Senexin B, CDK8/19 inhibitor (TBI4863)

Description

Product Details

Formal Name: 4-[2-[6-(4-Methylpiperazine-1-carbonyl)naphthalen-2-yl]ethylamino]quinazoline-6-carbonitrile

Alternate Names: BCD-115; SenB

Molecular Formula: C₂₇H₂₆N₆O

Formula Weight: 450.6

CAS Number: 1449228-40-3

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (> 25 mg/ml).

Storage: -20°C

Stability: ≥ 2 years

Applications

CDK8/19 inhibitor

Functions

Potent inhibitor of cyclin-dependent kinases 8 and 19. It suppressed tumor growth and augmented the effects of fulvestrant in ER-positive breast cancer xenografts. KD₅₀s: CDK8 = 59 nM, CDK19 = 23 nM. Also showed synergistic effects with lapatinib and trastuzumab in a panel of HER2+ breast cancer cell lines. Senexin B and ALK5 inhibitor SB431542 afforded generation of pancreatic islet cells from pluripotent stem cells without any mutagenic effects. Combination treatment of Senexin B and Imatinib intensified apoptotic cell death in chronic myelogenous leukemia cells and prevented quiescence-mediated escape from apoptosis.

Application Procedures

First dissolved in DMSO (> 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Additional information

Datasheet:

TBI4863_Senexin B_datasheet

MSDS:

TBI4863_Senexin B_MSDS

Research use only.