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Chemical Structure| 1369761-01-2 Chemical Structure| 1369761-01-2

Structure of Cerdulatinib HCl
CAS No.: 1369761-01-2

Chemical Structure| 1369761-01-2

Cerdulatinib HCl

CAS No.: 1369761-01-2

Cerdulatinib HCl is a dual JAK/SYK inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. It also inhibits other kinases with IC50 less than 200 nM.

Synonyms: PRT2070 hydrochloride; PRT062070 hydrochloride; Cerdulatinib hydrochloride

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Cat. No.: A356094 Purity: 98%

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Product Details of Cerdulatinib HCl

CAS No. :1369761-01-2
Formula : C20H28ClN7O3S
M.W : 482.00
SMILES Code : O=C(C1=CN=C(NC2=CC=C(N3CCN(S(=O)(CC)=O)CC3)C=C2)N=C1NC4CC4)N.[H]Cl
Synonyms :
PRT2070 hydrochloride; PRT062070 hydrochloride; Cerdulatinib hydrochloride
MDL No. :MFCD28348366
InChI Key :IYULGYKOHUAYCG-UHFFFAOYSA-N
Pubchem ID :56960607

Safety of Cerdulatinib HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Cerdulatinib HCl

epigenetics
RTK
JAK-STAT

Isoform Comparison

Biological Activity

Description
Cerdulatinib hydrochloride (PRT062070) is a selective, orally bioavailable, and reversible ATP-competitive inhibitor targeting both SYK and JAK kinases, with IC50 values of 32 nM for SYK, and impressively low IC50s of 0.5 nM, 12 nM, 6 nM, and 8 nM for Tyk2, JAK1, JAK2, and JAK3, respectively. This dual inhibition profile positions cerdulatinib hydrochloride as a promising candidate for the study of autoimmune diseases and B-cell malignancies[1].[2].

In Vitro:

Cell Line
Concentration Treated Time Description References
A549 cells 5 µM 1 hour Inhibit the antiviral activity of RSV-EVs PMC9412241
CLL cells 1µM 24 hours Cerdulatinib synergized with venetoclax to induce greater apoptosis of CLL cells in the presence of IL-4/CD40L. PMC5417366
MEC1-UGT2B17OE 0.5 μM 24 hours To evaluate the anti-proliferative effect of Cerdulatinib on UGT2B17 overexpressing cells, results showed that Cerdulatinib significantly inhibited the proliferation of UGT2B17 overexpressing cells. PMC10177405
JVM2-UGT2B17OE 0.5 μM 24 hours To evaluate the anti-proliferative effect of Cerdulatinib on UGT2B17 overexpressing cells, results showed that Cerdulatinib significantly inhibited the proliferation of UGT2B17 overexpressing cells. PMC10177405
CLL cells 0.003-3µM 24, 48, 72 hours Cerdulatinib induced apoptosis of CLL cells in a concentration and time-dependent manner, particularly in IGHV unmutated samples. PMC5417366
MOLT4 40 μM 6 hours Inhibited SLFN11 expression and reduced phosphorylated TYK2 PMC8517841
CCRF-CEM 40 μM 6 hours Inhibited SLFN11 expression and reduced phosphorylated TYK2 PMC8517841
HEL 40 μM 6 hours Inhibited SLFN11 expression and reduced phosphorylated TYK2, JAK1, JAK2, and STAT1 PMC8517841
primary AML cells 0.01–10 µM 7 days Cerdulatinib showed a strong antiproliferative effect in all seven patient samples. PMC9737311
primary AML cells 0.01 µM and 0.05 µM 7 days Cerdulatinib demonstrated a wide range of antiproliferative effects in 59 patient samples, with median percent proliferation of 66% and 86%. PMC9737311
A549 cells 1 μM 72 hours Cerdulatinib significantly inhibited the proliferation of A549 cells and reversed the promoting effect of Rab27A-overexpression on cell proliferation. PMC10960821
H1299 cells 1 μM 72 hours Cerdulatinib significantly inhibited the proliferation of H1299 cells and reversed the promoting effect of Rab27A-overexpression on cell proliferation. PMC10960821
K562 cells 0.5 µM overnight To evaluate the responsiveness of K562 cells to Cerdulatinib, results showed that Cerdulatinib could induce reporter gene expression. PMC10530646

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/C Nude mice NSCLC xenograft model Oral 35 mg/kg 5 days per week for 4 weeks Cerdulatinib significantly inhibited the tumor-promoting effect induced by Rab27A-overexpression and exhibited antitumor effects in vivo. PMC10960821

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.07mL

0.41mL

0.21mL

10.37mL

2.07mL

1.04mL

20.75mL

4.15mL

2.07mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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