Cat. No.: HY-111546

BI-3663

1 Cited Publications

고객리뷰

Based on 1 publication(s) in Google Scholar

BI-3663 is a highly selective PTK2/FAK PROTAC (DC₅₀ = 30 nM) with a Cereblon E3 ligase ligand capable of degrading PTK2, with an IC₅₀ value of 18 nM. BI-3663 is a PROTAC generated by linking the PTK2/FAK inhibitor BI-4464 (HY-124625) with a Pomalidomide (HY-10984) derivative via a linker. BI-3663 can induce PTK2 degradation at low nanomolar concentrations. BI-3663 has antitumor activity.
(Pink: FAK ligand (HY-43760); Blue: Cereblon ligand (HY-10984); Black: linker (HY-42490)).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

The BI-3663 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.

Purity: 99.84%
CAS No.: 2341740-84-7
화학식: C₄₄H₄₂F₃N₇O₁₂
분자량:917.84

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

BI-3663 Chemical Structure

CAS No.: 2341740-84-7

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Fluorescent Dye

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Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (1)
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

BI-3663 is a highly selective PTK2/FAK PROTAC (DC₅₀ = 30 nM) with a Cereblon E3 ligase ligand capable of degrading PTK2, with an IC₅₀ value of 18 nM. BI-3663 is a PROTAC generated by linking the PTK2/FAK inhibitor BI-4464 (HY-124625) with a Pomalidomide (HY-10984) derivative via a linker. BI-3663 can induce PTK2 degradation at low nanomolar concentrations. BI-3663 has antitumor activity^[1]. (Pink: FAK ligand (HY-43760); Blue: Cereblon ligand (HY-10984); Black: linker (HY-42490)).

IC₅₀ & Target^[1]

PTK2/FAK

18 nM (IC₅₀)

Cereblon

All PROTACs Isoforms :

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].

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

Chemical Information

CAS No. 2341740-84-7
Appearance Solid
분자량 917.84
화학식 C₄₄H₄₂F₃N₇O₁₂
Color Light yellow to yellow
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
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Structure

PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]

2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062

용액&용해도

In Vitro:

DMSO : 300 mg/mL (326.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Popow J, et al. Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions. J Med Chem. 2019 Mar 14;62(5):2508-2520. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.0895 mL	5.4476 mL	10.8951 mL	27.2379 mL
	5 mM	0.2179 mL	1.0895 mL	2.1790 mL	5.4476 mL
	10 mM	0.1090 mL	0.5448 mL	1.0895 mL	2.7238 mL
	15 mM	0.0726 mL	0.3632 mL	0.7263 mL	1.8159 mL
	20 mM	0.0545 mL	0.2724 mL	0.5448 mL	1.3619 mL
	25 mM	0.0436 mL	0.2179 mL	0.4358 mL	1.0895 mL
	30 mM	0.0363 mL	0.1816 mL	0.3632 mL	0.9079 mL
	40 mM	0.0272 mL	0.1362 mL	0.2724 mL	0.6809 mL
	50 mM	0.0218 mL	0.1090 mL	0.2179 mL	0.5448 mL
	60 mM	0.0182 mL	0.0908 mL	0.1816 mL	0.4540 mL
	80 mM	0.0136 mL	0.0681 mL	0.1362 mL	0.3405 mL
	100 mM	0.0109 mL	0.0545 mL	0.1090 mL	0.2724 mL

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BI-3663

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Cytoskeleton Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) BI-3663

All PROTACs Isoforms

Biological Activity

Chemical Information

Publications (1)

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

BI-3663

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Cytoskeleton Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) BI-3663

All PROTACs Isoforms

Biological Activity

Chemical Information

Publications (1)

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

BI-3663 Related Classifications

HY-111546 Related Classifications