2. Cell Cycle/DNA Damage
  3. CDK
  4. CDK5 inhibitor 20-223

CDK5 inhibitor 20-223  (Synonyms: CP668863)

Cat. No.: HY-123772 Purity: 99.78%
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CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC50s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent.

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

CDK5 inhibitor 20-223 Chemical Structure

CDK5 inhibitor 20-223 Chemical Structure

CAS No. : 865317-30-2

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

CDK5 inhibitor 20-223 Related Antibodies

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Description

CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC50s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent[1].

IC50 & Target[1]

CDK2

6.0 nM (IC50)

CDK5

8.8 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
ASPC1 IC50
1163 nM
Compound: 21
Antiproliferative activity against human AsPC1 cells after 72 hrs by prestoblue assay
Antiproliferative activity against human AsPC1 cells after 72 hrs by prestoblue assay
[PMID: 30343954]
BXPC-3 IC50
> 2000 nM
Compound: 21
Antiproliferative activity against human BxPC3 cells after 72 hrs by prestoblue assay
Antiproliferative activity against human BxPC3 cells after 72 hrs by prestoblue assay
[PMID: 30343954]
MIA PaCa-2 IC50
861 nM
Compound: 21
Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by prestoblue assay
Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by prestoblue assay
[PMID: 30343954]
In Vitro

CDK5 inhibitor 20-223 (10 nM-10 μM; 72 hours) potently inhibits cell growth in a panel of colorectal cancer (CRC) cell lines[1].
CDK5 inhibitor 20-223 (0.3125-20 μM; 6 hours) induces a dose-dependent decrease in pRB (S807/811) and pFAK (S732) levels in each of the three CRC cell lines[1].

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

CDK5 inhibitor 20-223 Related Antibodies

Cell Viability Assay[1]

Cell Line: CRC cell lines SW620, DLD1, HT29, HCT116, FET, CBS, and GEO cells
Concentration: 10 μM, 1 μM, 100 nM, 10 nM
Incubation Time: 72 hours
Result: Reduced cell growth. IC50s of 168±20, 480±41, 360±72, 763±92, 117±49, 568±49, 79±31 nM for SW620, DLD1, HT29, HCT116, FET, CBS, and GEO cells.

Western Blot Analysis[1]

Cell Line: CRC cell lines GEO, HCT116 and HT29
Concentration: 20, 10, 5, 2.5, 1.25, 0.625, 0.3125 μM
Incubation Time: 6 hours
Result: Did not affect the total levels of CDK2/5, and the levels of total FAK or total Retinoblastoma protein (Rb).
Induced a dose-dependent decrease in pRB (S807/811) and pFAK (S732) levels.
In Vivo

CDK5 inhibitor 20-223 (8mg/kg; subcutaneously; for 14 injections) shows anti-tumor activity in human CRC xenograft tumors in nude mice[1].

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

Animal Model: Athymic nude mice[1]
Dosage: 8 mg/kg
Administration: Injections were given subcutaneously daily for the first week and every other day for two more weeks for a total of 14 injections.
Result: Reduced tumor growth and tumor weight in vivo.
Molecular Weight

305.37

Formula

C19H19N3O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1=NNC(C2CCC2)=C1)CC3=CC=C4C=CC=CC4=C3
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 : 100 mg/mL (327.47 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 3.2747 mL 16.3736 mL 32.7472 mL
5 mM 0.6549 mL 3.2747 mL 6.5494 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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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: ≥ 5 mg/mL (16.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 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 (50.0 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)

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
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 3.2747 mL 16.3736 mL 32.7472 mL 81.8679 mL
5 mM 0.6549 mL 3.2747 mL 6.5494 mL 16.3736 mL
10 mM 0.3275 mL 1.6374 mL 3.2747 mL 8.1868 mL
15 mM 0.2183 mL 1.0916 mL 2.1831 mL 5.4579 mL
20 mM 0.1637 mL 0.8187 mL 1.6374 mL 4.0934 mL
25 mM 0.1310 mL 0.6549 mL 1.3099 mL 3.2747 mL
30 mM 0.1092 mL 0.5458 mL 1.0916 mL 2.7289 mL
40 mM 0.0819 mL 0.4093 mL 0.8187 mL 2.0467 mL
50 mM 0.0655 mL 0.3275 mL 0.6549 mL 1.6374 mL
60 mM 0.0546 mL 0.2729 mL 0.5458 mL 1.3645 mL
80 mM 0.0409 mL 0.2047 mL 0.4093 mL 1.0233 mL
100 mM 0.0327 mL 0.1637 mL 0.3275 mL 0.8187 mL
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CDK5 inhibitor 20-223 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:

CDK5 inhibitor 20-223865317-30-2CP668863CP 668863CP-668863CDKCyclin dependent kinaseCDK2CDK5colorectalcancerCRCInhibitorinhibitorinhibit

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