Cat. No.: HY-120469

2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide

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Based on 1 Customer Validation

GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with K_is of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively.

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Pureté: 99.80%
CAS No.: 1258292-64-6
Formule: C₁₆H₁₃Cl₂N₃O₂
Masse moléculaire:350.20

Stockage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide Chemical Structure

CAS No.: 1258292-64-6

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with K_is of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively^[1].

IC₅₀ & Target^[1]

Tyk2

4.8 nM (Ki)

JAK1

0.7 nM (Ki)

JAK2

0.7 nM (Ki)

JAK3

0.4 nM (Ki)

Voir tous les produits spécifiques à Isoform JAK :

Cellular Effect

Cell Line	Type	Value	Description	References
TF-1	EC₅₀	1.7 μM Compound: 46	Inhibition of JAK2 in human TF1 cells assessed as inhibition of Epo-induced STAT5 phosphorylation pretreated for 20 minutes prior to addition of cytokine by cell-based assay Inhibition of JAK2 in human TF1 cells assessed as inhibition of Epo-induced STAT5 phosphorylation pretreated for 20 minutes prior to addition of cytokine by cell-based assay	[PMID: 23867602]
TF-1	EC₅₀	2 μM Compound: 46	Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation pretreated for 20 minutes prior to addition of cytokine by cell-based assay Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation pretreated for 20 minutes prior to addition of cytokine by cell-based assay	[PMID: 23867602]

In Vitro

In cell-based assays, GDC-046 demonstrates reasonable potency in blocking the IL-12 pathway (IL-12 pSTAT4 EC₅₀=380 nM) while displaying less activity in the EPO (JAK2) pathway (EPO pSTAT5 EC₅₀=1700 nM) and IL-6 (JAK1) pathway (IL-6 pSTAT3 EC₅₀=2000 nM)^[1].

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

In Vivo

In mice, GDC-046 exhibits relatively high clearance (65 mL/min/kg) when dosed intravenously (i.v. 1 mg/kg) and exhibits modest oral exposure (AUC=2.6 μM·h at p.o. 5 mg/kg)^[1].

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

Chemical Information

CAS No. 1258292-64-6
Appearance Solid
Masse moléculaire 350.20
Formule C₁₆H₁₃Cl₂N₃O₂
Color Off-white to yellow
SMILES

O=C(NC1=CC(NC(C2CC2)=O)=NC=C1)C3=C(Cl)C=CC=C3Cl
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvant et solubilité

In Vitro:

DMSO : 62.5 mg/mL (178.47 mM; Need ultrasonic; 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

2.8555 mL

14.2776 mL

28.5551 mL

5 mM

0.5711 mL

2.8555 mL

5.7110 mL

10 mM

0.2856 mL

1.4278 mL

2.8555 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 (protect from light). 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: ≥ 2.08 mg/mL (5.94 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.

Protocol 2

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

Solubility: ≥ 2.08 mg/mL (5.94 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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 (273 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Jun Liang, et al. Lead Optimization of a 4-aminopyridine Benzamide Scaffold to Identify Potent, Selective, and Orally Bioavailable TYK2 Inhibitors. J Med Chem. 2013 Jun 13;56(11):4521-36. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8555 mL	14.2776 mL	28.5551 mL	71.3878 mL
	5 mM	0.5711 mL	2.8555 mL	5.7110 mL	14.2776 mL
	10 mM	0.2856 mL	1.4278 mL	2.8555 mL	7.1388 mL
	15 mM	0.1904 mL	0.9518 mL	1.9037 mL	4.7592 mL
	20 mM	0.1428 mL	0.7139 mL	1.4278 mL	3.5694 mL
	25 mM	0.1142 mL	0.5711 mL	1.1422 mL	2.8555 mL
	30 mM	0.0952 mL	0.4759 mL	0.9518 mL	2.3796 mL
	40 mM	0.0714 mL	0.3569 mL	0.7139 mL	1.7847 mL
	50 mM	0.0571 mL	0.2856 mL	0.5711 mL	1.4278 mL
	60 mM	0.0476 mL	0.2380 mL	0.4759 mL	1.1898 mL
	80 mM	0.0357 mL	0.1785 mL	0.3569 mL	0.8923 mL
	100 mM	0.0286 mL	0.1428 mL	0.2856 mL	0.7139 mL

Keywords

2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide

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2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

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Anti-Breast Cancer Compound Library

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Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

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Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Voir tous les produits spécifiques à Isoform JAK

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Obesity Compound Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Voir tous les produits spécifiques à Isoform JAK

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide Related Classifications

HY-120469 Related Classifications