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Cat. No.: HY-151894

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I-BET432

I-BET432 is a BET inhibitor. I-BET432 inhibits BRD4 N-terminal bromodomain (BD1) and the C-terminal bromodomain (BD2) with pIC₅₀ values of 7.5 and 7.2, respectively. I-BET432 can be used as an oral candidate quality molecule for the research of multiple oncology and inflammatory diseases.

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CAS No.: 3035187-74-4
Formule: C₁₈H₂₁N₃O₃
Masse moléculaire:327.38

Stockage:

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

Data Sheet (275 KB)

I-BET432 Chemical Structure

CAS No.: 3035187-74-4

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Use of MCE Products

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

Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
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Activité biologique

Description

Voir tous les produits spécifiques à Isoform Epigenetic Reader Domain :

In Vitro

I-BET432 inhibits BRD4 BD1 and BD2 with pIC₅₀ values of 7.5 and 7.2, respectively^[1].
I-BET432 inhibits human whole blood MCP-1 with an pIC₅₀ value of 7.4^[1].
I-BET432 inhibits hERG with an pIC₅₀ value ＜4.3^[1].

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

In Vivo

I-BET432 shows great oral bioavailability in rats and dogs^[1].
1.19 Pharmacokinetic Properties of I-BET432 in Rats and Dogs^[1].

	Rats PO/IV 3/1 mg/kg	Dogs PO/IV 1.5/0.5 mg/kg
CL_b (mL/min/kg)	26	28
CL_b,u (mL/min/kg)	38	20
V_ss (L/kg)	1.3	2.7
V_ss,u (L/kg)	1.9	5.7
t_1/2 (h)	0.74	1.4
Fpo (%)	67	79
fu_b	0.68	0.47

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

Chemical Information

CAS No. 3035187-74-4
Masse moléculaire 327.38
Formule C₁₈H₂₁N₃O₃
SMILES

O=C1N(C)C=C(C2=CN(C)N=C2)C3=CC([C@@H](O)CO)=CC=C3[C@H]1C
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 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)
Instruction de manipulation (2659 KB)

Références

[1]. Humphreys PG, et al. Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I-BET432. J Med Chem. 2022 Nov 24;65(22):15174-15207. [Content Brief]

Calculators

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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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