Cerdulatinib

SKU: orb1305410

Description

Cerdulatinib

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

−

Key Properties

−

CAS Number	1198300-79-6
MW	445.54
Purity	99.64%
Formula	C₂₀H₂₇N₇O₃S
SMILES	CCS(=O)(=O)N1CCN(CC1)c1ccc(Nc2ncc(C(N)=O)c(NC3CC3)n2)cc1
Target	JAK,Syk,Tyrosine Kinases
Solubility	DMSO:40 mg/mL (89.78 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.49 mM)

Bioactivity

−

Target IC50	MLK1:5 nM\|JAK3:8 nM\|Rsk4:28 nM\|Flt3:90 nM\|PAR1B-a:13 nM\|MST2:15 nM\|TYK2:0.5 nM\|TSSK:14 nM\|JAK1:12 nM\|GCK:18 nM\|TBK1:10 nM\|ARK5:4 nM\|JAK2:6 nM\|Chk1:42 nM\|MST1:4 nM\|MARK1:10 nM\|FLT4:51 nM\|RET:105 nM\|RSK2:20 nM\|AMPK:6 nM\|Syk:32 nM\|ITK:194 nM\|FMS:5 nM\|JNK3:18 nM Read more...
In Vivo	Cerdulatinib (0.5 mg/kg) causes a nonstatistically significant trend toward reduced ankle inflammation, whereas significant reductions in inflammation are achieved with the 1.5, 3, and 5 mg/kg doses. Besides, Cerdulatinib also affects anticollagen antibody formation. Cerdulatinib (15 mg/kg) suppresses upregulation of splenic B-cell surface CD80/86 and CD69, and inhibits BCR signaling and activation in the spleen after oral dosing in mice. Read more...
In Vitro	Cerdulatinib effectively inhibits 60 CLL cells with IC50 values ranging between 0.37 to 10.02 μM, induces apoptosis via MCL-1 down-regulation and PARP cleavage, and overcomes microenvironmental support to trigger CLL cell death at 2 μM. It inhibits both ibrutinib-sensitive and -resistant primary CLL cell proliferation at concentrations of 250-500 nM, targets BTKC481S-transfected cell lines, halts BCR and JAK-STAT signaling, and blocks SYK and JAK leading to the downstream inhibition of AKT, ERK, and the NF-kB pathway. PRT062070, with an IC50 of 0.11 μM, limits stimulated B cell activation marker CD69 expression, demonstrating varied effectiveness against JAK/STAT pathways and induces apoptosis in BCR-signaling competent NHL cell lines at 1 or 3 μM. Cerdulatinib shows inhibitory actions on both ABC and GCB DLBCL cell subtypes, induces caspase 3 and PARP cleavage-mediated apoptosis, inhibits cell cycle progression through RB phosphorylation reduction and cyclin E down-regulation, and blocks JAK/STAT and BCR signaling. It elicits cell death in DLBCL cells under BCR stimulation and in primary human DLBCL samples, disrupts BCR-induced signaling, especially potent from 0.3 to 1 μM in IGHV-unmutated, high BCR signaling, sIgM, CD49d+, or ZAP70+ expressing samples, and neutralizes anti-IgM, IL4/CD40L, or NLC-mediated protection by preventing MCL-1 and BCL-XL upregulation, without affecting BCL-2 expression. Cerdulatinib also synergizes with venetoclax to enhance apoptosis in IL4/CD40L treated samples. Read more...
Cell Research	Cerdulatinib is dissolved in DMSO. 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. Read more...

Storage & Handling

−

Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

−

Inhibitor, inhibit, JAKs, Janus kinase, JAK, JAK1, Cerdulatinib, Syk, Spleen tyrosine kinase, PRT2070, PRT-2070, PRT 062070, PRT062070, PRT-062070, PRT 2070, Tyk2, TyrosineKinases, Tyrosine Kinases

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID

44595079 ↗

Key Properties

−

No computed properties available.

Documents Download

Datasheet

Product Information

Download

Request a Document

Protocol Information

Find More Protocols

Cerdulatinib (orb1305410)

Based on 0 reviews

Participating in our Biorbyt product reviews program enables you to support fellow scientists by sharing your firsthand experience with our products.

No reviews yet

Purity:	99.85%
CAS Number:	1369761-01-2
MW:	482
Formula:	C₂₀H₂₈ClN₇O₃S

Purity:	>98% (HPLC)
CAS Number:	1198300-79-6
MW:	445.5
Formula:	C₂₀H₂₇N₇O₃S

Cerdulatinib

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Similar Products

Cerdulatinib hydrochloride [orb1688997]

Cerdulatinib [orb1222819]

Quality Guarantee

Compound Identifiers

Key Properties

Documents Download

Request a Document

Protocol Information

Cerdulatinib (orb1305410)

Step 1: Enter information below

Step 2: Enter the in vivo formulation

Available Sizes

Email

UK Office

US Office

CN Office

Distributors