Cerdulatinib hydrochloride(Synonyms: PRT062070 hydrochloride; PRT2070 hydrochloride)

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Cerdulatinib hydrochloride (Synonyms: PRT062070 hydrochloride; PRT2070 hydrochloride) 纯度: 99.54%

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。

Cerdulatinib hydrochloride(Synonyms: PRT062070 hydrochloride; PRT2070 hydrochloride)

Cerdulatinib hydrochloride Chemical Structure

CAS No. : 1369761-01-2

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10 mM * 1 mL in DMSO ￥1150 In-stock
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10 mg ￥1200 In-stock
50 mg ￥3600 In-stock
100 mg ￥6200 In-stock
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Cerdulatinib hydrochloride 相关产品

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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[1][2].

IC50 & Target

Tyk2

0.5 nM (IC50)

JAK1

12 nM (IC50)

JAK2

6 nM (IC50)

JAK3

8 nM (IC50)

SYK

32 nM (IC50)

MST1

4 nM (IC50)

ARK5

4 nM (IC50)

MLK1

5 nM (IC50)

FMS

5 nM (IC50)

AMPK

6 nM (IC50)

TBK1

10 nM (IC50)

MARK1

10 nM (IC50)

PAR1B-a

13 nM (IC50)

TSSK

14 nM (IC50)

MST2

15 nM (IC50)

GCK

18 nM (IC50)

JNK3

18 nM (IC50)

Rsk2

20 nM (IC50)

Rsk4

28 nM (IC50)

CHK1

42 nM (IC50)

Flt4

51 nM (IC50)

Flt3

90 nM (IC50)

Ret

105 nM (IC50)

Itk

194 nM (IC50)

体外研究
(In Vitro)

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[1].
Cerdulatinib (0.015-2 μM) inhibits FcεRI-mediated basophil degranulation with an IC50 of 0.12 μM[1].
Cerdulatinib (0.5-4 μM) exhibits differential potency against cytokine JAK/STAT signaling pathways[1].
Cerdulatinib (0-15 μM; 72 hours) results in viability effects similar to that of the combines SYK plus JAK-selective inhibition[1].
Cerdulatinib (1-3 μM; 48 hours) induces apoptosis in BCR-signaling competent non-Hodgkin lymphoma (NHL) cell lines[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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[1]

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[1].
Cerdulatinib ( mg/kg; twice daily p.o. for 5 days) blocks BCR-induced B-cell activation and splenomegaly in mice[1].

上海金畔生物科技有限公司 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[1]
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[1]
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.

Clinical Trial

分子量

482.00

Formula

C20H28ClN7O3S
CAS 号

1369761-01-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Coffey G, et al. The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. J Pharmacol Exp Ther. 2014 Dec; 351(3): 538-48.

    [2]. Ishikawa C, et, al. Anti-adult T‑cell leukemia/lymphoma activity of cerdulatinib, a dual SYK/JAK kinase inhibitor. Int J Oncol. 2018 Oct; 53(4): 1681-1690.

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