2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. ACBI2

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.

For research use only. We do not sell to patients.

ACBI2 Chemical Structure

ACBI2 Chemical Structure

CAS No. : 2913161-19-8

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Based on 1 publication(s) in Google Scholar

ACBI2 Related Antibodies

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Description

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[1].

IC50 & Target[1]

VHL

7 nM (EC50)

SMARCA2

 

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.

ACBI2 Related Antibodies
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.
Molecular Weight

1064.16

Formula

C56H68BrFN8O5S
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9397 mL 4.6985 mL 9.3971 mL
5 mM 0.1879 mL 0.9397 mL 1.8794 mL
View the Complete Stock Solution Preparation Table

* 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.76%

SDS (251 KB)

COA (252 KB) HNMR (355 KB) LCMS (97 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

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
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ACBI2 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ACBI22913161-19-8ACBI 2ACBI-2PROTACsEpigenetic Reader DomainA549NCI-H1568lung cancerSMARCA2RKO cellInhibitorinhibitorinhibit

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