Sovleplenib HMPL-523|cas:1415792-84-5|西域试剂

Sovleplenib HMPL-523,99.56%

产品编号：Bellancom-145598| CAS NO：1415792-84-5| 分子式：C₂₄H₃₀N₆O₃S| 分子量：482.60

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-145598		￥6800.00	杭州北京（现货）
Bellancom-145598		￥11000.00	杭州北京（现货）

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Sovleplenib HMPL-523

产品介绍

Sovleplenib (HMPL-523) 是一种高效的、可口服的选择性 SYK 抑制剂，IC₅₀ 为 25 nM。具有抗肿瘤活性。Sovleplenib 可用于免疫性血小板减少症（ITP）的研究。

生物活性

Sovleplenib (HMPL-523) is a highly potent, orally available and selective SYK inhibitor with an IC₅₀ of 25 nM. Anti-tumor activity. Sovleplenib can be used for the research of immune thrombocytopenia (ITP).

体外研究

Sovleplenib (HMPL-523) inhibits SYK, FLT3, KDR, LYN, FGFR2, and AUR A with IC₅₀s of 0.025, 0.063, 0.390, 0.921, 3.214, 3.969 μM, respectively.
Sovleplenib (HMPL-523) blocks phosphorylation of BLNK, downstream protein of Syk, in human mantle cell line REC-1 and human plasma cell line ARH-7777 with IC₅₀s of 0.105 µM and 0.173 μM, respectively.
Sovleplenib also inhibits cell viability of Ba/F3 Tel-Syk with the IC₅₀ of 0.033 μM.
Sovleplenib also increases the apoptotic rate of REC-1 cells.
Sovleplenib shows the synergistic activities on killing human diffused large B cell lymphoma (DLBCL) in combination with other drugs such as BTK inhibitor, PI3Kδ inhibitors and Bcl2 family inhibitor.

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

体内研究

Sovleplenib (HMPL-523) shows anti-tumor activity in vivo. Sovleplenib (100 mg/kg) inhibits tumor growth in REC-1 subcutaneous xenograft model.
Sovleplenib (HMPL-523; 100 mg/kg; daily oral administration) shows potent anti-tumor activity in B cell lymphoma REC-1 (TGI: 59%) in Syk dependent xenograft models .

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

Animal Model:	Balb/c nude mice bearing subcutaneously implanted REC-1 cells or intravenously injected BA/F3 cells or BA/F3 TEL-SYK cells
Dosage:	10 and 100 mg/kg
Administration:	q.d.; for 8 days
Result:	Inhibited tumor growth in REC-1 subcutaneous xenograft model at 100 mg/kg.

体内研究

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

Animal Model:	Balb/c nude mice bearing subcutaneously implanted REC-1 cells or intravenously injected BA/F3 cells or BA/F3 TEL-SYK cells
Dosage:	10 and 100 mg/kg
Administration:	q.d.; for 8 days
Result:	Inhibited tumor growth in REC-1 subcutaneous xenograft model at 100 mg/kg.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (51.80 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0721 mL	10.3605 mL	20.7211 mL
5 mM	0.4144 mL	2.0721 mL	4.1442 mL
10 mM	0.2072 mL	1.0361 mL	2.0721 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: ≥ 2.08 mg/mL (4.31 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.31 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (4.31 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.31 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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