製品番号: HY-151623

ACBI2

1 Cited Publications

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

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.

純度: 99.38%
CAS 番号: 2913161-19-8
分子式: C₅₆H₆₈BrFN₈O₅S
分子量:1064.16

保管条件:

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

ACBI2 構造式

CAS 番号: 2913161-19-8

容量

価格（税別）

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数量

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (1)
溶剤 & 溶解度
- 体外
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

VHL

7 nM (EC₅₀)

SMARCA2

PROTACs アイソフォーム固有の製品をすべて表示 :

SWI/SNF Complex アイソフォーム固有の製品をすべて表示 :

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]

体外実験

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.

体内実験

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.

化学情報

CAS 番号 2913161-19-8
性状 Solid
分子量 1064.16
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

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.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (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)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

MedChemExpress（MCE）の使用を引用している文献 ACBI2

PROTACs アイソフォーム固有の製品をすべて表示

SWI/SNF Complex アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (1)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

ACBI2

PROTAC Library

MedChemExpress（MCE）の使用を引用している文献 ACBI2

PROTACs アイソフォーム固有の製品をすべて表示

SWI/SNF Complex アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (1)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

ACBI2 関連分類

HY-151623 関連分類