2. PROTAC MAPK/ERK Pathway
  3. PROTACs Raf
  4. CFT1946

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. CFT1946 is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAFV600E splice variant. CFT1946 can be used in tumor research.

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

CFT1946 Chemical Structure

CFT1946 Chemical Structure

CAS No. : 2882165-79-7

Size Price Stock Quantity
1 mg USD 580 In-stock
5 mg USD 2300 In-stock
10 mg   Get quote  
50 mg   Get quote  

* Please select Quantity before adding items.

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

Customer Review

Based on 1 publication(s) in Google Scholar

CFT1946 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All Raf Isoform Specific Products:

View All Isoforms
BRaf c-Raf Raf

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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. CFT1946 is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAFV600E splice variant. CFT1946 can be used in tumor research[1][2].

IC50 & Target[1]

Cereblon

 

BRafV600E

 

In Vitro

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.

CFT1946 Related Antibodies

Western Blot Analysis[2]

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

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.
Clinical Trial
Molecular Weight

958.00

Formula

C45H49F2N11O9S
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light, stored under nitrogen

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

Solvent & Solubility
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.

  • Molarity Calculator

  • Dilution Calculator

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
Purity & Documentation
References

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

CFT1946 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:

CFT19462882165-79-7CFT 1946CFT-1946PROTACsRafRaf kinasesOrallyCRBNbifunctional degradation activating compoundBiDAC?BRAFV600EA375G469AG466Vp61-BRAFV600EtumorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CFT1946
Cat. No.:
HY-153341
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.