Referencia número: HY-151623

ACBI2

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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.

Para uso exclusivo en investigación. No vendemos a pacientes.

The ACBI2 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.

Pureza: 99.38%
No. CAS: 2913161-19-8
Fòrmula: C₅₆H₆₈BrFN₈O₅S
Peso molecular:1064.16

Almacenamiento:

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

ACBI2 Chemical Structure

No. CAS: 2913161-19-8

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Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

VHL

7 nM (EC₅₀)

SMARCA2

Ver todos los productos específicos de isoformas PROTACs :

Ver todos los productos específicos de isoformas SWI/SNF Complex :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	30 nM Compound: 6; ACBI2	Antiproliferative activity against SMARCA4-deficient human A549 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay Antiproliferative activity against SMARCA4-deficient human A549 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay	[PMID: 37523716]
NCI-H1299	GI₅₀	116 nM Compound: 6; ACBI2	Antiproliferative activity against SMARCA4-deficient human NCI-H1299 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay Antiproliferative activity against SMARCA4-deficient human NCI-H1299 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay	[PMID: 37523716]
NCI-H1693	GI₅₀	2.8 nM Compound: 6; ACBI2	Antiproliferative activity against SMARCA4-deficient human NCI-H1693 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay Antiproliferative activity against SMARCA4-deficient human NCI-H1693 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay	[PMID: 37523716]
NCI-H1792	GI₅₀	135 nM Compound: 6; ACBI2	Antiproliferative activity against human NCI-H1792 cells expressing wild-type SMARCA2 assessed as cell growth inhibition measured after 7 days by WST-8 assay Antiproliferative activity against human NCI-H1792 cells expressing wild-type SMARCA2 assessed as cell growth inhibition measured after 7 days by WST-8 assay	[PMID: 37523716]
NCI-H1793	GI₅₀	7.3 nM Compound: 6; ACBI2	Antiproliferative activity against SMARCA4-deficient human NCI-H1793 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay Antiproliferative activity against SMARCA4-deficient human NCI-H1793 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay	[PMID: 37523716]
NCI-H1944	GI₅₀	13 nM Compound: 6; ACBI2	Antiproliferative activity against SMARCA4-deficient human NCI-H1944 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay Antiproliferative activity against SMARCA4-deficient human NCI-H1944 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay	[PMID: 37523716]
NCI-H1975	GI₅₀	65 nM Compound: 6; ACBI2	Antiproliferative activity against human NCI-H1975 cells expressing wild-type SMARCA2 assessed as cell growth inhibition measured after 7 days by WST-8 assay Antiproliferative activity against human NCI-H1975 cells expressing wild-type SMARCA2 assessed as cell growth inhibition measured after 7 days by WST-8 assay	[PMID: 37523716]
NCI-H647	GI₅₀	165 nM Compound: 6; ACBI2	Antiproliferative activity against human NCI-H647 cells expressing wild-type SMARCA2 assessed as cell growth inhibition measured after 7 days by WST-8 assay Antiproliferative activity against human NCI-H647 cells expressing wild-type SMARCA2 assessed as cell growth inhibition measured after 7 days by WST-8 assay	[PMID: 37523716]
NCI-H838	GI₅₀	67 nM Compound: 6; ACBI2	Antiproliferative activity against SMARCA4-deficient human NCI-H838 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay Antiproliferative activity against SMARCA4-deficient human NCI-H838 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay	[PMID: 37523716]
SK-MEL-28	GI₅₀	>10 μM Compound: 6; ACBI2	Antiproliferative activity against human SK-MEL-28 cells expressing wild-type SMARCA2 assessed as cell growth inhibition measured after 7 days by WST-8 assay Antiproliferative activity against human SK-MEL-28 cells expressing wild-type SMARCA2 assessed as cell growth inhibition measured after 7 days by WST-8 assay	[PMID: 37523716]
SK-MEL-5	GI₅₀	4.9 nM Compound: 6; ACBI2	Antiproliferative activity against SMARCA4-deficient human SK-MEL-5 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay Antiproliferative activity against SMARCA4-deficient human SK-MEL-5 cells assessed as cell growth inhibition measured after 7 days by WST-8 assay	[PMID: 37523716]

In Vitro

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].

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

In Vivo

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].

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

Animal Model:

A549 xenograft mice model^[1]
Dosage:

80 mg/kg
Administration:

Oral administration (p.o.), once daily
Result:

Inhibited tumor growth and was well tolerated.

Chemical Information

No. CAS 2913161-19-8
Appearance Solid
Peso molecular 1064.16
Fòrmula C₅₆H₆₈BrFN₈O₅S
Color White to light yellow
SMILES

BrC1=CC=CC(N(C2=CC=C(C3CCN(CC[C@@H](C)CC[C@@H](C4=CC=C(C5=C(C)N=CS5)C=C4)NC([C@@H]6C[C@@H](O)CN6C([C@H](C(C)(C)C)NC(C7(CC7)F)=O)=O)=O)CC3)C=C2N8C9CCCC9)C8=N%10)=C1C%10=O
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Publications (1)

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Journal Impact Factor

Cell Chem Biol

Enhancer reprogramming underlies therapeutic utility of a SMARCA2 degrader in SMARCA4 mutant cancer. [Abstract]

2024 Oct 1:S2451-9456(24)00396-9. PMID: 39378885

Solvente y solubilidad

In Vitro:

DMSO : 125 mg/mL (117.46 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

0.9397 mL

4.6985 mL

9.3971 mL

5 mM

0.1879 mL

0.9397 mL

1.8794 mL

10 mM

0.0940 mL

0.4699 mL

0.9397 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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (276 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)
Instrucciones de manejo (2659 KB)

Referencias

[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. [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	0.9397 mL	4.6985 mL	9.3971 mL	23.4927 mL
	5 mM	0.1879 mL	0.9397 mL	1.8794 mL	4.6985 mL
	10 mM	0.0940 mL	0.4699 mL	0.9397 mL	2.3493 mL
	15 mM	0.0626 mL	0.3132 mL	0.6265 mL	1.5662 mL
	20 mM	0.0470 mL	0.2349 mL	0.4699 mL	1.1746 mL
	25 mM	0.0376 mL	0.1879 mL	0.3759 mL	0.9397 mL
	30 mM	0.0313 mL	0.1566 mL	0.3132 mL	0.7831 mL
	40 mM	0.0235 mL	0.1175 mL	0.2349 mL	0.5873 mL
	50 mM	0.0188 mL	0.0940 mL	0.1879 mL	0.4699 mL
	60 mM	0.0157 mL	0.0783 mL	0.1566 mL	0.3915 mL
	80 mM	0.0117 mL	0.0587 mL	0.1175 mL	0.2937 mL
	100 mM	0.0094 mL	0.0470 mL	0.0940 mL	0.2349 mL

Keywords

ACBI2

1 Cited Publications

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ACBI2

PROTAC Library

Publications Citing Use of MedChemExpress (MCE) ACBI2

Ver todos los productos específicos de isoformas PROTACs

Ver todos los productos específicos de isoformas SWI/SNF Complex

Actividad biológica

Chemical Information

Publications (1)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

ACBI2

PROTAC Library

Publications Citing Use of MedChemExpress (MCE) ACBI2

Ver todos los productos específicos de isoformas PROTACs

Ver todos los productos específicos de isoformas SWI/SNF Complex

Actividad biológica

Chemical Information

Publications (1)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

ACBI2 Related Classifications

HY-151623 Related Classifications