1. Cell Cycle/DNA Damage
    Epigenetics
  2. PARP
  3. AZ6102

AZ6102 

Cat. No.: HY-12975 Purity: 99.65%
Handling Instructions

AZ6102 is a potent dual TNKS1 and TNKS2 inhibitor, with IC50s of 3 nM and 1 nM, respectively, and alao has 100-fold selectivity against other PARP family enzymes, with IC50s of 2.0 μM, 0.5 μM, and >3 μM, for PARP1, PARP2, and PARP6, respectively.

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

AZ6102 Chemical Structure

AZ6102 Chemical Structure

CAS No. : 1645286-75-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 88 In-stock
Estimated Time of Arrival: December 31
5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 140 In-stock
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25 mg USD 280 In-stock
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50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 750 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

AZ6102 is a potent dual TNKS1 and TNKS2 inhibitor, with IC50s of 3 nM and 1 nM, respectively, and alao has 100-fold selectivity against other PARP family enzymes, with IC50s of 2.0 μM, 0.5 μM, and >3 μM, for PARP1, PARP2, and PARP6, respectively.

IC50 & Target

IC50: 3 nM (TNKS1), 1 nM (TNKS2), 2.0 μM (PARP1), 0.5 μM (PARP2), >3 μM (PARP6)[1]

In Vitro

AZ6102 is a potent dual TNKS1 and TNKS2 inhibitor, with IC50s of 3 nM and 1 nM, respectively. AZ6102 alao has 100-fold selectivity against other PARP family enzymes, with IC50s of 2.0 μM, 0.5 μM, and >3 μM, for PARP1, PARP2, and PARP6, respectively. AZ6102 shows Wnt pathway inhibition in DLD-1 cells[1].

Molecular Weight

428.53

Formula

C₂₅H₂₈N₆O

CAS No.

1645286-75-4

SMILES

O=C1C2=C(N(C)C=C2)N=C(C3=CC=C(C4=C(C)C=C(N5C[[email protected]@H](C)N[[email protected]@H](C)C5)N=C4)C=C3)N1

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 : ≥ 29 mg/mL (67.67 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3336 mL 11.6678 mL 23.3356 mL
5 mM 0.4667 mL 2.3336 mL 4.6671 mL
10 mM 0.2334 mL 1.1668 mL 2.3336 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

The assay is conducted using 0.11 μM of tankyrase-1 protein and 3 μM nicotinamide adenine dinucleotide (NAD+, 2.12 μM 3H-NAD+ with a specific radioactivity of 1690 Ci/mol, 0.88 μM biotin- NAD+), in pH 7.5 Tris buffer (60 mM Tris, 1 mM DTT, 0.01% (v/v) Tween-20®, 2.5 mM MgCl2, 0.3 mg/mL BSA). For IC50 determination, 10 mM DMSO stock solution of a compound (AZ6102) is sequentially diluted by two-fold in DMSO, and aliquots of the diluted solutions are transferred to 384-well assay plates and mixed with Tankyrase-1 solution[1].

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

References

Purity: 99.65%

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AZ6102
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