1. PROTAC Cell Cycle/DNA Damage
  2. PROTACs SWI/SNF Complex
  3. 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.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

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.

ACBI2

ACBI2 화학구조

CAS No. : 2913161-19-8

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
1 mg 해외재고보유
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

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

 

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.
분자량

1064.16

화학식

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

선적

Room temperature in continental US; may vary elsewhere.

보관
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
용액&용해도
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.

  • 몰농도 계산기

  • 농도 희석 계산기

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

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

Purity: 99.38%

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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  • 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.

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Inquiry Information

상품명:
ACBI2
Cat. No.:
HY-151623
수량:
MCE Japan Authorized Agent: