BTX-6654 formate |
Catalog No.GC81460
One-Click Copy Product Info
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BTX-6654 formate is a SOS1 PROTAC degrader.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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In Vivo, BTX-6654 (25-40 days) dose-dependently degrades SOS1 protein and inhibits tumor growth in two KRAS G12C xenograft mouse models, and exerts a synergistic tumor growth inhibitory effect when combined with the KRAS inhibitor (Sotorasib) or the MEK inhibitor (Trametinib) [1].
In Vitro, BTX-6654 potently and specifically degrades SOS1 in KRAS-mutant cancer cells, with a DC50 value of < 11 nM; it also inhibits the downstream pERK and pS6 signaling pathways, with corresponding IC50 values of 1-32 nM and 4-22 nM, respectively[1]. BTX-6654 potently inhibits the viability of specific human cancer cell lines (including MIA PaCa-2, A549, NCI-H1975 and SNU-175), with IC50 values as low as 1.2 nM, but shows no significant activity against many other cancer cell lines with specific KRAS, NRAS, BRAF, NF1 mutations or KRAS deletion status (IC50 >2500 nM)[1].
References:
[1]. Begovich K, et al. Cereblon-based Bifunctional Degrader of SOS1, BTX-6654, Targets Multiple KRAS Mutations and Inhibits Tumor Growth. Molecular cancer therapeutics. 2024 Apr 02;23(4):407-420.
| Cas No. | SDF | ||
| Formula | C51H59F4N9O7 | M.Wt | 986.06 |
| Solubility | DMSO: 100 mg/mL (101.41 mM; Need ultrasonic) | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.0141 mL | 5.0707 mL | 10.1414 mL |
| 5 mM | 202.8 μL | 1.0141 mL | 2.0283 mL |
| 10 mM | 101.4 μL | 507.1 μL | 1.0141 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: >98.50% 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.)