ACBI2 |
Catalog No.GC73359
One-Click Copy Product Info
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ACBI2 is a highly potent and orally active VHL PROTAC SMARCA2 degrader (EC50: 7 nM), which selectively degrades SMARCA2 with a DC50 value of 1 nM in RKO cells.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2913161-19-8
Sample solution is provided at 25 µL, 10mM.
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ACBI2 is a highly potent and orally active VHL PROTAC SMARCA2 degrader (EC50: 7 nM), which selectively degrades SMARCA2 with a DC50 value of 1 nM in RKO cells. ACBI2 can be used in the research of lung cancer.
ACBI2 degrades SMARCA2 and SMARCA4 in RKO cells, with DC50s of 1 nM and 32 nM respectively[1].ACBI2 (0.1 nM-1 μM, 4-18 h) rapidly and completely degrades SMARCA2 in two sensitive cell lines (A549 and NCI-H1568)[1].ACBI2 (1 nM-1 μM, 18 h) significantly degrades SMARCA2 with clear selectivity over SMARCA4[1].ACBI2 (0-1 μM; 18 h) dose-dependently degrades SMARCA2 in human whole blood[1].
ACBI2 (80 mg/kg, p.o., once daily) significantly inhibits tumor growth in an A549 xenograft mice model[1].ACBI2 (5-100 mg/kg, p.o., tumors collected 24 or 48 h after treatment) dose-dependently degrades tumor SMARCA2 in A549 engrafted tumor bearing mice (IHC staining)[1].ACBI2 (30 mg/kg, p.o., mice) shows oral bioavailability of 22%[1].
References:
[1]. Kofink C, et al. A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo. Nat Commun. 2022 Oct 10;13(1):5969.
| Cas No. | 2913161-19-8 | SDF | |
| Formula | C56H68BrFN8O5S | M.Wt | 1064.16 |
| Solubility | DMSO : 125 mg/mL (117.46 mM; Need ultrasonic) | Storage | -20°C |
| 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 | 939.7 μL | 4.6985 mL | 9.3971 mL |
| 5 mM | 187.9 μL | 939.7 μL | 1.8794 mL |
| 10 mM | 94 μL | 469.9 μL | 939.7 μL |
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.)