ACBI3 |
カタログ番号GC73732
One-Click Copy Product Info
|
ACBI3（化合物7）は汎KRAS分解剤である。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2938169-76-5
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
ACBI3 is a selective pan-KRAS degrader (PROTAC), composed of a target protein ligand (pan-KRAS degrader 1, used to bind KRAS protein), an E3 ligase ligand (E3 ligase Ligand 43, used to recruit the VHL E3 ubiquitin ligase complex), and a linker (1-Bromo-4-(ethynyloxy)butane, used to optimize spatial conformation). ACBI3 degrades oncogenic KRAS mutants and induces ubiquitination and degradation of KRAS protein by recruiting the E3 ubiquitin ligase VHL. ACBI3 can be used in research related to KRAS-driven cancers[1-4].
In vitro, GP5d (KRASG12D) cells and Cal-62 (KRASG12R) cells were treated with ACBI3 (0.03-10μM) for 18-24 hours. ACBI3 significantly degraded KRAS in GP5d cells but had no degradation effect on KRASG12R in Cal-62 cells[5]. Cell lines expressing KRAS mutations (GP5d, SW620, NCI-H358) were treated with ACBI3 (0.1nM-1μM) for 24 hours. ACBI3 significantly degraded KRAS protein, inhibited the MAPK signaling pathway, and suppressed cell proliferation[6].
In vivo, mice bearing GP2d cells were treated with ACBI3 (30mg/kg; s.c.; once daily) for 14 days. ACBI3 promoted KRAS degradation in vivo and led to tumor regression[6].
References:
[1] Kos T, Saur D. Breaking down KRAS: small-molecule degraders for cancer therapy. Signal Transduct Target Ther. 2025 Mar 14;10(1):86.
[2] Tang D, Kroemer G, Kang R. KRAS-targeted therapies in cancer: novel approaches and overcoming resistance. BMJ Oncol. 2025 Nov 21;4(1):e000946.
[3] Cox AD, Der CJ. KRAS takes the road to destruction. Science. 2024 Sep 20;385(6715):1274-1275.
[4] Hamilton G, Eggerstorfer MT, Stickler S. Development of PROTACS degrading KRAS and SOS1. Oncol Res. 2024 Jul 17;32(8):1257-1264..
[5] Vetma V, Puoti I, Karolak NK, et al. Identification of a Highly Cooperative PROTAC Degrader Targeting GTP-Loaded KRAS(On) Alleles. J Am Chem Soc. 2025 Nov 12;147(45):41367-41378.
[6] Popow J, Farnaby W, Gollner A, et al. Targeting cancer with small-molecule pan-KRAS degraders. Science. 2024 Sep 20;385(6715):1338-1347.
| Cell experiment [1]: | |
Cell lines | GP5d (KRASG12D mutant cell line), Cal-62 (KRASG12R mutant cell line), and other KRAS mutant-driven cancer cell lines |
Preparation Method | Cells were treated with ACBI3 (0.03-10μM) for 18-24 hours. |
Reaction Conditions | 0.03-10μM; 18-24h |
Applications | ACBI3 potently degraded multiple KRAS(off) alleles, including KRASG12D in GP5d cells, but did not effectively degrade KRASG12R in Cal-62 cells. ACBI3 inhibited the MAPK signaling pathway and exhibited antiproliferative effects in KRAS mutant-driven cancer cells. |
| Animal experiment [2]: | |
Animal models | GP2d tumor bearing mice (KRASG12D mutant) and RKN xenograft model (KRASG12V TP53R175H mutant) |
Preparation Method | GP2d tumor bearing mice were treated with ACBI3 daily via subcutaneous injection for up to 14 days. In separate experiments, ACBI3 was administered intraperitoneally as a nano-milled suspension. |
Dosage form | 30mg/kg; s.c.; daily for 14 days |
Applications | ACBI3 resulted in pronounced tumor regressions with 127% tumor growth inhibition, degraded murine KRAS in vivo, and was systemically tolerated with no impact on body weight. Subcutaneous administration caused skin lesions, leading to a switch to intraperitoneal delivery. |
References: | |
| Cas No. | 2938169-76-5 | SDF | |
| Formula | C50H62N14O6S2 | M.Wt | 1019.25 |
| 溶解度 | DMSO : 250 mg/mL (245.28 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. |
||
| 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 | 981.1 μL | 4.9056 mL | 9.8111 mL |
| 5 mM | 196.2 μL | 981.1 μL | 1.9622 mL |
| 10 mM | 98.1 μL | 490.6 μL | 981.1 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: >98.00% 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.)