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Chemical Structure| 1370261-97-4 Chemical Structure| 1370261-97-4

Structure of PRT062607 HCl
CAS No.: 1370261-97-4

Chemical Structure| 1370261-97-4

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PRT062607 (P505-15) is a novel, highly specific, and potent orally available small-molecule inhibitor of Syk.

Synonyms: P505-15 Hydrochloride; BIIB057; PRT-2607

4.5 *For Research Use Only !

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Product Details of PRT062607 HCl

CAS No. :1370261-97-4
Formula : C19H24ClN9O
M.W : 429.91
SMILES Code : NC(C1=CN=C(N=C1NC2=CC=CC(N3N=CC=N3)=C2)N[C@H]4[C@H](CCCC4)N)=O.[H]Cl
Synonyms :
P505-15 Hydrochloride; BIIB057; PRT-2607
MDL No. :MFCD25976708
InChI Key :RMNLLPXCNDZJMJ-IDVLALEDSA-N
Pubchem ID :56948527

Safety of PRT062607 HCl

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

Related Pathways of PRT062607 HCl

RTK

Isoform Comparison

Biological Activity

Target
  • Syk

    Syk, IC50:1 nM

  • MLK1

    MLK1, IC50:88 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Ramos cells 2 µM 30 minutes Inhibited SYK autophosphorylation, significantly reduced SYK activity PMC3558816
SU-DHL4, SU-DHL6, Ramos cells 1 µM, 3 µM 72 hours Induced caspase 3-dependent apoptosis, observed only in BCR-signaling competent cell lines PMC3558816
CLL cells 2 μM 48 hours PRT062607 significantly decreased CLL cell viability, inducing apoptosis PMC5459370
CLL cells 2 μM 24 hours PRT062607 significantly inhibited CCL3 and CCL4 secretion by CLL cells PMC5459370
CLL cells 2 μM 3 hours PRT062607 significantly decreased CLL cell chemotaxis towards CXCL12 and CXCL13 PMC5459370
CLL cells 2 μM 4 hours PRT062607 significantly inhibited CLL cell migration beneath stromal cells PMC5459370
CLL cells 2 μM 10 minutes PRT062607 significantly inhibited BCR-induced ERK phosphorylation PMC5459370
BV2 cells 10 μM 24 hours To test the inhibitory effect of PRT062607 on Syk autophosphorylation in BV2 cells, results showed that PRT062607 significantly reduced Syk autophosphorylation. PMC10050448
Primary microglia 10 μM 24 hours To test the effect of PRT062607 on the survival of primary microglia, results showed that PRT062607 significantly increased the percentage of PI-positive cells, indicating it induced microglial cell death. PMC10050448

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Cecal ligation and puncture (CLP) model Intraperitoneal injection 8 mg/ml Twice daily for 3 days PRT062607 significantly reduced CLP-induced cardiac dysfunction, renal dysfunction, and liver injury, and decreased systemic inflammation and activation of NF-kB and NLRP3 inflammasome in the heart. PMC11570271
Mice Ramos xenograft model Oral 25 kBq Single injection, observed at 1 and 4 hours Inhibited Ramos tumor growth, significantly reduced tumor weight PMC3558816

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.63mL

2.33mL

1.16mL

23.26mL

4.65mL

2.33mL

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
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. 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

References

 

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