2. Protein Tyrosine Kinase/RTK
  3. Src
  4. CSK-IN-1

CSK-IN-1 (compound 13) is a potent, orally active c-terminal Src kinase (CSK) with IC50 values below 3 nM and 4 nM in CSK HTRF and Caliper assay, respectively. CSK-IN-1 shows the ability to increase T cell proliferation induced by T cell receptor signaling.

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

CSK-IN-1 Chemical Structure

CSK-IN-1 Chemical Structure

CAS No. : 2380027-49-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 591 In-stock
Solution
10 mM * 1 mL in DMSO USD 591 In-stock
Solid
1 mg USD 190 In-stock
5 mg USD 400 In-stock
10 mg USD 680 In-stock
25 mg USD 1350 In-stock
50 mg USD 2200 In-stock
100 mg USD 3400 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

CSK-IN-1 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE CSK-IN-1

View All Src Isoform Specific Products:

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Lck Fyn Blk

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CSK-IN-1 (compound 13) is a potent, orally active c-terminal Src kinase (CSK) with IC50 values below 3 nM and 4 nM in CSK HTRF and Caliper assay, respectively. CSK-IN-1 shows the ability to increase T cell proliferation induced by T cell receptor signaling[1].

IC50 & Target

IC50: <3 nM (c-terminal Src kinase CSK in HTRF assay), 4 nM (c-terminal Src kinase in Caliper assay)[1]
Cellular Effect
Cell Line Type Value Description References
Jurkat EC50
41 nM
Compound: 13
Effect on ZAP70 phosphorylation in human Jurkat cells pre-incubated for 30 mins followed by anti-CD3/CD28 stimulation measured after 10 mins
Effect on ZAP70 phosphorylation in human Jurkat cells pre-incubated for 30 mins followed by anti-CD3/CD28 stimulation measured after 10 mins
[PMID: 31620238]
In Vivo

CSK-IN-1 (compound 13) reduces inhibitory LCK phosphorylation in vivo upon oral dosing and shows the ability to enhance T cell activation in response to antigen stimulation[1].

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

671.12

Formula

C34H32ClFN8O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=NN(C2CCN(C(CC(C)(C#N)C)=O)CC2)C3=C1C=C(F)C=C3)NC4=CC=C(NC(C5=C6C=CC(OC)=CN6N=C5)=O)C(Cl)=C4
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 (149.00 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 1.4900 mL 7.4502 mL 14.9005 mL
5 mM 0.2980 mL 1.4900 mL 2.9801 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (3.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

  • Protocol 2

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

    Solubility: ≥ 2.08 mg/mL (3.10 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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: 98.61%

SDS (251 KB)

COA (253 KB) HNMR (201 KB) LCMS (113 KB)

Handling Instructions (2659 KB)
References

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.4900 mL 7.4502 mL 14.9005 mL 37.2512 mL
5 mM 0.2980 mL 1.4900 mL 2.9801 mL 7.4502 mL
10 mM 0.1490 mL 0.7450 mL 1.4900 mL 3.7251 mL
15 mM 0.0993 mL 0.4967 mL 0.9934 mL 2.4834 mL
20 mM 0.0745 mL 0.3725 mL 0.7450 mL 1.8626 mL
25 mM 0.0596 mL 0.2980 mL 0.5960 mL 1.4900 mL
30 mM 0.0497 mL 0.2483 mL 0.4967 mL 1.2417 mL
40 mM 0.0373 mL 0.1863 mL 0.3725 mL 0.9313 mL
50 mM 0.0298 mL 0.1490 mL 0.2980 mL 0.7450 mL
60 mM 0.0248 mL 0.1242 mL 0.2483 mL 0.6209 mL
80 mM 0.0186 mL 0.0931 mL 0.1863 mL 0.4656 mL
100 mM 0.0149 mL 0.0745 mL 0.1490 mL 0.3725 mL
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CSK-IN-1 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:

CSK-IN-12380027-49-4SrcInhibitorinhibitorinhibit

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