Shopping Cart

Your shopping cart is currently empty

Tagarafdeg

Name: Tagarafdeg
Brand: TargetMol
SKU: T77972
Price: 479 USD
Availability: InStock
Rating: 5 (10 reviews)

Copy Product Info

😃Good

Catalog No. T77972Cas No. 2882165-79-7

Alias CFT-1946, CFT1946, CFT 1946

Tagarafdeg (CFT1946) is an orally available PROTAC degradator targeting mutant BRAF, capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (type III) mutations, and the p61-BRAF V600E splice variant. It exhibits favourable selectivity within the proteome, including for wild-type BRAF and CRAF, and inhibits tumour cell proliferation.

Tagarafdeg

Copy Product Info

😃Good

Catalog No. T77972Alias CFT-1946, CFT1946, CFT 1946Cas No. 2882165-79-7

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$479	-	In Stock
5 mg	$1,880	-	In Stock
10 mg	$2,570	-	In Stock

Add to Cart

Add to Quotation

In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Questions

Batch Information

Select Batch

Purity:＞99.99%

Appearance:Solid

Color:White

Resource Download

COA HPLC HNMR MS

Product Introduction

Bioactivity

Description	Tagarafdeg (CFT1946) is an orally available PROTAC degradator targeting mutant BRAF, capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (type III) mutations, and the p61-BRAF V600E splice variant. It exhibits favourable selectivity within the proteome, including for wild-type BRAF and CRAF, and inhibits tumour cell proliferation.
In vitro	In A375 cells, Tagarafdeg (CFT1946) effectively degraded BRAFV600E (Emax = 26%; DC50 = 14 nM, 24 hours) and inhibited ERK phosphorylation (IC50 = 11 nM, 24 hours) and cell growth (GI50 = 94 nM, 96 hours), while having no effect on the mutant KRAS-driven cell line HCT116. [2]
In vivo	METHODS: Tagarafdeg (10 mg/kg, orally, twice daily) was used to treat A375 xenograft mice, and tumor growth in the mice was observed. RESULTS: Tagarafdeg resulted in deeper tumor regression. [2]
Synonyms	CFT-1946, CFT1946, CFT 1946

Chemical Properties

Molecular Weight	958
Formula	C₄₅H₄₉F₂N₁₁O₉S
Cas No.	2882165-79-7
Smiles	CN1C=2C(C(=N1)N3C(=O)NC(=O)CC3)=CC(F)=C(C2)N4CCC(CC(=O)N5CCC6(CC5)C[C@H](CO6)N7C(=O)C=8C(N=C7)=CC=C(OC9=C(C#N)C(NS(N(CC)C)(=O)=O)=CC=C9F)C8)(O)CC4

Storage & Solubility Information

Storage

keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 80 mg/mL (83.51 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.0438 mL	5.2192 mL	10.4384 mL	52.1921 mL
5 mM	0.2088 mL	1.0438 mL	2.0877 mL	10.4384 mL
10 mM	0.1044 mL	0.5219 mL	1.0438 mL	5.2192 mL
20 mM	0.0522 mL	0.2610 mL	0.5219 mL	2.6096 mL
50 mM	0.0209 mL	0.1044 mL	0.2088 mL	1.0438 mL

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc