Cerdulatinib hydrochloride
Based on 8 publication(s) in Google Scholar
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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 98.96%
- CAS No.: 1369761-01-2
- 화학식: C20H28ClN7O3S
- 분자량:482.00
-
보관:
4°C, sealed storage, away from moisture.
In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
용액&용해도
- 순도&문서
- References
-
Help & FAQs
-
HY-50856
RuxolitinibJAK1/2 Inhibitor -
HY-15315
BaricitinibJAK1/2 Inhibitor -
HY-40354
TofacitinibJAK1/JAK3 Inhibitor -
HY-12067
R406Syk/FLT3 Inhibitor -
HY-18300
FilgotinibJAK1 Inhibitor -
HY-15999
CerdulatinibTyk2 Inhibitor -
HY-19569
UpadacitinibJAK1 Inhibitor -
HY-50514
AT9283Aurora/JAK Inhibitor -
HY-50856A
Ruxolitinib (S enantiomer)JAK Inhibitor -
HY-117287
DeucravacitinibTYK2 Inhibitor -
HY-15343
CEP-33779JAK2 Inhibitor -
HY-40354R
Tofacitinib (Standard)Reference Standard
Publications Citing Use of MedChemExpress (MCE) Cerdulatinib hydrochloride
More- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- J Ethnopharmacol. 2025 Mar 13:343:119461. [Abstract]
- NAR Cancer. 2025 Oct 7;7(4):zcaf037. [Abstract]
- iScience. 2021 Sep 25;24(10):103173. [Abstract]
- Int Immunol. 2025 Jul 11:dxaf041. [Abstract]
- Immunohorizons. 2019 May 16;3(5):172-185. [Abstract]
- Patent. US20180263995A1.
- Methods Mol Biol. 2018:1711:351-398. [Abstract]
Customer Validation & Images
-
WB
-
WB
Biological Activity
제품 설명
IC50 & Target
[1]|
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) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
-
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.
-
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.
In Vivo
? Cerdulatinib (twice daily p.o. for 5 days) blocks BCR-induced B-cell activation and splenomegaly in mice[1].
MedChemExpress (MCE) 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.
Chemical Information
-
CAS No. 1369761-01-2
-
Appearance Solid
-
분자량 482.00
-
화학식 C20H28ClN7O3S
-
Color Off-white to light brown
-
SMILES
O=S(N(CC1)CCN1C2=CC=C(NC3=NC=C(C(N)=O)C(NC4CC4)=N3)C=C2)(CC)=O.Cl
-
Synonyms
PRT062070 hydrochloride; PRT2070 hydrochloride
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
4°C, sealed storage, away from moisture
In solvent -80°C 2 years -20°C 1 year
Publications (8)
-
Journal Impact Factor
-
Most Recent
-
Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Cerdulatinib hydrochloride purchased from MedChemExpress. Usage Cited in: Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
Kinobead western Blot readout for selected inhibitor:protein combinations.
Cerdulatinib hydrochloride purchased from MedChemExpress. Usage Cited in: Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
Immunoblot analysis in MV-4-11 cells and MOLM-13, FLT3-WT and FLT3-ITD transfected HEK293 cells, and Ba/F3 FLT3-ITD cells revealed FLT3 target engagement for Golvatinib and Cabozantinib.
-
J Ethnopharmacol
Network pharmacology integrated with experimental validation reveals the mechanism of Xanthii Fructus against allergic rhinitis via JAK2/STAT3/HIF-1α signaling pathway. [Abstract]2025 Mar 13:343:119461. PMID: 39923957 -
NAR Cancer
Co-expression of CD30 and SLFN11 serves as a dual biomarker for the treatment of cutaneous T-cell lymphoma. [Abstract]2025 Oct 7;7(4):zcaf037. PMID: 41064808 -
iScience
Schlafen 11 expression in human acute leukemia cells with gain-of-function mutations in the interferon-JAK signaling pathway. [Abstract]2021 Sep 25;24(10):103173. PMID: 34693224 -
Int Immunol
Interleukin-35 regulates the differentiation of regulatory T cells through the JAK-STAT pathway and influences glutamine metabolism in ARDS. [Abstract]2025 Jul 11:dxaf041. PMID: 40643216 -
Immunohorizons
IκB-ζ Expression Requires Both TYK2/STAT3 Activity and IL-17-Regulated mRNA Stabilization. [Abstract]2019 May 16;3(5):172-185. PMID: 31356171 -
-
Methods Mol Biol
2018:1711:351-398. PMID: 29344898
용액&용해도
In Vitro:
DMSO : 20 mg/mL (41.49 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (4.15 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (4.15 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
-
Data Sheet (281 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0747 mL | 10.3734 mL | 20.7469 mL | 51.8672 mL |
| 5 mM | 0.4149 mL | 2.0747 mL | 4.1494 mL | 10.3734 mL | |
| 10 mM | 0.2075 mL | 1.0373 mL | 2.0747 mL | 5.1867 mL | |
| 15 mM | 0.1383 mL | 0.6916 mL | 1.3831 mL | 3.4578 mL | |
| 20 mM | 0.1037 mL | 0.5187 mL | 1.0373 mL | 2.5934 mL | |
| 25 mM | 0.0830 mL | 0.4149 mL | 0.8299 mL | 2.0747 mL | |
| 30 mM | 0.0692 mL | 0.3458 mL | 0.6916 mL | 1.7289 mL | |
| 40 mM | 0.0519 mL | 0.2593 mL | 0.5187 mL | 1.2967 mL |
Cerdulatinib hydrochloride Related Classifications
HY-15999A Related Classifications
Powered by Bioz