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  3. BET bromodomain inhibitor 1

BET bromodomain inhibitor 1 

目录号: HY-131061
产品使用指南

BET bromodomain inhibitor 1 是一种具有口服活性的,选择性 BET 溴结构域抑制剂,对 BRD4 的 IC50 为 2.6 nM。BET bromodomain inhibitor 1 与 BRD2(2),BRD3(2),BRD4(1),BRD4(2) 和 BRDT(2) 高亲和力结合 (Kd 值分别为 1.3 nM、1.0 nM、3.0 nM、1.6 nM、2.1 nM)。BET bromodomain inhibitor 1 具有抗癌活性。

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BET bromodomain inhibitor 1 Chemical Structure

BET bromodomain inhibitor 1 Chemical Structure

CAS No. : 2411226-02-1

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Description

BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity[1].

IC50 & Target[1]

BRD4

2.6 nM (IC50)

BRD2(2)

1.3 nM (Kd)

BRD3(2)

1.0 nM (Kd)

BRD4(1)

3.0 nM (Kd)

BRD4(2)

1.6 nM (Kd)

BRDT(2)

2.1 nM (Kd)

In Vitro

BET bromodomain inhibitor 1 (compound 38; 31.25-125 nM; 24 hours) leads to more pronounced G1-phase cell cycle arrest[1].
BET bromodomain inhibitor 1 (31.25-500 nM; 6 or 24 hours) is highly effective in inducing dose-dependent inhibition on c-Myc expression and upregulation of p21 levels[1].
BET bromodomain inhibitor 1 (31.25-125 nM; 6 hours) robustly reduces the expressions of c-Myc, BCL-2, and CDK6[1].
BET bromodomain inhibitor 1 does not inhibit five cytochrome P450 enzymes (IC50>20 μM)[1].
BET bromodomain inhibitor 1 demonstrates an excellent selectivity for the BET bromodomain family over other bromodomains, with an ∼1500-fold selectivity for BRD4(1) over EP300 (IC50=3857 nM)[1].
BET bromodomain inhibitor 1 strongly inhibited the growth of acute myeloid leukemia cell line MV4-11, acute leukemia cell lines Kasumi-1 and RS-4-11, and multiple myeloma cancer cell line MM1.S cells with IC50 values of 2.4, 4.8, 17.6 and 15.1 nM, respectively[1].

Cell Cycle Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 31.25, 62.5, 125 nM
Incubation Time: 24 hours
Result: Led to more pronounced G1-phase cell cycle arrest.

Western Blot Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 31.25, 62.5, 125, 250, 500 nM
Incubation Time: 6 or 24 hours
Result: Induced dose-dependent inhibition on c-Myc expression and upregulation of p21 levels.

RT-PCR[1]

Cell Line: MV-4-11 cells
Concentration: 31.25, 62.5, 125 nM
Incubation Time: 6 hours
Result: Robustly reduced the expressions of c-Myc, BCL-2, and CDK6.
In Vivo

BET bromodomain inhibitor 1 (compound 38; 6.25, 12.5 mg/kg; PO; daily ; for 28 days) exhibits stronger antitumor activities and completely inhibits the growth of tumor with a tumor growth inhibition (TGI) of 99.7% at 12.5 mg/kg[1].
BET bromodomain inhibitor 1 (1 mg/kg; IV) has a T1/2 of 1.3 hours, a CL of 21.5 mL/min•kg, and a Vss of 1464 mL/kg for rats[1].
BET bromodomain inhibitor 1 (3 mg/kg; PO) has a T1/2 of 3.6 hours, a Cmax of 159 ng/mL and an AUC of 884 ng•h/mL for rats[1].
BET bromodomain inhibitor 1 (1 mg/kg; IV) has a T1/2 of 0.9 hours, a CL of 15.3 mL/min•kg, and a Vss of 782 mL/kg for mouse[1].
BET bromodomain inhibitor 1 (1.3 mg/kg; PO) has a T1/2 of 1.3 hours, a Cmax of 399 ng/mL and an AUC of 1710 ng•h/mL for mouse[1].

Animal Model: An MV4-11 mouse xenograft model[1]
Dosage: 6.25, 12.5 mg/kg
Administration: PO; daily ; for 28 days
Result: Exhibited stronger antitumor activities and completely inhibited the growth of tumor with a tumor growth inhibition (TGI) of 99.7% at 12.5 mg/kg.
Animal Model: Male SD rats[1]
Dosage: 1 mg/kg (Pharmacokinetic Analysis)
Administration: IV
Result: Had a T1/2 of 1.3 hours, a CL of 21.5 mL/min•kg, and a Vss of 1464 mL/kg.
Molecular Weight

459.47

Formula

C₂₂H₁₉F₂N₃O₄S

CAS No.

2411226-02-1

SMILES

O=C1C2=C(C)C=C(C3=CC(CS(=O)(CC)=O)=CN=C3OC4=CC=C(F)C=C4F)N2C=CN1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

BET bromodomain inhibitor 1BET bromodomain inhibitor1BET bromodomain inhibitor-1Epigenetic Reader Domainorallybromodomainandextra-terminalBETanti-canceracutemyeloidleukemiacellMV4-11Kasumi-1RS-4-11multiplemyelomaInhibitorinhibitorinhibit

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BET bromodomain inhibitor 1
目录号:
HY-131061
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