RK-24466 (Synonyms: KIN 001-51)

Name: RK-24466
Brand: MedChemExpress
SKU: HY-108318
Rating: 4.5 (1 reviews)

製品番号: HY-108318 純度: 99.91%: Data Sheet SDS COA 取扱説明書
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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.

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RK-24466 構造式

CAS 番号 : 213743-31-8

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 198	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 198	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$180	在庫あり	Estimated Time of Arrival: December 31
10 mg	$290	在庫あり	Estimated Time of Arrival: December 31
25 mg	$500	在庫あり	Estimated Time of Arrival: December 31
50 mg	$750	在庫あり	Estimated Time of Arrival: December 31
100 mg	$1150	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

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Based on 1 publication(s) in Google Scholar

Other Forms of RK-24466:

RK-24466 (Standard) お問い合わせ

顧客検証

•Jagiellonian University. 2026.

Src アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

Lck Fyn Blk Fgr Hck Lyn Yes SRC-3

生物活性
プロトコル
純度とドキュメンテーション
参考文献
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製品説明

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]

Cellular Effect

Cell Line	Type	Value	Description	References
Jurkat	IC₅₀	1.5 3 Compound: 6	Inhibition of anti-CD3 stimulated IL-2 production by Jurkat cells Inhibition of anti-CD3 stimulated IL-2 production by Jurkat cells	[PMID: 11012021]
Jurkat	IC₅₀	1.5 3 Compound: 6	Inhibition of anti-CD3 stimulated IL-2 production by Jurkat cells Inhibition of anti-CD3 stimulated IL-2 production by Jurkat cells	[PMID: 11012021]
Jurkat	IC₅₀	0.8 3 Compound: 6	Inhibition of PMA stimulated IL-2 production in Jurkat cells Inhibition of PMA stimulated IL-2 production in Jurkat cells	[PMID: 11012021]
Jurkat	IC₅₀	1.5 3 Compound: 6	Inhibition of anti-CD3 stimulated IL-2 production by Jurkat cells Inhibition of anti-CD3 stimulated IL-2 production by Jurkat cells	[PMID: 11012021]
Jurkat	IC₅₀	0.8 3 Compound: 6	Inhibition of PMA stimulated IL-2 production in Jurkat cells Inhibition of PMA stimulated IL-2 production in Jurkat cells	[PMID: 11012021]
Sf21	IC₅₀	177 1 Compound: B43	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	[PMID: 31368705]
Sf21	IC₅₀	177 1 Compound: B43	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	[PMID: 31368705]

体外実験

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.

体内実験

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].

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

分子量

370.45

分子式

C₂₃H₂₂N₄O

CAS 番号

213743-31-8

Appearance

Solid

Color

Off-white to light yellow

SMILES

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

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)

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

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, 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.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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: ≥ 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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.25 mg/mL (6.07 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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).

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.

純度とドキュメンテーション

純度: 99.91%

Select Batch:

データシート (280 KB) SDS (393 KB)

COA (255 KB) HNMR (257 KB) LCMS (94 KB)

取扱説明書 (2659 KB)

参考文献

[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]

細胞実験 ^[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]. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[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]. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[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

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

RK-24466 Related Classifications

Inflammation/Immunology Cardiovascular Disease

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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:

RK-24466213743-31-8KIN 001-51RK24466RK 24466SrcInhibitorinhibitorinhibit

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RK-24466 (Synonyms: KIN 001-51)

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Molarity Calculator

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Complete Stock Solution Preparation Table

RK-24466 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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RK-24466 (Synonyms: KIN 001-51)

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Other Forms of RK-24466:

RK-24466 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

Src アイソフォーム固有の製品をすべて表示:

生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

RK-24466 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

RK-24466 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

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