BI-D1870 , 98% , 501437-28-1

CAS NO.：501437-28-1

Empirical Formula: C19H23F2N5O2

Molecular Weight: 391.42

MDL number: MFCD11223662

PRODUCT Properties

• Boiling point: 579.3±60.0 °C(Predicted)
• Density: 1.297
• storage temp.: -20°C
• solubility: Soluble in DMSO (up to 15 mg/ml)
• form: Off-white solid.
• pka: 7.68±0.36(Predicted)
• color: Off-white
• Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.

Description and Uses

BI-D1870 (501437-28-1) is an inhibitor of p90 ribosomal S6 kinase (RSK; IC50’s = RSK1, 31 nM; RSK2, 24 nM; RSK3, 18 nM; RSK4, 15 nM) with selectivity over other AGC kinases.1?It protected mice from experimental autoimmune encephalomyelitis suggesting a new strategy to treat multiple sclerosis.2?BI-D1870 has also been found to alter mTORC1 signaling in an RSK-independent manner.3?BI-D1870 induced apoptosis in oral squamous cell carcinoma cells4, suppressed growth and induced apoptosis in pediatric medulloblastoma cell lines as well as sensitizing these lines to Sonic hedgehog agents5, and blocked cell proliferation and protein synthesis in dual BRAF and MEK inhibitor-resistant melanoma6.

The 90 kDa ribosomal S6 kinases (RSKs) are a group of serine/threonine kinases involved in diverse cellular processes, including growth, survival, and motility. BI-D1870 is a cell permeable, ATP-competitive inhibitor of the four vertebrate isoforms of RSK, RSK1-4 (IC50s = 31, 24, 18, and 15 nM, respectively). At 100 nM, it also significantly inhibits polo-like kinase 1, Aurora B, maternal embryonic leucine zipper kinase, and mammalian STE20-like kinase 2. BI-D1870 acts at the N-terminal kinase domain, but not the C-terminal domain, of RSK.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H315-H319-H227
• Precautionary statements: P501-P210-P264-P280-P302+P352-P370+P378-P337+P313-P305+P351+P338-P362+P364-P332+P313-P403+P235
• HS Code: 2933599590