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Purity: ≥98%
Cerdulatinib HCl (formerly PRT2070; PRT062070) is a novel, potent, selective orally bioactive, and multi-targeted tyrosine kinase inhibitor of JAK1/2/3/TYK2 and Syk with potential antitumor activity. It inhibits JAK1/JAK2/JAK3/TYK2 and Syk with IC50s of 12 nM/6 nM/8 nM/0.5 nM and 32 nM, respectively. It shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy. Cerdulatinib also inhibits 19 other tested kinases with IC50 less than 200 nM. It is currently being studied in patients with genetically-defined hematologic cancers, as well as for patients who have failed therapy due to relapse or acquired mutations.
| ln Vitro |
CerduLatinib (0.03–4 μM) decreases the capacity to upregulate cell surface expression of the early activation marker CD69 with an IC50 of 0.11 μM and inhibits ERK Y204 phosphorylation in B cells in human whole blood with an IC50 of 0.5 μM [1]. With an IC50 of 0.12 μM, ceruletinib (0.015-2 μM) inhibits basophil degranulation mediated by FcεRI [1]. CerduLatinib demonstrates variable effects on the cytokine JAK/STAT signaling pathway at concentrations of 0.5–4 μM [1]. The viability effects of cerulodinib (0–15 μM; 72 hours) are comparable to the combined selective inhibition of JAK and SYK [1]. Non-Hodgkin lymphoma (NHL) cell lines that are capable of BCR signaling undergo apoptosis when exposed to cerulodinib (1-3 μM) for 48 hours [1].
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| ln Vivo |
In rats with collagen-induced arthritis (CIA), ceruletinib (0.5–5 mg/kg; PO twice daily for 2 weeks) exhibits dose-dependent effectiveness [1]. Oral administration of CerduLatinib twice a day for five days inhibits splenomegaly and BCR-induced B cell activation in mice [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: SU-DHL4; SU-DHL6; Ramosand and Daudi cells Tested Concentrations: 0, 1, 3 μM Incubation Duration: 48 hrs (hours) Experimental Results: Inhibits cells viability with the IC50s of 0.73-1.39 μM. Apoptosis Analysis [1] Cell Types: SU-DHL4, SU-DHL6, and Ramos cells Tested Concentrations: 0, 1.6, 5.0, 15 μM Incubation Duration: 72 hrs (hours) Experimental Results: Induced SU-DHL4, SU-DHL6, and Ramos cells apoptosis. |
| Animal Protocol |
Animal/Disease Models: Female Lewis rats (7-8 weeks old; 159-187 g) are immunized[1]
Doses: 0, 0.5, 1.5, 3, 5 mg/kg Route of Administration: po (oral gavage) twice (two times) daily for 2 weeks Experimental Results: Modulated inflammation in the rat CIA treatment model. Affected anticollagen antibody formation. Animal/Disease Models: balb/c (Bagg ALBino) mouse are received BCR stimulation[1] Doses: 0, 1, 5, 15, 20, 30 mg/kg Route of Administration: po (oral gavage) twice (two times) daily for 5 days Experimental Results: Suppressed upregulation of splenic B-cell surface CD80/86 and CD69 by＞60%. Inhibited mouse splenomegaly in a dose- and concentration-dependent manner. |
| 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.
[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. |
| Molecular Formula |
C20H28CLN7O3S
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|---|---|
| Molecular Weight |
482 (HCl salt)
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| CAS # |
1369761-01-2
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| Related CAS # |
Cerdulatinib;1198300-79-6
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| SMILES |
O=C(C1=CN=C(NC2=CC=C(N3CCN(S(=O)(CC)=O)CC3)C=C2)N=C1NC4CC4)N
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| InChi Key |
BGLPECHZZQDNCD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H27N7O3S/c1-2-31(29,30)27-11-9-26(10-12-27)16-7-5-15(6-8-16)24-20-22-13-17(18(21)28)19(25-20)23-14-3-4-14/h5-8,13-14H,2-4,9-12H2,1H3,(H2,21,28)(H2,22,23,24,25)
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| Chemical Name |
4-(cyclopropylamino)-2-((4-(4-(ethylsulfonyl)piperazin-1-yl)phenyl)amino)pyrimidine-5-carboxamide hydrochloride
InChi Key: BGLPECHZZQDNCD-UHFFFAOYSA-N
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| Synonyms |
PRT062070; PRT 062070; PRT062070, PRT2070; PRT2070; PRT-2070; PRT 2070; PRT-06270
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (4.15 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2 mg/mL (4.15 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2 mg/mL (4.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5% DMSO+corn oil: 3mg/mL |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01994382 | Completed Has Results |
Drug: Cerdulatinib Biological: Rituximab |
Follicular Lymphoma (FL/Indolent NHL) Aggressive NHL (a NHL) |
Alexion Pharmaceuticals, Inc. | August 30, 2013 | Phase 1 Phase 2 |
| NCT04021082 | Withdrawn | Drug: Cerdulatinib | Peripheral T-Cell Lymphoma (PTCL NOS) Nodal Lymphomas of T Follicular Helper (TFH) |
Portola Pharmaceuticals | November 15, 2019 | Phase 2 Phase 3 |
PRT062070 exhibits differential potency against cytokine JAK/STAT signaling pathways.J Pharmacol Exp Ther.2014 Dec;351(3):538-48. |
Dose responsive effect of PRT062070 in rat CIA treatment model.J Pharmacol Exp Ther.2014 Dec;351(3):538-48. |
PRT062070 blocks BCR-induced B-cell activation and splenomegaly in mice.J Pharmacol Exp Ther.2014 Dec;351(3):538-48. |
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