Mefuparib hydrochloride MPH|cas:1449746-00-2|西域试剂

Mefuparib hydrochloride MPH,98.94%

产品编号：Bellancom-122661| CAS NO：1449746-00-2| 分子式：C₁₇H₁₆ClFN₂O₂| 分子量：334.77

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-122661	￥2000.00	杭州北京（现货）
Bellancom-122661	￥3500.00	杭州北京（现货）
Bellancom-122661	￥7000.00	杭州北京（现货）

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Mefuparib hydrochloride MPH

产品介绍

Mefuparib hydrochloride (MPH) 是一种具有口服活性的，底物竞争性和选择性的 PARP1/2 抑制剂，IC₅₀ 分别为 3.2 nM 和 1.9 nM。Mefuparib hydrochloride 诱导细胞凋亡 (apoptosis)，并在体内外具有显着的抗癌活性。

生物活性

Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC₅₀s of 3.2 nM and 1.9 nM, respectively. Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo.

体外研究

Mefuparib hydrochloride (1-10 μM; 48 hours) causes cell apoptosis.
Mefuparib hydrochloride (MPH; 1-10 μM; 24 hours) causes V-C8 cells into typical G2/M arrest.
Mefuparib hydrochloride (1-10 μM; 24 hours) causes the accumulation of DSB marked by the increased levels of γH2AX in the MDA-MB-436 (BRCA1^−/−) cells in a concentration-dependent manner.
Mefuparib hydrochloride exerts potent in vitro proliferation-inhibitory effects on cancer cells derived from different human tissues with an average IC₅₀ of 2.16 μM (0.12 μM~3.64 μM).
Mefuparib hydrochloride inhibits PARP3 (IC₅₀>10 μM), PARP6 (IC₅₀>10 μM), TNKS1 (IC₅₀=1.6 μM), TNKS2 (IC₅₀=1.3 μM).

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

Apoptosis Analysis

Cell Line:	V-C8 cells
Concentration:	1, 3, 10 μM
Incubation Time:	48 hours
Result:	Caused cell apoptosis.

Cell Cycle Analysis

Cell Line:	V-C8 cells
Concentration:	1, 3, 10 μM
Incubation Time:	24 hours
Result:	Cell came into typical G2/M arrest.

Western Blot Analysis

Cell Line:	MDA-MB-436 (BRCA1^−/−) cells
Concentration:	1, 10 μM
Incubation Time:	24 hours
Result:	Caused the accumulation of DSB marked by the increased levels of γH2AX in the MDA-MB-436 (BRCA1^−/−) cells in a concentration-dependent manner.

体内研究
(In Vivo)

Mefuparib hydrochloride (MPH; 40-160 mg/kg; orally; once every other day; for 21 days) displays dose- and time-dependent killing on V-C8 xenografts accompanied by complete disappearance of some xenografts, especially in the high-dose group.
Mefuparib hydrochloride (160 mg/kg; orally; once every other day; for 21 days) inhibits the growth of the BR-05-0028 breast patient-derived xenograft (PDX) without obvious loss of body weight.
Mefuparib hydrochloride (10, 20, 40 mg/kg; oral) has a T_1/2 of 1.07-1.3 hours and a C _max of 116-725 ng/mL for SD rats.
Mefuparib hydrochloride (5, 10, 20 mg/kg; oral) has a T_1/2 of 2.16-2.7 hours and a C _max of 114-608 ng/mL for cynomolgus monkeys.

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

Animal Model:	Nude mice with V-C8 xenografts
Dosage:	40, 80, 160 mg/kg
Administration:	Orally; once every other day; for 21 days
Result:	Displayed dose- and time-dependent killing on V-C8 xenografts accompanied by complete disappearance of some xenografts, especially in the high-dose group.

Animal Model:	SD rats
Dosage:	10, 20, 40 mg/kg (Pharmacokinetic Analysis)
Administration:	Oral
Result:	Had a T_1/2 of 1.07-1.3 hours and a C _max of 116-725 ng/mL.

体内研究

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

Animal Model:	Nude mice with V-C8 xenografts
Dosage:	40, 80, 160 mg/kg
Administration:	Orally; once every other day; for 21 days
Result:	Displayed dose- and time-dependent killing on V-C8 xenografts accompanied by complete disappearance of some xenografts, especially in the high-dose group.

Animal Model:	SD rats
Dosage:	10, 20, 40 mg/kg (Pharmacokinetic Analysis)
Administration:	Oral
Result:	Had a T_1/2 of 1.07-1.3 hours and a C _max of 116-725 ng/mL.

体内研究

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

Animal Model:	Nude mice with V-C8 xenografts
Dosage:	40, 80, 160 mg/kg
Administration:	Orally; once every other day; for 21 days
Result:	Displayed dose- and time-dependent killing on V-C8 xenografts accompanied by complete disappearance of some xenografts, especially in the high-dose group.

Animal Model:	SD rats
Dosage:	10, 20, 40 mg/kg (Pharmacokinetic Analysis)
Administration:	Oral
Result:	Had a T_1/2 of 1.07-1.3 hours and a C _max of 116-725 ng/mL.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (74.68 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9871 mL	14.9356 mL	29.8713 mL
5 mM	0.5974 mL	2.9871 mL	5.9743 mL
10 mM	0.2987 mL	1.4936 mL	2.9871 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)。-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 (7.47 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.47 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% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (7.47 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.47 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.47 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.47 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。