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Tagarafdeg

Name: Tagarafdeg
Brand: TargetMol
SKU: T77972
Rating: 4.5 (1 reviews)

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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

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

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

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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.

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Purity:＞99.99%

Resource Download

COA HNMR MS HPLC

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
Color	White
Appearance	Solid

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

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In Vivo Formulation Calculator (Clear solution)

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

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

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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