Art. -Nr.: HY-153341

Tagarafdeg

Name: Tagarafdeg
Brand: MedChemExpress
SKU: HY-153341
Price: 580.00 USD
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(Synonyms: CFT1946)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Tagarafdeg (CFT1946) is an orally active, blood-brain barrier-penetrant, and selective bifunctional BiDAC degrader of the BRAF^V600E/K mutant protein, with a DC₅₀ of 14 nM in A375 cells. Tagarafdeg mediates the ubiquitination and proteasomal degradation of BRAF mutant proteins. Tagarafdeg inhibits tumor progression in multiple models of BRAF^V600E-mutant intracranial tumors, melanoma, and colorectal cancer. Tagarafdeg is applicable to tumor-related research.
(Pink: Braf ligand (HY-187012); Blue: Cereblon ligand (HY-49385); Black: linker).

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Reinheit : 99.41%
CAS. Nr.: 2882165-79-7
Formel: C₄₅H₄₉F₂N₁₁O₉S
Molecular Weight:958.00

Speicherung:

4°C, protect from light, stored under nitrogen

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

Tagarafdeg Chemical Structure

CAS. Nr.: 2882165-79-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Tagarafdeg (CFT1946) is an orally active, blood-brain barrier-penetrant, and selective bifunctional BiDAC degrader of the BRAF^V600E/K mutant protein, with a DC₅₀ of 14 nM in A375 cells. Tagarafdeg mediates the ubiquitination and proteasomal degradation of BRAF mutant proteins. Tagarafdeg inhibits tumor progression in multiple models of BRAF^V600E-mutant intracranial tumors, melanoma, and colorectal cancer. Tagarafdeg is applicable to tumor-related research^[1]^[2]^[3]. (Pink: Braf ligand (HY-187012); Blue: Cereblon ligand (HY-49385); Black: linker).

IC₅₀ & Target

^[1]

BRaf^V600E

14 nM (DC₅₀)

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In Vitro

Tagarafdeg (CFT1946) (1-10000 nM; 24 h) degrades BRAF^V600E protein and downregulates pERK protein levels in a dose-dependent manner in A375 cells (DC₅₀ = 14 nM, E_max = 26%); it does not degrade wild-type BRAF protein in HCT116 cells harboring wild-type BRAF, and exerts almost no effect on the MAPK signaling pathway and cell proliferation^[1].
Tagarafdeg inhibits the proliferation of BRAF inhibitor-resistant A375‑NRAS Q61K cells (GI₅₀ = 150 nM); it exhibits weak antiproliferative activity against HepG2 cells (GI₅₀ >10 μM)^[1].
Tagarafdeg (100 nM; 24 h) induces the degradation of BRAF^V600E and inhibits MAPK signal transduction, resulting in the loss of pERK in BRAF^V600E cells, but exerts no effect in WT^V600E cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

A375 cells
Concentration:

100 nM
co‑treatment with 10 μM competing ligand (targeting ligand / CRBN ligand / MLN4924 (HY-70062) / Bortezomib (HY-10227))
Incubation Time:

24 h
Result:

Abolished CFT1946‑mediated BRAF‑V600E degradation via target‑ligand competition, CRBN‑ligand competition, CUL4‑E3 inhibition and proteasome inhibition.

Western Blot Analysis^[1]

Cell Line:

A375 cells
Concentration:

1, 10, 100, 1000, 10000 nM
Incubation Time:

24 h
Result:

Induced dose‑dependent BRAF‑V600E degradation and reduced pERK levels; the CRBN‑binding‑deficient analogue CFT1946^NMe failed to degrade BRAF‑V600E.

Western Blot Analysis^[1]

Cell Line:

HCT116 cells
Concentration:

1, 10, 100, 1000, 10000 nM
Incubation Time:

24 h
Result:

Exerted no obvious alterations on protein abundance of WT‑BRAF, pERK and total‑ERK.

In Vivo

Tagarafdeg (CFT1946) (0.3‑10 mg/kg; p.o., twice daily) produces dose-dependent tumor regression in the A375 BRAF^V600E xenograft mouse model^[1].

Tagarafdeg (10-30 mg/kg; oral administration, twice daily) inhibits tumor growth in BRAF inhibitor-resistant A375-NRAS Q61K xenograft mice, and its combination with the MEK inhibitor Trametinib (HY-10999) yields an enhanced antitumor effect^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2882165-79-7
Appearance Solid
Molecular Weight 958.00
Formel C₄₅H₄₉F₂N₁₁O₉S
Color Off-white to light yellow
SMILES

CN1C(C(C(N(CCC2=O)C(N2)=O)=N1)=C3)=CC(N(CC4)CCC4(O)CC(N5CCC6(C[C@@H](N(C=NC7=CC=C8OC(C(F)=CC=C9N[S](N(C)CC)(=O)=O)=C9C#N)C(C7=C8)=O)CO6)CC5)=O)=C3F
Synonyms

CFT1946
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light, stored under nitrogen

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

Publications (1)

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Drug Metab Dispos

2026 Jul 17.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (104.38 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

1.0438 mL

5.2192 mL

10.4384 mL

5 mM

0.2088 mL

1.0438 mL

2.0877 mL

10 mM

0.1044 mL

0.5219 mL

1.0438 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, 6 months; -20°C, 1 month (protect from light, 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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)

Verweise

[1]. Yanke Liang. The Discovery and Characterization of CFT1946: A Potent, Selective, and Orally Bioavailable Degrader of Mutant BRAF for the Treatment of BRAF-driven Cancers. ANNUAL MEETING, American Association for Cancer Research, 2023.

[2]. Rudolph J, et al. Contemporary design of small-molecule kinase modulators: orthosteric, allosteric and induced-proximity strategies. Nature reviews. Drug discovery. 2026 Aug;25(8):595-618.

[3]. Kreger B T, et al. CFT1946 Is an Orally Available Brain‑Penetrant BRAF^V600‑Mutant Degrader That Overcomes BRAF Inhibitor Resistance. Cancer Research, 2026, 86(2):438‑452.

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.0438 mL	5.2192 mL	10.4384 mL	26.0960 mL
	5 mM	0.2088 mL	1.0438 mL	2.0877 mL	5.2192 mL
	10 mM	0.1044 mL	0.5219 mL	1.0438 mL	2.6096 mL
	15 mM	0.0696 mL	0.3479 mL	0.6959 mL	1.7397 mL
	20 mM	0.0522 mL	0.2610 mL	0.5219 mL	1.3048 mL
	25 mM	0.0418 mL	0.2088 mL	0.4175 mL	1.0438 mL
	30 mM	0.0348 mL	0.1740 mL	0.3479 mL	0.8699 mL
	40 mM	0.0261 mL	0.1305 mL	0.2610 mL	0.6524 mL
	50 mM	0.0209 mL	0.1044 mL	0.2088 mL	0.5219 mL
	60 mM	0.0174 mL	0.0870 mL	0.1740 mL	0.4349 mL
	80 mM	0.0130 mL	0.0652 mL	0.1305 mL	0.3262 mL
	100 mM	0.0104 mL	0.0522 mL	0.1044 mL	0.2610 mL

Bioz

Tagarafdeg

1 Cited Publications

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Tagarafdeg

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