1. PROTAC
    Protein Tyrosine Kinase/RTK
  2. PROTAC
    FAK
  3. BI-3663

BI-3663 

Cat. No.: HY-111546 Purity: 98.14%
Handling Instructions

BI-3663 is a highly selective PTK2/FAK PROTAC, with cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC50 of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 (HY-124625) linked to Pomalidomide (HY-10984) with a linker. Anti-cancer activity.

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

BI-3663 Chemical Structure

BI-3663 Chemical Structure

CAS No. : 2341740-84-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 2423 In-stock
Estimated Time of Arrival: December 31
1 mg USD 550 In-stock
Estimated Time of Arrival: December 31
5 mg USD 1400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 2400 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Description

BI-3663 is a highly selective PTK2/FAK PROTAC, with cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC50 of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 (HY-124625) linked to Pomalidomide (HY-10984) with a linker[1]. Anti-cancer activity[1].

IC50 & Target[1]

PTK2/FAK

18 nM (IC50)

Cereblon

 

In Vitro

BI-3663 potently degrades PTK2 in Hep3B2.1-7 cells, and A549 cells, with pDC50s of 7.6 and 7.9, respectively[1].

Molecular Weight

917.84

Formula

C₄₄H₄₂F₃N₇O₁₂

CAS No.

2341740-84-7

SMILES

O=C(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCOCCOCCOCCNC(C4=CC=C(NC5=NC=C(C(F)(F)F)C(OC6=CC=CC(CC7)=C6C7=O)=N5)C(OC)=C4)=O

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 : 300 mg/mL (326.85 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0895 mL 5.4476 mL 10.8951 mL
5 mM 0.2179 mL 1.0895 mL 2.1790 mL
10 mM 0.1090 mL 0.5448 mL 1.0895 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: ≥ 7.5 mg/mL (8.17 mM); Clear solution

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

BI-3663BI3663BI 3663PROTACFAKProteolysis-targeting chimeraPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseInhibitorinhibitorinhibit

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BI-3663
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HY-111546
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