1. Protein Tyrosine Kinase/RTK
  2. Src
  3. Lck Inhibitor

Lck Inhibitor 

Cat. No.: HY-12072 Purity: 98.98%
Handling Instructions

Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis.

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

Lck Inhibitor Chemical Structure

Lck Inhibitor Chemical Structure

CAS No. : 847950-09-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 166 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 166 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 142 In-stock
Estimated Time of Arrival: December 31
10 mg USD 226 In-stock
Estimated Time of Arrival: December 31
50 mg USD 907 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1716 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Lck Inhibitor:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis[1].

In Vitro

Lck Inhibitor (compound 25) exhibits good potency in the T-cell receptor-induced IL-2 secretion assay (IL-2, IC50=0.46 μM) and also inhibits subsequent T-cell proliferation (T-cell prolif, IC50=0.53 μM) in the same human T-cells. Lck Inhibitor also inhibits a human mixed lymphocyte reaction (huMLR) with a 10-fold increase in potency as compared to the other invitro cell assays utilizing purified human cells. Lck Inhibitor also displays inhibition of a mechanism-based biochemical cell assay probing Lck-dependent TCR-chain phosphorylation (TCR-chain). Lck Inhibitor shows a 10-fold reduction in potency when IL-2 is induced in a receptor-independent fashion by stimulating with phorbo lester and calcium ionophore (PMA/iono). Lck Inhibitor exhibits a similar level of potency when tested in a general proliferation assay using the human T-cell line, Jurkat (JKT)[1].

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

In Vivo

Lck Inhibitor (0-60 mg/kg; p.o.; once daily; from day 9 today 17) shows a dose-dependent inhibition of arthritis[1].
Lck Inhibitor (p.o.; 5 mg/kg) treatment shows the Cmax, AUC0-∞, tmax and F% are 82 ng/mL, 862 ng h/mL, and 17%, respectively[1].

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

Animal Model: Male Lewis rat (adjuvant-inducedarthritis model) [1]
Dosage: 0, 30, and 60 mg/kg
Administration: P.o.; once daily; from day 9 today 17
Result: Showed a dose-dependent inhibition of arthritis, with an ED50 estimated at 24 mg/kg.
Animal Model: Sprague-Dawley Rats[1]
Dosage: P.o. (Pharmacokinetic Analysis)
Administration: 5 mg/kg
Result: The Cmax, AUC0-∞, tmax and F% were 82 ng/mL, 862 ng h/mL, and 17%, respectively.
Molecular Weight

530.62

Formula

C₃₁H₃₀N₈O

CAS No.
SMILES

O=C1N(C2=C(C)C=CC=C2C)C3=NC4=CC=CC=C4N3C5=NC(NC6=CC=C(N7CCN(C)CC7)C=C6)=NC=C15

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: 

DMSO : 100 mg/mL (188.46 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8846 mL 9.4229 mL 18.8459 mL
5 mM 0.3769 mL 1.8846 mL 3.7692 mL
10 mM 0.1885 mL 0.9423 mL 1.8846 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 98.98%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

Lck InhibitorSrcTcellproliferationarthritisoralselectiveInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Lck Inhibitor
Cat. No.:
HY-12072
Quantity:
MCE Japan Authorized Agent: