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

Lck Inhibitor 

Cat. No.: HY-12072 Purity: 99.44%
COA 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.

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Lck Inhibitor Chemical Structure

Lck Inhibitor Chemical Structure

CAS No. : 847950-09-8

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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
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Based on 1 publication(s) in Google Scholar

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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

Appearance

Solid

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 available by MCE.
Purity & Documentation

Purity: 99.44%

COA (264 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References
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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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Keywords:

Lck Inhibitor847950-09-8SrcTcellproliferationarthritisoralselectiveInhibitorinhibitorinhibit

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