MSC2360844 hemifumarate

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MSC2360844 hemifumarate  纯度: 99.95%

MSC2360844 hemifumarate 是一种有效的，具有口服活性的选择性 PI3Kδ 抑制剂，IC50为 145 nM。MSC2360844 hemifumarate 对一组 278 种其他激酶显示出高度选择性。

MSC2360844 hemifumarate

MSC2360844 hemifumarate Chemical Structure

CAS No. : 1621688-31-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3860 In-stock
5 mg ￥3000 In-stock
10 mg ￥5000 In-stock
25 mg ￥9500 In-stock
50 mg ￥15500 In-stock
100 mg ￥23500 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

MSC2360844 hemifumarate is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. MSC2360844 hemifumarate shows highly selective against a panel of 278 additional kinases[1].

IC50 & Target[1]

PI3Kδ

145 nM (IC50)

体外研究
(In Vitro)

MSC2360844 hemifumarate (0-10 μM; 1 hours) completely abolished BCR-induced pAkt in Ramos B cells in a concentration-dependent manner with IC50 values of 280 nM[1].
MSC2360844 hemifumarate inhibits B cell proliferation in a concentration-dependent manner with an IC50 of 48 nM. MSC2360844 hemifumarate blocks BCR- and TCR-mediated responses in lymphocytes and TLR-induced IFNα by pDC in human primary cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: B cells
Concentration: 0-10 μM
Incubation Time: 1 hour
Result: Inhibited B cell proliferation in a concentration-dependent manner with an IC50 of 48 nM.

体内研究
(In Vivo)

MSC2360844 hemifumarate (6.6-66 mg/kg; daily from week 2 to 10) ameliorates disease manifestations in a murine SLE model[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NZB/W F1 female mice[1]
Dosage: 6.6, 22, or 66 mg/kg
Administration: Oral; starting at week 2 post ADV-IFNα delivery, once daily at 10 weeks
Result: Significantly reduced proteinuria incidence and severity in a dose-dependent manner.

分子量

584.62

Formula

C30H31FN4O9S
CAS 号

1621688-31-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (171.05 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7105 mL 8.5526 mL 17.1051 mL
5 mM 0.3421 mL 1.7105 mL 3.4210 mL
10 mM 0.1711 mL 0.8553 mL 1.7105 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 (4.28 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.28 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 (4.28 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.28 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 (4.28 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.28 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。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Haselmayer P, et al. Characterization of Novel PI3Kδ Inhibitors as Potential Therapeutics for SLE and Lupus Nephritis in Pre-Clinical Studies. Front Immunol. 2014 May 22;5:233.

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