1. Protein Tyrosine Kinase/RTK
  2. Syk
  3. PRT-060318

PRT-060318 (Synonyms: PRT318)

Cat. No.: HY-12974 Purity: 99.50%
Handling Instructions

PRT-060318 (PRT318) is a novel selective inhibitor of the tyrosine kinase Syk with an IC50 of 4 nM.

For research use only. We do not sell to patients.

PRT-060318 Chemical Structure

PRT-060318 Chemical Structure

CAS No. : 1194961-19-7

Size Price Stock Quantity
10 mM * 1 mL in Water USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
25 mg USD 408 In-stock
Estimated Time of Arrival: December 31
50 mg USD 732 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

PRT-060318 (PRT318) is a novel selective inhibitor of the tyrosine kinase Syk with an IC50 of 4 nM.

IC50 & Target

IC50: 4 nM (Syk)[1]

In Vitro

PRT318 is a potent inhibitor of purified Syk kinase with an IC50 of 4 nM. Syk kinase is inhibited by 92%, whereas all other kinases retains more than 70% at a concentration of 50 nM of PRT318[1]. PRT318 and P505-15 effectively antagonize CLL cell survival after B-cell receptor (BCR) triggering and in nurse-like cell-co-cultures. They inhibit BCR-dependent secretion of the chemokines CCL3 and CCL4 by CLL cells, and leukemia cell migration toward the tissue homing chemokines CXCL12, CXCL13, and beneath stromal cells. PRT318 and P505-15 inhibit Syk and extracellular signal-regulated kinase phosphorylation after BCR triggering[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PRT318 completely inhibits HIT immune complex-induced aggregation of both human and transgenic HIT mouse platelets. Pretreatment of mice with PRT318 markedly reduces HIT IC-induced thrombosis in the lungs. The Thrombosis Score is significantly lower for PRT318-treated mice compared with control[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

340.42

Formula

C₁₈H₂₄N₆O

CAS No.

1194961-19-7

SMILES

O=C(C1=CN=C(N[[email protected]]2[[email protected]@H](N)CCCC2)N=C1NC3=CC=CC(C)=C3)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 5.6 mg/mL (16.45 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9375 mL 14.6877 mL 29.3755 mL
5 mM 0.5875 mL 2.9375 mL 5.8751 mL
10 mM 0.2938 mL 1.4688 mL 2.9375 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

PRT318 is dissolved in DMSO. Cells are incubated for 14 days in 24-well plates. CLL cells are cultured under standardized conditions on NLC or in suspension, in the presence or absence of PRT318 and P505-15. At 24, 48, 72 h, CLL cells are collected and assayed for cell viability[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: Heparin-induced thrombocytopenia (HIT) model mice are treated with KKO (20 mg/kg body weight, intraperitoneally) on day 0. The mice are divided into sex- and weight-matched experimental and control groups. On days 1 to 7, experimental mice (n=6) receives PRT318 (30 mg/kg body weight) orally via gavage twice a day, whereas control mice (n=6) receives vehicle only (sterile water). Both groups receives heparin (1600 U/kg body weight, subcutaneously) once daily. Mice are anesthetized by isoflurane inhalation for injections and blood collections[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.50%

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Keywords:

PRT-060318PRT318PRT060318PRT 060318PRT 318PRT-318SykSpleen tyrosine kinaseInhibitorinhibitorinhibit

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Product Name:
PRT-060318
Cat. No.:
HY-12974
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