CFT1946 |
Katalog-Nr.GC73432
One-Click Copy Product Info
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CFT1946 ist ein oral aktiver, CRBN-basierter und mutantenselektiver BiDAC-Abbauprodukt (BiDAC™) von BRAFV600E mit einem DC50 von 14 nM in A375-Zellen.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2882165-79-7
Sample solution is provided at 25 µL, 10mM.
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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.
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].
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].
References:
[1]. Sowa M E, et al. Preclinical evaluation of CFT1946 as a selective degrader of mutant BRAF for the treatment of BRAF driven cancers[J]. Cancer Research, 2022, 82(12_Supplement): 2158-2158. [2]. 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.
| Cas No. | 2882165-79-7 | SDF | |
| Formula | C45H49F2N11O9S | M.Wt | 958 |
| Löslichkeit | DMSO : 100 mg/mL (104.38 mM; Need ultrasonic) | Storage | 4°C, protect from light, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.0438 mL | 5.2192 mL | 10.4384 mL |
| 5 mM | 208.8 μL | 1.0438 mL | 2.0877 mL |
| 10 mM | 104.4 μL | 521.9 μL | 1.0438 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)