2. Protein Tyrosine Kinase/RTK Apoptosis
  3. Syk Apoptosis
  4. PRT-060318 dihydrochloride

PRT-060318 dihydrochloride  (Synonyms: PRT318 dihydrochloride)

Cat. No.: HY-12974A Purity: 98.98%
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Handling Instructions Technical Support

PRT-060318 (PRT318) dihydrochloride is a potent, selective and orally active tyrosine kinase Syk inhibitor with an IC50 of 3 nM. PRT-060318 dihydrochloride suppresses chronic lymphocytic leukemia (CLL) B cell activation and migration, and induces apoptosis. PRT-060318 dihydrochloride prevents Heparin (HY-17567)-induced thrombocytopenia and thrombosis in a transgenic mouse model. PRT-060318 dihydrochloride can be used for CLL and thrombus research.

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

PRT-060318 dihydrochloride

PRT-060318 dihydrochloride Chemical Structure

CAS No. : 3032567-93-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
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10 mg In-stock
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Based on 4 publication(s) in Google Scholar

Other Forms of PRT-060318 dihydrochloride:

PRT-060318 dihydrochloride Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PRT-060318 (PRT318) dihydrochloride is a potent, selective and orally active tyrosine kinase Syk inhibitor with an IC50 of 3 nM. PRT-060318 dihydrochloride suppresses chronic lymphocytic leukemia (CLL) B cell activation and migration, and induces apoptosis. PRT-060318 dihydrochloride prevents Heparin (HY-17567)-induced thrombocytopenia and thrombosis in a transgenic mouse model. PRT-060318 dihydrochloride can be used for CLL and thrombus research[1][2].

In Vitro

PRT-060318 (PRT318) (0-3 µM, 15 min) dihydrochloride completely inhibits Heparin-induced thrombocytopenia (HIT) immune complex-induced aggregation of both human and transgenic HIT mouse platelets[1].

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

PRT-060318 dihydrochloride Related Antibodies
In Vivo

PRT-060318 (PRT318) (10 and 30 mg/kg, i.g., b.i.d. for 7 days) dihydrochloride prevents heparin-induced thrombocytopenia and thrombosis in a transgenic mouse model[1].

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

Animal Model: C57Bl/6 mice treated with KKO (20 mg/kg, i.p.)[1]
Dosage: 10 and 30 mg/kg
Administration: i.g., b.i.d. for 7 days
Result: Significantly inhibited platelet deposition without affecting bleeding time.
Markedly reduced HIT immune complex-induced thrombosis in the lungs.
Significantly reduced the thrombosis score compared to vehicle.
Molecular Weight

413.34

Formula

C18H26Cl2N6O
CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

O=C(C1=CN=C(N[C@H]2[C@@H](N)CCCC2)N=C1NC3=CC=CC(C)=C3)N.Cl.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (30.24 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4193 mL 12.0966 mL 24.1932 mL
5 mM 0.4839 mL 2.4193 mL 4.8386 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (3.02 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.25 mg/mL (3.02 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4193 mL 12.0966 mL 24.1932 mL 60.4829 mL
5 mM 0.4839 mL 2.4193 mL 4.8386 mL 12.0966 mL
10 mM 0.2419 mL 1.2097 mL 2.4193 mL 6.0483 mL
15 mM 0.1613 mL 0.8064 mL 1.6129 mL 4.0322 mL
20 mM 0.1210 mL 0.6048 mL 1.2097 mL 3.0241 mL
25 mM 0.0968 mL 0.4839 mL 0.9677 mL 2.4193 mL
30 mM 0.0806 mL 0.4032 mL 0.8064 mL 2.0161 mL
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PRT-060318 dihydrochloride 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.

Keywords:

PRT-0603183032567-93-1PRT318PRT060318PRT 060318PRT 318PRT-318SykApoptosisSpleen tyrosine kinasechronic lymphocytic leukemiaB cell activationHeparin-induced thrombocytopeniathrombosistransgenic mouse modelInhibitorinhibitorinhibit

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