Structure of Cerdulatinib HCl
CAS No.: 1369761-01-2
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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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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
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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 |
GHS Pictogram: | ![]() |
Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
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 |
Tags: Cerdulatinib | PRT062070 | PRT2070 | PRT 062070 | PRT-062070 | PRT 2070 | PRT-2070 | Syk | JAK | Spleen tyrosine kinase | Janus kinase | Tyk2 | autoimmune | B-cell malignancies | SYK inhibitor | JAK inhibitor | Tyk2 inhibitor | JAK1 inhibitor | JAK2 inhibitor | JAK3 inhibitor | 1369761-01-2
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P337 + P313 | IF eye irritation persists: Get medical advice/attention. |
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H311 | Toxic in contact with skin |
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H314 | Causes severe skin burns and eye damage |
H315 | Causes skin irritation |
H316 | Causes mild skin irritation |
H317 | May cause an allergic skin reaction |
H318 | Causes serious eye damage |
H319 | Causes serious eye irritation |
H320 | Causes eye irritation |
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H331 | Toxic if inhaled |
H332 | Harmful if inhaled |
H333 | May be harmful if inhaled |
H334 | May cause allergy or asthma symptoms or breathing difficulties if inhaled |
H335 | May cause respiratory irritation |
H336 | May cause drowsiness or dizziness |
H340 | May cause genetic defects |
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H361 | Suspected of damaging fertility or the unborn child |
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H362 | May cause harm to breast-fed children |
H370 | Causes damage to organs |
H371 | May cause damage to organs |
H372 | Causes damage to organs through prolonged or repeated exposure |
H373 | May cause damage to organs through prolonged or repeated exposure |
Environmental hazards | |
Code | Phrase |
H400 | Very toxic to aquatic life |
H401 | Toxic to aquatic life |
H402 | Harmful to aquatic life |
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H411 | Toxic to aquatic life with long-lasting effects |
H412 | Harmful to aquatic life with long-lasting effects |
H413 | May cause long-lasting harmful effects to aquatic life |
H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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