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Referencia número: 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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No. CAS: 2379416-48-3
Fòrmula: C₂₇H₂₃F₄N₅O₄
Peso molecular:557.50

Almacenamiento:

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

Data Sheet (280 KB)

B026 Chemical Structure

No. CAS: 2379416-48-3

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Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

p300

8.1 nM (IC₅₀)

CBP

9.5 nM (IC₅₀)

Ver todos los productos específicos de isoformas Histone Acetyltransferase :

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

No. CAS 2379416-48-3
Peso molecular 557.50
Fòrmula 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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (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)
Instrucciones de manejo (2659 KB)

Referencias

[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

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)

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.

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MOQ

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100 mg

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureza y Documentación
Referencias

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B026

Ver todos los productos específicos de isoformas Histone Acetyltransferase

Actividad biológica

Chemical Information

Pureza y Documentación

Referencias

Calculators

Help & FAQs

B026 Related Classifications

HY-147261 Related Classifications