1. Protein Tyrosine Kinase/RTK
  2. Src
  3. RK-24466

RK-24466 (Synonyms: KIN 001-51)

Cat. No.: HY-108318 Purity: >98.0%
Handling Instructions

RK-24466 (KIN 001-51) is a potent and selective Lck inhibitor; inhibits Lck (64-509) and LckCD isoforms with IC50s of less than 1 and 2 nM, respectively.

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

RK-24466 Chemical Structure

RK-24466 Chemical Structure

CAS No. : 213743-31-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 225 In-stock
Estimated Time of Arrival: December 31
1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 276 In-stock
Estimated Time of Arrival: December 31
10 mg   Get quote  
50 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

RK-24466 (KIN 001-51) is a potent and selective Lck inhibitor; inhibits Lck (64-509) and LckCD isoforms with IC50s of less than 1 and 2 nM, respectively.

IC50 & Target

IC50: <1 nM (Lck (64-509)), 2 nM (LckCD)[1]

In Vitro

RK-24466 is selective for Lck over a range of receptor, non-receptor tyrosine kinases and seronine/threonine kinases. RK-24466 are potent inhibitors of IL2 production in Jurkat cells stimulated with anti-CD3 antibody, being at least 100-fold more potent than PP1. RK-24466 displays remarkable cellular selectivity[1]. RK-24466 significantly inhibits both VSMC proliferation and migration. RK-24466 suppresses VSMC proliferation and migration via down-regulating the protein kinase B (Akt) and extracellular signal regulated kinase (ERK) pathways, and it significantly decreases the expression of proliferating cell nuclear antigen (PCNA) and cyclin D1 and, the phosphorylation of retinoblastoma protein (pRb)[2].

In Vivo

RK-24466 inhibits T-cell receptor stimulated (a-CD3 mAb) IL-2 production in mice at low doses (ED50=4 mg/kg) after ip administration. However, efficacy is greatly reduced after oral administration (ED50=25 mg/kg) which is presumed to reflect poor intestinal absorption in the latter regimen. Inhibition of antigen specific T-cell immune responses is also seen for RK-24466. After administration of RK-24466 twice daily (100 mg/kg po) for 3 days during the in vivo priming phase, a 70% inhibition of IFNγ production is seen upon subsequent antigen-specific (KLH) challenge of lymphocytes from the draining lymph nodes in vitro[3]. RK-24466 suppresses the migration of VSMCs from endothelium-removed aortic rings, as well as neointima formation following rat carotid balloon injury[2].

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 : 45 mg/mL (121.47 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6994 mL 13.4971 mL 26.9942 mL
5 mM 0.5399 mL 2.6994 mL 5.3988 mL
10 mM 0.2699 mL 1.3497 mL 2.6994 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: 2.25 mg/mL (6.07 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.25 mg/mL (6.07 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.25 mg/mL (6.07 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

To examine the concentration-dependent effect of the RK-24466, VSMCs are cultured in 10% FBS-supplemented DMEM containing either vehicle (DMSO 2%, v/v) or increasing concentrations of the RK-24466 (1 to 10 μM) for 24 h, and cellular proliferation is determined by using CCK-8[2].

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

Animal Administration
[2]

Rats: For the RK-24466 treated group, RK-24466 at a final blood concentration of 5 μM is intravenously injected through femoral vein. At 14d after BI, the rats are anesthetized, and the carotid arteries are excised. The entire length of the right carotid artery is balloon injured. The left carotid artery serves as an uninjured intra-animal control. To assess the neointima formation, H&E stained section is imaged, and the intima to media thickness ratio is measured[2].

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

References
Molecular Weight

370.45

Formula

C₂₃H₂₂N₄O

CAS No.

213743-31-8

SMILES

NC1=C2C(N(C3CCCC3)C=C2C4=CC=C(OC5=CC=CC=C5)C=C4)=NC=N1

Shipping

Room temperature in continental US; may vary elsewhere

Purity: >98.0%

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Product Name:
RK-24466
Cat. No.:
HY-108318
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RK-24466

Cat. No.: HY-108318