MSC2360844 hemifumarate IOA-244 hemifumarate|cas:1621688-31-0|西域试剂

MSC2360844 hemifumarate IOA-244 hemifumarate,99.95%

产品编号：Bellancom-135827A| CAS NO：1621688-31-0| 分子式：C₂₆H₂₇FN₄O₅S.1/2C₄H₄O₄| 分子量：584.62

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货号	价格	库存与货期
Bellancom-135827A	￥3000.00	杭州北京（现货）
Bellancom-135827A	￥5000.00	杭州北京（现货）
Bellancom-135827A	￥9500.00	杭州北京（现货）
Bellancom-135827A	￥15500.00	杭州北京（现货）
Bellancom-135827A	￥23500.00	杭州北京（现货）

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MSC2360844 hemifumarate IOA-244 hemifumarate

产品介绍

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。

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.

体外研究

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.
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.

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

Cell Viability Assay

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.

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

Animal Model:	NZB/W F1 female mice
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.

体内研究

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

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

Animal Model:	NZB/W F1 female mice
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.

体内研究

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

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

Animal Model:	NZB/W F1 female mice
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.

性状

Solid

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。