2. Epigenetics
    Stem Cell/Wnt
    Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  3. JAK
  4. 2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide

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

Cat. No.: HY-120469 Purity: 98.78%
COA Handling Instructions

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

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

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

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

CAS No. : 1258292-64-6

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 165 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 165 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
25 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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  • Customer Review

Description

GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with Kis 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)

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].

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].

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

350.20

Appearance

Solid

Formula

C16H13Cl2N3O2
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

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

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

  • Molarity Calculator

  • Dilution Calculator

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide1258292-64-6JAKJanus kinaseinflammatoryboweldiseasesIBDIL-23IL-12TYK2JAK1JAK2JAK3Inhibitorinhibitorinhibit

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