mL	3.6302 mL
5 mM	0.0726 mL	0.3630 mL	0.7260 mL
10 mM	0.0363 mL	0.1815 mL	0.3630 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 (sealed storage, away from moisture and light, under nitrogen)。-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