Cerdulatinib hydrochloride PRT062070 hydrochloride; PRT2070 hydrochloride|cas:1369761-01-2|西域试剂

Cerdulatinib hydrochloride PRT062070 hydrochloride; PRT2070 hydrochloride,99.54%

产品编号：Bellancom-15999A| CAS NO：1369761-01-2| 分子式：C₂₀H₂₈ClN₇O₃S| 分子量：482.00

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货号	价格	库存与货期
Bellancom-15999A	￥800.00	杭州北京（现货）
Bellancom-15999A	￥1200.00	杭州北京（现货）
Bellancom-15999A	￥3600.00	杭州北京（现货）
Bellancom-15999A	￥6200.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Cerdulatinib hydrochloride PRT062070 hydrochloride; PRT2070 hydrochloride

产品介绍

Cerdulatinib hydrochloride (PRT062070) 是一种选择性，具有口服活性和可逆的 ATP 竞争性的 SYK 和 JAK 的双重抑制剂，抑制 SYK 和 Tyk2、JAK1、2、3 的 IC₅₀ 值分别为 32 nM、0.5 nM、12 nM、6 nM 和 8 nM。Cerdulatinib hydrochloride 可用于研究自身免疫性疾病和B细胞恶性肿瘤。

生物活性

Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with IC₅₀s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM for SYK and Tyk2, JAK1, 2, 3, respectively. Cerdulatinib hydrochloride could be used to research autoimmune disease and B-cell malignancies.

体外研究

Cerdulatinib (0.03-4 μM) inhibits ERK Y204 phosphorylation with an IC₅₀ of 0.5 μM and reduces the ability to upregulate cellsurface expression of the early activation marker CD69 with an IC₅₀ of 0.11 μM in B cells in human whole blood.
Cerdulatinib (0.015-2 μM) inhibits FcεRI-mediated basophil degranulation with an IC₅₀ of 0.12 μM.
Cerdulatinib (0.5-4 μM) exhibits differential potency against cytokine JAK/STAT signaling pathways.
Cerdulatinib (0-15 μM; 72 hours) results in viability effects similar to that of the combines SYK plus JAK-selective inhibition.
Cerdulatinib (1-3 μM; 48 hours) induces apoptosis in BCR-signaling competent non-Hodgkin lymphoma (NHL) cell lines.

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

Cell Viability Assay

Cell Line:	SU-DHL4; SU-DHL6; Ramosand and Daudi cells
Concentration:	0, 1, 3 μM
Incubation Time:	48 hours
Result:	Inhibits cells viability with the IC₅₀s of 0.73-1.39 μM.

Apoptosis Analysis

Cell Line:	SU-DHL4, SU-DHL6, and Ramos cells
Concentration:	0, 1.6, 5.0, 15 μM
Incubation Time:	72 hours
Result:	Induced SU-DHL4, SU-DHL6, and Ramos cells apoptosis.

体内研究
(In Vivo)

Cerdulatinib (0.5-5 mg/kg; twice daily p.o. for 2 weeks) elicits dose-dependent efficacy in the rat collagen-induced arthritis (CIA) model.
Cerdulatinib ( mg/kg; twice daily p.o. for 5 days) blocks BCR-induced B-cell activation and splenomegaly in mice.

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

Animal Model:	Female Lewis rats (7-8 weeks old; 159-187 g) are immunized
Dosage:	0, 0.5, 1.5, 3, 5 mg/kg
Administration:	Oral gavage twice daily for 2 weeks
Result:	Modulated inflammation in the rat CIA treatment model. Affected anticollagen antibody formation.

Animal Model:	Balb/c mice are received BCR stimulation
Dosage:	0, 1, 5, 15, 20, 30 mg/kg
Administration:	Oral gavage twice daily for 5 days
Result:	Suppressed upregulation of splenic B-cell surface CD80/86 and CD69 by＞60%. Inhibited mouse splenomegaly in a dose- and concentration-dependent manner.

体内研究

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

Animal Model:	Female Lewis rats (7-8 weeks old; 159-187 g) are immunized
Dosage:	0, 0.5, 1.5, 3, 5 mg/kg
Administration:	Oral gavage twice daily for 2 weeks
Result:	Modulated inflammation in the rat CIA treatment model. Affected anticollagen antibody formation.

Animal Model:	Balb/c mice are received BCR stimulation
Dosage:	0, 1, 5, 15, 20, 30 mg/kg
Administration:	Oral gavage twice daily for 5 days
Result:	Suppressed upregulation of splenic B-cell surface CD80/86 and CD69 by＞60%. Inhibited mouse splenomegaly in a dose- and concentration-dependent manner.

体内研究

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

Animal Model:	Female Lewis rats (7-8 weeks old; 159-187 g) are immunized
Dosage:	0, 0.5, 1.5, 3, 5 mg/kg
Administration:	Oral gavage twice daily for 2 weeks
Result:	Modulated inflammation in the rat CIA treatment model. Affected anticollagen antibody formation.

Animal Model:	Balb/c mice are received BCR stimulation
Dosage:	0, 1, 5, 15, 20, 30 mg/kg
Administration:	Oral gavage twice daily for 5 days
Result:	Suppressed upregulation of splenic B-cell surface CD80/86 and CD69 by＞60%. Inhibited mouse splenomegaly in a dose- and concentration-dependent manner.

性状

Solid

溶解性数据

In Vitro:

DMSO : 20 mg/mL (41.49 mM; ultrasonic and warming and heat to 80°C)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0747 mL	10.3734 mL	20.7469 mL
5 mM	0.4149 mL	2.0747 mL	4.1494 mL
10 mM	0.2075 mL	1.0373 mL	2.0747 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 mg/mL (4.15 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (4.15 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 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 mg/mL (4.15 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (4.15 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 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 mg/mL (4.15 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (4.15 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 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。