Benzamide, 2-(2-fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)-

Product Name: Benzamide, 2-(2-fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)-
CAS No.: 2682114-39-0
Chemical Name: Benzamide, 2-(2-fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)-
Synonyms: RBPJ inhibitor RIN1;RIN1 (RBPJ Inhibitor-1);RBPJ Inhibitor-1 (RIN1) ，S3376;RBPJ Inhibitor-1, 10 mM in DMSO;Benzamide, 2-(2-fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)-
CBNumber: CB610557921
Molecular Formula: C17H14FN3O2
Formula Weight: 311.31
MOL File: 2682114-39-0.mol

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Benzamide, 2-(2-fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)- Property

Boiling point:: 454.9±45.0 °C(Predicted)
Density: 1.30±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO: 62 mg/mL (199.16 mM);Ethanol: 62 mg/mL (199.16 mM)
pka: 15.45±0.50(Predicted)
form: Solid
color: Light yellow to light brown
Water Solubility: Water: Insoluble

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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Benzamide, 2-(2-fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)- Chemical Properties,Usage,Production

Uses

RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation[1].

Biological Activity

RBPJ Inhibitor-1 (RIN1) is a selective inhibitor against the transcription factor RBPJ. RIN1 blocks RBPJ-SHARP transcriptional repressor complex formation, inhibits RBPJ-mediated Notch intracellular domain (NICD) transcription activity (IC50/Emax = 180 nM/82% and 190 nM/88% using Notch2 ICD or Notch3 ICD, respectively), as well as NICD-independent transcription activity of RBPJ-VP16 (IC50 = 200 nM, Emax = 81%). RIN1 inhibits Notch-driven cancer proliferation (by ~70% post 4-day 10 μM RIN1 treatment; Jurkat) and promotes muscle differentiation (0.6 μM for 4 days; C2C12 myoblasts).

References

[1] Cecilia Hurtado, et al. Disruption of NOTCH signaling by a small molecule inhibitor of the transcription factor RBPJ. Sci Rep. 2019 Jul 25;9(1):10811. DOI:10.1038/s41598-019-46948-5

Benzamide, 2-(2-fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)- Preparation Products And Raw materials

Raw materials

Preparation Products

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2682114-39-0, Benzamide, 2-(2-fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)-Related Search:

Benzamide, 2-(2-fluorophenoxy)-4-(1-methyl-1H-pyrazol-5-yl)-

RBPJ inhibitor RIN1

RBPJ Inhibitor-1, 10 mM in DMSO

RIN1 (RBPJ Inhibitor-1)

RBPJ Inhibitor-1 (RIN1) ，S3376

2682114-39-0