1. GPCR/G Protein MAPK/ERK Pathway Apoptosis
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  3. CASIN

CASIN is a selective GTPase Cdc42 inhibitor with an IC50 of 2 uM. CASIN can be used for the research of cancer.

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

CASIN Chemical Structure

CASIN Chemical Structure

CAS No. : 425399-05-9

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Solid + Solvent
10 mM * 1 mL in DMSO
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Solid
5 mg USD 92 In-stock
10 mg USD 158 In-stock
25 mg USD 317 In-stock
50 mg USD 581 In-stock
100 mg USD 950 In-stock
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Description

CASIN is a selective GTPase Cdc42 inhibitor with an IC50 of 2 uM. CASIN can be used for the research of cancer[1][2].

IC50 & Target

IC50: 2 μM (GTPase Cdc42)[1]

In Vitro

CASIN (0-10 μM; 3 d) inhibits the growth of AMO-1, ARH-77, IM-9 , JJN-3, L-363, MOLP-8 and RPMI-8226/S cells[1].
CASIN (0-10 μM; 16 h) inhibits melphalan induced FANCD2 mono-ubiquitination in LR5 cells but shows no effect to S cells[1].
CASIN (5 μM; 2 d) increases cell apoptosis of bortezomib-resistant MM patient cells[1].

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

Cell Viability Assay[3]

Cell Line: AMO-1, ARH-77, IM-9 , JJN-3, L-363, MOLP-8 and RPMI-8226/S cells
Concentration: 0-10 μM
Incubation Time: 3 days
Result: Inhibited MM cell lines including AMO-1, ARH-77, IM-9 , JJN-3, L-363, MOLP-8 and RPMI-8226/S cells with GI50s vof 3.23, 4.31, 4.87, 2.56, 4.64, 4.67 and 3.97 μM, respectively.

Western Blot Analysis[3]

Cell Line: MM (S) and melphalan-resistant (LR5) MM cells
Concentration: 5 μM
Incubation Time: 16 hours
Result: Abolished melphalan induced FANCD2 mono-ubiquitination and DNA damage in LR5, sensitized LR5 to melphalan-induced cell death by blocking FANCD2-mediated DNA damage repair.

Apoptosis Analysis[3]

Cell Line: Bortezomib-resistant MM patients cells
Concentration: 5 μM
Incubation Time: 2 days
Result: 2-fold increased cell apoptosis in the cell derived from bortezomib-resistant MM patients.
In Vivo

CASIN (20 mg/kg; i.p. 2 times a day) prolongs lifetime of mice with busulfan injection[1].

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

Animal Model: NSG mice with busulfan injection[3]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection; 20 mg/kg 2 times a day
Result: Significantly prolonged the lifespan of xenografts mice better than bortezomib, and showed a leading position when combined with bortezomib.
Molecular Weight

306.40

Formula

C20H22N2O

CAS No.
Appearance

Solid

SMILES

OCCNC1C(NC2=C3C=C(C4=CC=CC=C4)C=C2)=C3CCC1

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 : ≥ 31 mg/mL (101.17 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2637 mL 16.3185 mL 32.6371 mL
5 mM 0.6527 mL 3.2637 mL 6.5274 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)

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (6.79 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.
  • Protocol 2

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

    Solubility: ≥ 2.08 mg/mL (6.79 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 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.
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: 99.82%

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, 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 3.2637 mL 16.3185 mL 32.6371 mL 81.5927 mL
5 mM 0.6527 mL 3.2637 mL 6.5274 mL 16.3185 mL
10 mM 0.3264 mL 1.6319 mL 3.2637 mL 8.1593 mL
15 mM 0.2176 mL 1.0879 mL 2.1758 mL 5.4395 mL
20 mM 0.1632 mL 0.8159 mL 1.6319 mL 4.0796 mL
25 mM 0.1305 mL 0.6527 mL 1.3055 mL 3.2637 mL
30 mM 0.1088 mL 0.5440 mL 1.0879 mL 2.7198 mL
40 mM 0.0816 mL 0.4080 mL 0.8159 mL 2.0398 mL
50 mM 0.0653 mL 0.3264 mL 0.6527 mL 1.6319 mL
60 mM 0.0544 mL 0.2720 mL 0.5440 mL 1.3599 mL
80 mM 0.0408 mL 0.2040 mL 0.4080 mL 1.0199 mL
100 mM 0.0326 mL 0.1632 mL 0.3264 mL 0.8159 mL
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CASIN 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.

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