Cerdulatinib
Based on 8 publication(s) in Google Scholar
Cerdulatinib (PRT062070) is a selective Tyk2 inhibitor with an IC50 of 0.5 nM. Cerdulatinib (PRT062070) also is a dual JAK and SYK inhibitor with IC50s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.06%
- CAS. Nr.: 1198300-79-6
- Formel: C20H27N7O3S
- Molecular Weight:445.54
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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HY-L005
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Publications Citing Use of MedChemExpress (MCE) Cerdulatinib
More- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- J Ethnopharmacol. 2025 Feb 7:119461. [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
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WB
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Biologische Aktivität
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Tyk2 0.5 nM (IC50) |
JAK2 6 nM (IC50) |
JAK3 8 nM (IC50) |
JAK1 12 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) |
Cerdulatinib shows inhibitory effect on 60 CLL with IC50 ranging from 0.37 to 10.02 μM. Cerdulatinib induces apoptosis in CLL in association with MCL-1 down-regulation and PARP cleavage. Cerdulatinib (2μM) is able to overcome the support of the microenvironment and induces CLL cell death. Cerdulatinib (250-500 nM) blocks proliferation of ibrutinib-sensitive and ibrutinib-resistant primary CLL cells. Cerdulatinib also blocks proliferation of both ibrutinib-sensitive and ibrutinib-resistant primary CLL cells as well as BTKC481S-transfected cell lines, and blocks BCR and JAK-STAT signaling pathways. Furthermore, inhibition of SYK and JAK by cerdulatinib translates to downstream inhibition of AKT and ERK. Cerdulatinib inhibits the activity of NF-kB pathway[1]. PRT062070 reduces the ability of stimulated B cells to upregulate cell-surface expression of the early activation marker CD69 (IC50=0.11 μM). PRT062070 exhibits differential potency against cytokine JAK/STAT signaling pathways. PRT062070 (1 or 3 μM) induces apoptosis in BCR-signaling competent NHL cell lines[2]. Cerdulatinib demonstrates inhibitory activity against both ABC and GCB subtypes of DLBCL cells. Cerdulatinib also induces apoptosis in both GCB and ABC subtypes of DLBCL cell lines via caspase 3 and PARP cleavage. And cerdulatinib blocks cell cycle in both ABC and GCB subtypes of DLBCL via inhibition of RB phosphorylation and down-regulation of cyclin E. Cerdulatinib induces cell cycle arrest and apoptosis under the condition of BCR stimulation in all DLBCL cell lines. Besides, cerdulatinib blocks JAK/STAT and BCR signaling in both ABC and GCB DLBCL cell lines. Cerdulatinib induces cell death in primary human DLBCL samples[3]. Cerdulatinib inhibits BCR-induced signals in a dose-dependent manner and most strongly between 0.3 to 1 μM. and particularly in IGHV-unmutated samples with greater BCR signaling capacity and response to IL4, or samples expressing higher levels of sIgM, CD49d+, or ZAP70+. Cerdulatinib overcomes anti-IgM, IL4/CD40L, or NLC-mediated protection by preventing upregulation of MCL-1 and BCL-XL; however, BCL-2 expression is unaffected. Furthermore, in samples treated with IL4/CD40L, cerdulatinib synergizes with venetoclax in vitro to induce greater apoptosis than either drug alone[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1198300-79-6
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Appearance Solid
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Molecular Weight 445.54
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Formel C20H27N7O3S
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Color Light yellow to yellow
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SMILES
O=S(N(CC1)CCN1C2=CC=C(NC3=NC=C(C(N)=O)C(NC4CC4)=N3)C=C2)(CC)=O
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Synonyms
PRT062070; PRT2070
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Cerdulatinib purchased from MedChemExpress. Usage Cited in: Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
Kinobead western Blot readout for selected inhibitor:protein combinations.
Cerdulatinib 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.
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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 Feb 7:119461. 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 -
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Methods Mol Biol
2018:1711:351-398. PMID: 29344898
Lösungsmittel & Löslichkeit
DMSO : ≥ 30 mg/mL (67.33 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.5 mg/mL (5.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
Protokoll
TMD8 cells are transfected with constructs of WT BTK or BTKC481S mutants using kit V, Program U-13 on Amaxa Nucleofector. After transfection, the cells are co-cultured with NKTert cells in a 24-well plate for 24 hrs for recovery. Ibrutinib, cerdulatinib and vehicle (DMSO) are then added into the transfected TMD8 cells and cellular viability is determined with MuseTM Count & Viability kit using Muse Cell Analyzer. The cell survival is determined by flow cytometry using the Annexin V/7-AAD Apoptosis Detection Kit I on freshly isolated CLL cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (280 KB)
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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)
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Handling Instructions (2659 KB)
Verweise
[1]. Guo A, et al. Dual SYK/JAK inhibition overcomes ibrutinib resistance in chronic lymphocytic leukemia: Cerdulatinib, but not ibrutinib, induces apoptosis of tumor cells protected by the microenvironment. Oncotarget. 2017 Feb 21;8(8):12953-12967. [Content Brief]
[2]. 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]
[3]. Ma J, et al. Cerdulatinib, a novel dual SYK/JAK kinase inhibitor, has broad anti-tumor activity in both ABC and GCB types of diffuse large B cell lymphoma. Oncotarget. 2015 Dec 22;6(41):43881-96. [Content Brief]
[4]. Blunt MD, et al. The Dual Syk/JAK Inhibitor Cerdulatinib Antagonizes B-cell Receptor and Microenvironmental Signaling in Chronic Lymphocytic Leukemia. Clin Cancer Res. 2017 May 1;23(9):2313-2324. [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 |
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| DMSO | 1 mM | 2.2445 mL | 11.2223 mL | 22.4447 mL | 56.1117 mL |
| 5 mM | 0.4489 mL | 2.2445 mL | 4.4889 mL | 11.2223 mL | |
| 10 mM | 0.2244 mL | 1.1222 mL | 2.2445 mL | 5.6112 mL | |
| 15 mM | 0.1496 mL | 0.7482 mL | 1.4963 mL | 3.7408 mL | |
| 20 mM | 0.1122 mL | 0.5611 mL | 1.1222 mL | 2.8056 mL | |
| 25 mM | 0.0898 mL | 0.4489 mL | 0.8978 mL | 2.2445 mL | |
| 30 mM | 0.0748 mL | 0.3741 mL | 0.7482 mL | 1.8704 mL | |
| 40 mM | 0.0561 mL | 0.2806 mL | 0.5611 mL | 1.4028 mL | |
| 50 mM | 0.0449 mL | 0.2244 mL | 0.4489 mL | 1.1222 mL | |
| 60 mM | 0.0374 mL | 0.1870 mL | 0.3741 mL | 0.9352 mL |
Cerdulatinib Related Classifications
HY-15999 Related Classifications
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