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Art. -Nr.: HY-147261

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B026

B026 is a selective, potent, orally active p300/CBP histone acetyltransferase (HAT) inhibitor with IC₅₀ values of 1.8 nM and 9.5 nM for p300 and CBP enzyme, respectively. B026 has anticancer activity for androgen receptor-positive (AR+) prostate cancer cell lines.

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CAS. Nr.: 2379416-48-3
Formel: C₂₇H₂₃F₄N₅O₄
Molecular Weight:557.50

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (280 KB)

B026 Chemical Structure

CAS. Nr.: 2379416-48-3

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

p300

8.1 nM (IC₅₀)

CBP

9.5 nM (IC₅₀)

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CWR22R	IC₅₀	4.4 nM Compound: B026	Antiproliferative activity against human 22Rv1 cells measured after 3 days by celltiter-glo luminescence assay Antiproliferative activity against human 22Rv1 cells measured after 3 days by celltiter-glo luminescence assay	[PMID: 31910017]
HT	IC₅₀	>10 μM Compound: B026	Antiproliferative activity against human HT cells measured after 3 days by celltiter-glo luminescence assay Antiproliferative activity against human HT cells measured after 3 days by celltiter-glo luminescence assay	[PMID: 31910017]
K562	IC₅₀	104.4 nM Compound: B026	Antiproliferative activity against human K562 cells measured after 3 days by celltiter-glo luminescence assay Antiproliferative activity against human K562 cells measured after 3 days by celltiter-glo luminescence assay	[PMID: 31910017]
Kasumi 1	IC₅₀	40.5 nM Compound: B026	Antiproliferative activity against human Kasumi-1 cells measured after 3 days by celltiter-glo luminescence assay Antiproliferative activity against human Kasumi-1 cells measured after 3 days by celltiter-glo luminescence assay	[PMID: 31910017]
LNCaP-Clone-FGC	IC₅₀	9.8 nM Compound: B026	Antiproliferative activity against human LNCaP-FGC cells measured after 5 days by celltiter-glo luminescence assay Antiproliferative activity against human LNCaP-FGC cells measured after 5 days by celltiter-glo luminescence assay	[PMID: 31910017]
Maver1	IC₅₀	2.6 nM Compound: B026	Antiproliferative activity against human Maver1 cells measured after 3 days by celltiter-glo luminescence assay Antiproliferative activity against human Maver1 cells measured after 3 days by celltiter-glo luminescence assay	[PMID: 31910017]
MV4-11	IC₅₀	4.2 nM Compound: B026	Antiproliferative activity against human MV4-11 cells measured after 3 days by celltiter-glo luminescence assay Antiproliferative activity against human MV4-11 cells measured after 3 days by celltiter-glo luminescence assay	[PMID: 31910017]

In Vitro

B026 (0-5 μM; 12 h; cancer cell lines) has antiproliferative activity^[1].
B026 (0-5 μM; 6 h; MV-4-11 cells) exhibits inhibitory effects on H3K27Ac expression^[1].
B026 (0-5 μM; 12 h; MV-4-11 cells) targets the cellular p300 protein and increases the thermal stability of p300 protein in a dose-dependent manner^[1].
B026 (0-1 μM; 24 h; MV-4-11 cells) decreases the expression of MYC, which a key oncogenictranscription factor that is regulated by superenhancer regions containing p300/CBP^[1].

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

Cell Viability Assay^[1]

Cell Line:

Maver-1, MV-4-11, K562, Kasumi-1, LnCaP-FGC and 22Rv1 cells
Concentration:

0-5 μM
Incubation Time:

12 hours
Result:

Inhibited cell growth with IC₅₀ values of 2.6, 4.2, 4.4, 9.8, 40.5 and 104.4 nM for Maver-1, MV-4-11, 22Rv1, LnCaP-FGC, Kasumi-1 and K562 cells, respectively.

Western Blot Analysis^[1]

Cell Line:

MV-4-11 cells
Concentration:

0, 0.313, 0.625, 1.25, 2.5 and 5 μM
Incubation Time:

6 hours
Result:

Decreased the expression of H3K27Ac in a dose-dependent manner.

In Vivo

B026 (1-3 mg/kg; i.v. and p.o.; 0-24 h; male SD rats) has a low clearance (13.4 mL/min/kg) and good oral exposure (AUC=3.71 μM·h) with good oral bioavailability (F=56%) in rat^[1].
B026 (50-100 mg/kg; p.o.; daily, for 28 days; balb/c female mice) inhibits tumor growth in a dose-dependent manner^[1].

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

Animal Model:

Balb/c female mice with MV-4-11 xenograft^[1]
Dosage:

50 and 100 mg/kg
Administration:

Oral administration; daily, for 28 days
Result:

Inhibited tumor growth with TGI of 75.0% at 50 mg/kg and 85.7% at 100 mg/kg, respectively.

Animal Model:

Male SD rats^[1]
Dosage:

1 and 3 mg/kg
Administration:

Intravenous injection and oral administration; 0.25, 0.5 , 1 , 2 , 4 , 8 and 24 hours

Result:

1.19

Administration	i.v. (1 mg/kg)	p.o. (3 mg/kg)
T_1/2 (h)	1.5	1.02
T_max (h)		0.83
C_max (μM)		1.12
AUC_last (μM·h)	2.22	3.71
Vd_ss (L/kg)	1.5
CL_{_obs} (mL/min/kg)	13.4
PPB %		98.2
F %		56

Chemical Information

CAS. Nr. 2379416-48-3
Molecular Weight 557.50
Formel C₂₇H₂₃F₄N₅O₄
SMILES

O=C1[C@@]2(NC(N1CC(N3[C@@H](COC4=CC=C(F)C=C4C3)C(F)(F)F)=O)=O)C5=CC=C(C6=CN(N=C6)C)C=C5CC2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 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]. Yang Y, et, al. Discovery of Highly Potent, Selective, and Orally Efficacious p300/CBP Histone Acetyltransferases Inhibitors. J Med Chem. 2020 Feb 13;63(3):1337-1360. [Content Brief]

Calculators

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)}

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.

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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B026

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

B026 Related Classifications

HY-147261 Related Classifications