2. PROTAC MAPK/ERK Pathway
  3. PROTACs Raf
  4. Tagarafdeg

Tagarafdeg (CFT1946) is an orally active, CRBN-based and mutant-selective bifunctional degradation activating compound (BiDAC) degrader of BRAFV600E with a DC50 of 14 nM in A375 cells. Tagarafdeg is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAFV600E splice variant. Tagarafdeg can be used in tumor research.

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Tagarafdeg

Tagarafdeg Chemische Struktur

CAS. Nr. : 2882165-79-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Tagarafdeg Related Antibodies

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Beschreibung

Tagarafdeg (CFT1946) is an orally active, CRBN-based and mutant-selective bifunctional degradation activating compound (BiDAC) degrader of BRAFV600E with a DC50 of 14 nM in A375 cells. Tagarafdeg is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAFV600E splice variant. Tagarafdeg can be used in tumor research[1][2].

IC50 & Target[1]

Cereblon

 

BRafV600E

 

In Vitro

Tagarafdeg (CFT1946) (100 nM; 24 h) causes BRAFV600E degradation and inhibits MAPK Signaling with pERK loss in BRAFV600E cells but not in WT-BRAF cells[2].

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

Tagarafdeg Related Antibodies

Western Blot Analysis[2]

Cell Line: A375 cells
Concentration: 100 nM
Incubation Time: 24 h
Result: Caused BRAFV600E degradation.
In Vivo

Tagarafdeg (CFT1946) (0.3-10 mg/kg; PO; BID; 20 days) induces tumor regression in the BRAFV600E A375 xenograft mouse model with 10 mg/kg[2].

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

Animal Model: BRAFV600E A375 xenograft mouse model[2]
Dosage: 0.3, 3, 10 mg/kg
Administration: PO; BID; 20 days
Result: Shows dose-dependent tumor regression.
10 mg/kg BID dose resulted in sustained tumor regression and is the minimum efficacious dose.
Klinische Studie
Molekulargewicht

958.00

Formel

C45H49F2N11O9S
CAS. Nr.
Appearance

Solid

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
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)

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0438 mL 5.2192 mL 10.4384 mL
5 mM 0.2088 mL 1.0438 mL 2.0877 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 (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

  • Verdünnungsrechner

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Reinheit & Dokumentation
Verweise

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 (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.

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
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Tagarafdeg Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tagarafdeg2882165-79-7CFT1946CFT 1946CFT-1946PROTACsRafRaf kinasesOrallyCRBNbifunctional degradation activating compoundBiDACBRAFV600EA375G469AG466Vp61-BRAFV600EtumorInhibitorinhibitorinhibit

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