Cat. No.: HY-131978

DB18

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DB18 is a potent and selective inhibitor of CDC2-like kinases (CLKs), with IC₅₀ values in the range of 10-30 nM for CLK1, CLK2 and CLK4. DB18 has anti-tumor activity.

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Pureté: 99.15%
CAS No.: 2587177-94-2
Formule: C₂₄H₁₈ClN₇O₃
Masse moléculaire:487.90

Stockage:

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

DB18 Chemical Structure

CAS No.: 2587177-94-2

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Activité biologique
- Description
- Cellular Effect
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

DB18 is a potent and selective inhibitor of CDC2-like kinases (CLKs), with IC₅₀ values in the range of 10-30 nM for CLK1, CLK2 and CLK4. DB18 has anti-tumor activity^[1].

Voir tous les produits spécifiques à Isoform CDK :

Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	IC₅₀	37 μM Compound: 7h; DB18	Cytotoxicity against human CaCo-2 cells assessed as reduction in cell viability incubated for 48 hrs by Hoechst-33342 staining based cell counting method (Rvb > 25 microM) Cytotoxicity against human CaCo-2 cells assessed as reduction in cell viability incubated for 48 hrs by Hoechst-33342 staining based cell counting method (Rvb > 25 microM)	[PMID: 33422908]
Fibroblast	IC₅₀	21 μM Compound: 7h; DB18	Cytotoxicity against human Fibroblast cells assessed as reduction in cell viability incubated for 48 hrs by Hoechst-33342 staining based cell counting method (Rvb > 25 microM) Cytotoxicity against human Fibroblast cells assessed as reduction in cell viability incubated for 48 hrs by Hoechst-33342 staining based cell counting method (Rvb > 25 microM)	[PMID: 33422908]
HCT-116	IC₅₀	>25 μM Compound: 7h; DB18	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by Hoechst-33342 staining based cell counting method (Rvb > 25 microM) Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by Hoechst-33342 staining based cell counting method (Rvb > 25 microM)	[PMID: 33422908]
HT-22	IC₅₀	100 μM Compound: 39; DB18	Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 36876904]
Huh-7	IC₅₀	25 μM Compound: 7h; DB18	Cytotoxicity against human HuH-7 cells assessed as reduction in cell viability incubated for 48 hrs by Hoechst-33342 staining based cell counting method (Rvb > 25 microM) Cytotoxicity against human HuH-7 cells assessed as reduction in cell viability incubated for 48 hrs by Hoechst-33342 staining based cell counting method (Rvb > 25 microM)	[PMID: 33422908]
MCF7	IC₅₀	4 μM Compound: 7h; DB18	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by Hoechst-33342 staining based cell counting method (Rvb > 25 microM) Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by Hoechst-33342 staining based cell counting method (Rvb > 25 microM)	[PMID: 33422908]
MDA-MB-231	IC₅₀	>25 μM Compound: 7h; DB18	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by Hoechst-33342 staining based cell counting method (Rvb > 25 microM) Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by Hoechst-33342 staining based cell counting method (Rvb > 25 microM)	[PMID: 33422908]
NCI-H727	IC₅₀	>25 μM Compound: 7h; DB18	Cytotoxicity against human NCI-H727 cells assessed as reduction in cell viability incubated for 48 hrs by Hoechst-33342 staining based cell counting method (Rvb > 25 microM) Cytotoxicity against human NCI-H727 cells assessed as reduction in cell viability incubated for 48 hrs by Hoechst-33342 staining based cell counting method (Rvb > 25 microM)	[PMID: 33422908]
PC-3	IC₅₀	7 μM Compound: 7h; DB18	Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 48 hrs by Hoechst-33342 staining based cell counting method (Rvb > 25 microM) Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 48 hrs by Hoechst-33342 staining based cell counting method (Rvb > 25 microM)	[PMID: 33422908]

Chemical Information

CAS No. 2587177-94-2
Appearance Solid
Masse moléculaire 487.90
Formule C₂₄H₁₈ClN₇O₃
Color Light yellow to yellow
SMILES

CC1=CC=C(C([N+]([O-])=O)=C1)N2C=C(N=N2)COC3=CC=CC4=C3N=C(N=C4)NC5=CC=CC(Cl)=C5
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (102.48 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0496 mL

10.2480 mL

20.4960 mL

5 mM

0.4099 mL

2.0496 mL

4.0992 mL

10 mM

0.2050 mL

1.0248 mL

2.0496 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: 2.5 mg/mL (5.12 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.5 mg/mL (5.12 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Brahmaiah D, et al. Discovery of DB18, a potent inhibitor of CLK kinases with a high selectivity against DYRK1A kinase. Bioorg Med Chem. 2021 Feb 1;31:115962. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.0496 mL	10.2480 mL	20.4960 mL	51.2400 mL
	5 mM	0.4099 mL	2.0496 mL	4.0992 mL	10.2480 mL
	10 mM	0.2050 mL	1.0248 mL	2.0496 mL	5.1240 mL
	15 mM	0.1366 mL	0.6832 mL	1.3664 mL	3.4160 mL
	20 mM	0.1025 mL	0.5124 mL	1.0248 mL	2.5620 mL
	25 mM	0.0820 mL	0.4099 mL	0.8198 mL	2.0496 mL
	30 mM	0.0683 mL	0.3416 mL	0.6832 mL	1.7080 mL
	40 mM	0.0512 mL	0.2562 mL	0.5124 mL	1.2810 mL
	50 mM	0.0410 mL	0.2050 mL	0.4099 mL	1.0248 mL
	60 mM	0.0342 mL	0.1708 mL	0.3416 mL	0.8540 mL
	80 mM	0.0256 mL	0.1281 mL	0.2562 mL	0.6405 mL
	100 mM	0.0205 mL	0.1025 mL	0.2050 mL	0.5124 mL

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DB18

MCE Bioactive Compound Library

Voir tous les produits spécifiques à Isoform CDK

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

DB18 Related Classifications

HY-131978 Related Classifications