ABBV-744 - CAS# 2138861-99-9


Catalog No. Size PriceQuantity
M16391-C Contact sales@xcessbio.com for quotation $100

Description

ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values range from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with drug-like properties enable the investigation of its antitumor efficacy and tolerability.

Product information

CAS Number: 2138861-99-9

Molecular Weight: 491.55

Formula: C28H30FN3O4

Chemical Name: N-ethyl-4-[2-(4-fluoro-2,6-dimethylphenoxy)-5-(2-hydroxypropan-2-yl)phenyl]-6-methyl-7-oxo-1H,6H,7H-pyrrolo[2,3-c]pyridine-2-carboxamide

Smiles: CCNC(=O)C1=CC2=C(N1)C(=O)N(C)C=C2C1=CC(=CC=C1OC1=C(C)C=C(F)C=C1C)C(C)(C)O

InChiKey: OEDSFMUSNZDJFD-UHFFFAOYSA-N

InChi: InChI=1S/C28H30FN3O4/c1-7-30-26(33)22-13-20-21(14-32(6)27(34)24(20)31-22)19-12-17(28(4,5)35)8-9-23(19)36-25-15(2)10-18(29)11-16(25)3/h8-14,31,35H,7H2,1-6H3,(H,30,33)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 37.14 mg/mL (75.56 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

ABBV-744 (90 nM; 0~24 h; LNCaP cells) downregulates the expression of KLK2 and MYC genes. ABBV-744 (90 nM; 0~72 h; LNCaP cells) induces cell cycle arrest in G1 followed by senescence.

In Vivo:

ABBV-744 (4.7 mg/kg; oral gavage; 28 days) causes a delay in tumor growth and displays equivalent or better antitumor activity compared with ABBV-075. ABBV-744 (30 mg/kg; 14 days) is able to produce significant antitumor activity. ABBV-744 (30 mg/kg) triggers a reduction in platelets of only 20 %.

Products are for research use only. Not for human use.

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