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Art. -Nr.: HY-157228

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ACBI3

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ACBI3 (compound 7), a chemical probe, is a PROTAC targeting KRAS. ACBI3 achieves in vivo degradation of oncogenic KRAS, resulting in durable pathway modulation and tumor regressions in KRAS mutant xenograft mouse models.
(Pink: K-Ras WT ligand (HY-162960); Blue: VHL ligand (HY-401613); Black: linker (HY-169992)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

The ACBI3 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.

Reinheit: 99.47%
CAS. Nr.: 2938169-76-5
Formel: C₅₀H₆₂N₁₄O₆S₂
Molecular Weight:1019.25

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

ACBI3 Chemical Structure

CAS. Nr.: 2938169-76-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

ACBI3 (compound 7), a chemical probe, is a PROTAC targeting KRAS. ACBI3 achieves in vivo degradation of oncogenic KRAS, resulting in durable pathway modulation and tumor regressions in KRAS mutant xenograft mouse models^[1]^[2]^[3]. (Pink: K-Ras WT ligand (HY-162960); Blue: VHL ligand (HY-401613); Black: linker (HY-169992)).

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Ras Isoform-spezifische Produkte anzeigen :

In Vitro

ACBI3 (0.01-10000 nM, 5 days) exhibits antiproliferative activity in KRAS mutant versus KRAS^WT cell lines (geometric mean IC₅₀ =478 nM versus 8.3 μM, respectively). ACBI3 exhibits high efflux in the Caco-2 assay in LS513 cells^[1]^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

ACBI3 (2 mg/kg i.v. or 30 mg/kg s.c., or 30 mg/kg i.p., once a day for 3 days) achieves in vivo degradation of oncogenic KRAS, resulting in durable pathway modulation and tumor regressions in KRAS mutant xenograft mouse models^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

KRAS mutant xenograft mouse models^[1]
Dosage:

2 mg/kg i.v. or 30 mg/kg s.c. or 30 mg/kg i.p.
Administration:

once a day for 3 days
Result:

Resulted in pronounced tumor regressions with a tumor growth inhibition of 127% in KRAS mutant xenograft mouse models.

Chemical Information

CAS. Nr. 2938169-76-5
Appearance Solid
Molecular Weight 1019.25
Formel C₅₀H₆₂N₁₄O₆S₂
Color White to yellow
SMILES

NC(SC1=C2[C@](C3=NC(C4=NC(N5CCCN(CCCCOC(N=N6)=CN6[C@@H](C(C)C)C(N7[C@H](C(N[C@@H](CO)C8=CC=C(C=C8)C9=C(N=CS9)C)=O)C[C@@H](O)C7)=O)C[C@@H]5C)=NC=C4)=NO3)(C)CCC1)=C2C#N
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 140 mg/mL (137.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.9811 mL

4.9056 mL

9.8111 mL

5 mM

0.1962 mL

0.9811 mL

1.9622 mL

10 mM

0.0981 mL

0.4906 mL

0.9811 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Popow J, et al. Targeting cancer with small molecule pan-KRAS degraders[J]. bioRxiv, 2023: 2023.10. 24.563163.

[2]. Hamilton G, et al. Development of PROTACS degrading KRAS and SOS1. Oncol Res. 2024 Jul 17;32(8):1257-1264. [Content Brief]

[3]. Cox AD, et al. KRAS takes the road to destruction. Science. 2024 Sep 20;385(6715):1274-1275. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	0.9811 mL	4.9056 mL	9.8111 mL	24.5278 mL
	5 mM	0.1962 mL	0.9811 mL	1.9622 mL	4.9056 mL
	10 mM	0.0981 mL	0.4906 mL	0.9811 mL	2.4528 mL
	15 mM	0.0654 mL	0.3270 mL	0.6541 mL	1.6352 mL
	20 mM	0.0491 mL	0.2453 mL	0.4906 mL	1.2264 mL
	25 mM	0.0392 mL	0.1962 mL	0.3924 mL	0.9811 mL
	30 mM	0.0327 mL	0.1635 mL	0.3270 mL	0.8176 mL
	40 mM	0.0245 mL	0.1226 mL	0.2453 mL	0.6132 mL
	50 mM	0.0196 mL	0.0981 mL	0.1962 mL	0.4906 mL
	60 mM	0.0164 mL	0.0818 mL	0.1635 mL	0.4088 mL
	80 mM	0.0123 mL	0.0613 mL	0.1226 mL	0.3066 mL
	100 mM	0.0098 mL	0.0491 mL	0.0981 mL	0.2453 mL

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

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ACBI3

PROTAC Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Ras Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ACBI3 Related Classifications

HY-157228 Related Classifications