RK-24466
Based on 2 publication(s) in Google Scholar
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.
- Purity: 99.91%
- CAS No.: 213743-31-8
- Formula: C23H22N4O
- Molecular Weight:370.45
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) RK-24466
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Biological Activity
IC50: <1 nM (Lck (64-509)), 2 nM (LckCD)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Jurkat | IC50 |
0.8 μM
Compound: 6
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Inhibition of PMA stimulated IL-2 production in Jurkat cells
Inhibition of PMA stimulated IL-2 production in Jurkat cells
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[PMID: 11012021] |
| Jurkat | IC50 |
1.5 μM
Compound: 6
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Inhibition of anti-CD3 stimulated IL-2 production by Jurkat cells
Inhibition of anti-CD3 stimulated IL-2 production by Jurkat cells
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[PMID: 11012021] |
| Sf21 | IC50 |
177 nM
Compound: B43
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Inhibition of N-terminal GST-tagged human EGFR (696 to end aminoacids) expressed in baculovirus infected Sf21 cells
Inhibition of N-terminal GST-tagged human EGFR (696 to end aminoacids) expressed in baculovirus infected Sf21 cells
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[PMID: 31368705] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 213743-31-8
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Appearance Solid
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Molecular Weight 370.45
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Formula C23H22N4O
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Color Off-white to light yellow
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SMILES
NC1=C2C(N(C3CCCC3)C=C2C4=CC=C(OC5=CC=CC=C5)C=C4)=NC=N1
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Synonyms
KIN 001-51
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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bioRxiv
The gp120 Envelope Glycoprotein of HIV-1 Triggers Macropinocytosis in Primary CD4+ T Cells to Promote HIV-1 Infection. [Abstract]2026 Apr 28:2026.04.27.721102. PMID: 42094527 -
Solvent & Solubility
DMSO : 45 mg/mL (121.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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
This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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.
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
This protocol yields a suspended solution of 2.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Arnold LD, et al. Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I. Bioorg Med Chem Lett. 2000 Oct 2;10(19):2167-70. [Content Brief]
[2]. Seo HH, et al. 7-cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d] pyrimidin-4-ylamine inhibits the proliferation and migration of vascular smooth muscle cells by suppressing ERK and Akt pathways. Eur J Pharmacol. 2017 Mar 5;798:35-42. [Content Brief]
[3]. Burchat AF, et al. Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitorsof lck II. Bioorg Med Chem Lett. 2000 Oct 2;10(19):2171-4. [Content Brief]
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6994 mL | 13.4971 mL | 26.9942 mL | 67.4855 mL |
| 5 mM | 0.5399 mL | 2.6994 mL | 5.3988 mL | 13.4971 mL | |
| 10 mM | 0.2699 mL | 1.3497 mL | 2.6994 mL | 6.7485 mL | |
| 15 mM | 0.1800 mL | 0.8998 mL | 1.7996 mL | 4.4990 mL | |
| 20 mM | 0.1350 mL | 0.6749 mL | 1.3497 mL | 3.3743 mL | |
| 25 mM | 0.1080 mL | 0.5399 mL | 1.0798 mL | 2.6994 mL | |
| 30 mM | 0.0900 mL | 0.4499 mL | 0.8998 mL | 2.2495 mL | |
| 40 mM | 0.0675 mL | 0.3374 mL | 0.6749 mL | 1.6871 mL | |
| 50 mM | 0.0540 mL | 0.2699 mL | 0.5399 mL | 1.3497 mL | |
| 60 mM | 0.0450 mL | 0.2250 mL | 0.4499 mL | 1.1248 mL | |
| 80 mM | 0.0337 mL | 0.1687 mL | 0.3374 mL | 0.8436 mL | |
| 100 mM | 0.0270 mL | 0.1350 mL | 0.2699 mL | 0.6749 mL |
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