Lck inhibitor 2

Cat. No.: HY-10644 Purity: 99.81%: FAQs
Data Sheet SDS COA Handling Instructions

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Lck inhibitor 2 Chemical Structure

CAS No. : 944795-06-6

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 165	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 165	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 680	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 950	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Lck

Biological Activity
Purity & Documentation
References
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Description

Lck inhibitor 2 is a bis-anilinopyrimidine inhibitor of tyrosine kinases including LCK, BTK, LYN, SYK, and TXK. The IC50 values are 13nM, 9nM, 3nM, 26nM and 2nM for Lck, Btk, Lyn, Btk and Txk respectively IC50 Value: 13 nM(Lck) [1] Target: Src family kinase Lck inhibitor 2(Compound 9) inhibited 48 kinases with %control < 1 (33 of them tyrosine kinases, almost half of the 71 tyrosine kinases in the panel). A further 27 kinases were bound with %control < 10. Kd values for 16 kinases were determined and found to be below 100 nM. These included TXK (10 nM)[2].

Molecular Weight

335.36

Formula

C₁₈H₁₇N₅O₂

CAS No.

944795-06-6

Appearance

Solid

Color

Light yellow to yellow

SMILES

OC1=CC=C(C)C(NC2=CC=NC(NC3=CC(C(N)=O)=CC=C3)=N2)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 20 mg/mL (59.64 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	2.9819 mL	14.9094 mL	29.8187 mL
5 mM	0.5964 mL	2.9819 mL	5.9637 mL
10 mM	0.2982 mL	1.4909 mL	2.9819 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.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

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 mg/mL (5.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 mg/mL (5.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 mg/mL (5.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2 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 (20.0 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.

Purity & Documentation

Purity: 99.81%

Select Batch:

Data Sheet (274 KB) SDS (0 KB)

COA (250 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

References

[1]. Bamborough, et al. Assessment of Chemical Coverage of Kinome Space and Its Implications for Kinase Drug Discovery. Journal of Medicinal Chemistry (2008), 51(24), 7898-7914. [Content Brief]

[2]. Bamborough, Paul, et al. N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: Indazoles as phenol isosteres with improved pharmacokinetics. Bioorganic & Medicinal Chemistry Letters (2007), 17(15), 4363-4368. [Content Brief]

[3]. Awale, Mahendra, et al. Molecular docking guided 3D-QSAR CoMFA analysis of N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of leukocyte-specific protein tyrosine kinase. Journal of Molecular Modeling (2008), 14(10), 937-947. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.9819 mL	14.9094 mL	29.8187 mL	74.5468 mL
	5 mM	0.5964 mL	2.9819 mL	5.9637 mL	14.9094 mL
	10 mM	0.2982 mL	1.4909 mL	2.9819 mL	7.4547 mL
	15 mM	0.1988 mL	0.9940 mL	1.9879 mL	4.9698 mL
	20 mM	0.1491 mL	0.7455 mL	1.4909 mL	3.7273 mL
	25 mM	0.1193 mL	0.5964 mL	1.1927 mL	2.9819 mL
	30 mM	0.0994 mL	0.4970 mL	0.9940 mL	2.4849 mL
	40 mM	0.0745 mL	0.3727 mL	0.7455 mL	1.8637 mL
	50 mM	0.0596 mL	0.2982 mL	0.5964 mL	1.4909 mL

Lck inhibitor 2 Related Classifications

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:

Lck inhibitor 2944795-06-6Lck inhibitor2Lck inhibitor-2SrcInhibitorinhibitorinhibit

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