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

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
Solid + Solvent
10 mM * 1 mL in Water
ready for reconstitution
USD 132 In-stock
Solution
10 mM * 1 mL in Water USD 132 In-stock
Solid
5 mg USD 120 In-stock
10 mg USD 190 In-stock
25 mg USD 380 In-stock
50 mg USD 620 In-stock
100 mg USD 990 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE PRT-060318

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

MedChemExpress (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].

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

Molecular Weight

340.42

Formula

C18H24N6O

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CN=C(N[C@H]2[C@@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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

H2O : 25 mg/mL (73.44 mM; Need ultrasonic)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 25 mg/mL (73.44 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.36%

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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 2.9375 mL 14.6877 mL 29.3755 mL 73.4387 mL
5 mM 0.5875 mL 2.9375 mL 5.8751 mL 14.6877 mL
10 mM 0.2938 mL 1.4688 mL 2.9375 mL 7.3439 mL
15 mM 0.1958 mL 0.9792 mL 1.9584 mL 4.8959 mL
20 mM 0.1469 mL 0.7344 mL 1.4688 mL 3.6719 mL
25 mM 0.1175 mL 0.5875 mL 1.1750 mL 2.9375 mL
30 mM 0.0979 mL 0.4896 mL 0.9792 mL 2.4480 mL
40 mM 0.0734 mL 0.3672 mL 0.7344 mL 1.8360 mL
50 mM 0.0588 mL 0.2938 mL 0.5875 mL 1.4688 mL
60 mM 0.0490 mL 0.2448 mL 0.4896 mL 1.2240 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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PRT-060318 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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