1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. AZ12672857

AZ12672857 

Cat. No.: HY-136895 Purity: 98.44%
Handling Instructions

AZ12672857 is an orally active inhibitor of EphB4 (IC50=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC50=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC50=9 nM).

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

AZ12672857 Chemical Structure

AZ12672857 Chemical Structure

CAS No. : 945396-55-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 428 In-stock
Estimated Time of Arrival: December 31
5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 680 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3400 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

AZ12672857 is an orally active inhibitor of EphB4 (IC50=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC50=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC50=9 nM)[1].

IC50 & Target[1]

EP4

1.3 nM (IC50)

Src

 

In Vitro

AZ12672857 shows only modest inhibition of CYP P450 (IC50=5 μM against 2C9 and 3A4, >10 μM against 1A4, 2D6 and 2C19). AZ12672857 inhibits p-KDR in HUVEC with an IC50 of 240 nM and inhibits p-PDGFR-βin MG63 cell line with an IC50 of 58 nM[1].

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

Molecular Weight

486.57

Formula

C₂₆H₃₀N₈O₂

CAS No.
SMILES

CN(C1=CC=CC2=C1C=NN2)C3=NC(NC4=CC(N5CCOCC5)=CC(N6CCOCC6)=C4)=NC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (51.38 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0552 mL 10.2760 mL 20.5520 mL
5 mM 0.4110 mL 2.0552 mL 4.1104 mL
10 mM 0.2055 mL 1.0276 mL 2.0552 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 (4.27 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.27 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

AZ12672857AZ 12672857AZ-12672857Prostaglandin Receptorproliferationsurvivalcancer3T3cellsCHO-K1autophosphorylationoralInhibitorinhibitorinhibit

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Product Name:
AZ12672857
Cat. No.:
HY-136895
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