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SGC-GAK-1 

Cat. No.: HY-122186 Purity: 99.76%
Handling Instructions

SGC-GAK-1 is a potent, selective cyclin G-associated kinase (GAK) inhibitor with a Ki of 3.1 nM. SGC-GAK-1 is a chemical probe for GAK.

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

SGC-GAK-1 Chemical Structure

SGC-GAK-1 Chemical Structure

CAS No. : 2226517-76-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 198 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 320 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Description

SGC-GAK-1 is a potent, selective cyclin G-associated kinase (GAK) inhibitor with a Ki of 3.1 nM. SGC-GAK-1 is a chemical probe for GAK[1].

IC50 & Target

Ki: 3.1 nM (GAK)[1]

In Vitro

SGC-GAK-1 potently binds cyclin G-associated kinase (GAK), adaptor protein 2-associated kinase (AAK1), serine/threonine kinase 16 (STK16) with Kis of 3.1 nM, 53 µM, 51 µM, respectively[1].
SGC-GAK-1 potently binds cyclin G-associated kinase (GAK), receptor-interacting protein kinase 2 (RIPK2), AarF domain containing kinase 3 (ADCK3), and nemo-like kinase (NLK) with KDs of 1.9 nM, 110 nM, 190 nM, and 520 nM, respectively[1].
SGCGAK-1 (0.1, 1, and 10 µM, 48 hours or 72 hours) shows strong growth inhibition in LNCaP, VCaP, and 22Rv1 cells at 10 µM, but minimal effect in PC3 and DU145 cells[1].

Cell Viability Assay[1]

Cell Line: Prostate cancer cells (22Rv1, LNCaP, VCaP, PC3, DU145)
Concentration: 0.1, 1, and 10 µM
Incubation Time: 48 hours or 72 hours
Result: Showed potent antiproliferative activity in LNCaP and 22Rv1 cells with IC50s of 0.05±0.15 µM and 0.17±0.65 µM, respectively.
Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (321.14 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5691 mL 12.8455 mL 25.6911 mL
5 mM 0.5138 mL 2.5691 mL 5.1382 mL
10 mM 0.2569 mL 1.2846 mL 2.5691 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 (5.34 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.34 mM); Clear solution

References
Molecular Weight

389.24

Formula

C₁₈H₁₇BrN₂O₃

CAS No.

2226517-76-4

SMILES

COC1=C(C(OC)=CC(NC2=CC=NC3=CC=C(C=C23)Br)=C1)OC

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

Room temperature in continental US; may vary elsewhere

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This equation is commonly abbreviated as: C1V1 = C2V2

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Product Name:
SGC-GAK-1
Cat. No.:
HY-122186
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SGC-GAK-1

Cat. No.: HY-122186