PROTAC FAK degrader 1

Name: PROTAC FAK degrader 1
Brand: MedChemExpress
SKU: HY-119932
Rating: 5.0 (5 reviews)

Cat. No.: HY-119932 Purity: 99.25%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

PROTAC FAK degrader 1 (Compound PROTAC-3) is a selective and effective degrader of Fak PROTAC with a DC₅₀ of 3.0 nM. PROTAC FAK degrader 1 reduces the ability of cancer cells to migrate and invade. PROTAC FAK degrader 1 can be used in the study of tumor. (Pink: Fak ligand (HY-44146); Black: Linker (HY-44141); Blue: VHL ligand 1 (HY-125845)).

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

PROTAC FAK degrader 1 Chemical Structure

CAS No. : 2301916-69-6

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 5 publication(s) in Google Scholar

Customer Validation

These results were obtained using AlphaLISA™ SureFire® Ultra™ assays

5 Publications Citing Use of MCE PROTAC FAK degrader 1

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Akt Akt1 Akt2 Akt3

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC₅₀: 6.5 nM (Focal adhesion kinase)
DC₅₀: 3.0 nM (Focal adhesion kinase) in PC3 cells^[1]

In Vitro

PROTAC FAK degrader 1 (0.5 nM-10 μM; 24 h) induces high-efficiency Fak degradation in PC3 cells in a dose-dependent manner, and significantly inhibits the phosphorylation levels of paxillin and Akt downstream of Fak^[1].
PROTAC FAK degrader 1 (50-250 nM; 24 h) reduces the migration and invasion ability of MDA-MB-231 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:	PC3 cells
Concentration:	0.5, 1, 5, 10, 50, 100 nM and 1 μM
Incubation Time:	24 h
Result:	Reduced the level of Fak in a dose-dependent manner.

Molecular Weight

996.13

Formula

C₄₇H₅₆F₃N₉O₈S₂

CAS No.

2301916-69-6

Appearance

Solid

Color

White to off-white

SMILES

O=C(N[C@H](C(N1[C@H](C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)C[C@@H](O)C1)=O)C(C)(C)C)CCOCCOC4=CC=C(NC5=NC(NCC6=CC=CC(N(C)S(C)(=O)=O)=C6)=C(C(F)(F)F)C=N5)C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 200 mg/mL (200.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.0039 mL	5.0194 mL	10.0389 mL
5 mM	0.2008 mL	1.0039 mL	2.0078 mL
10 mM	0.1004 mL	0.5019 mL	1.0039 mL

View the Complete Stock Solution Preparation Table

* 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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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: ≥ 5 mg/mL (5.02 mM); Suspended solution

This protocol yields a suspended solution of ≥ 5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (5.02 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.25%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (249 KB) HNMR (143 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

References

[1]. Cromm PM, et al. Addressing Kinase-Independent Functions of Fak via PROTAC-Mediated Degradation. J Am Chem Soc. 2018 Dec 12;140(49):17019-17026. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.0039 mL	5.0194 mL	10.0389 mL	25.0971 mL
	5 mM	0.2008 mL	1.0039 mL	2.0078 mL	5.0194 mL
	10 mM	0.1004 mL	0.5019 mL	1.0039 mL	2.5097 mL
	15 mM	0.0669 mL	0.3346 mL	0.6693 mL	1.6731 mL
	20 mM	0.0502 mL	0.2510 mL	0.5019 mL	1.2549 mL
	25 mM	0.0402 mL	0.2008 mL	0.4016 mL	1.0039 mL
	30 mM	0.0335 mL	0.1673 mL	0.3346 mL	0.8366 mL
	40 mM	0.0251 mL	0.1255 mL	0.2510 mL	0.6274 mL
	50 mM	0.0201 mL	0.1004 mL	0.2008 mL	0.5019 mL
	60 mM	0.0167 mL	0.0837 mL	0.1673 mL	0.4183 mL
	80 mM	0.0125 mL	0.0627 mL	0.1255 mL	0.3137 mL
	100 mM	0.0100 mL	0.0502 mL	0.1004 mL	0.2510 mL