[CAS NO. 1436383-95-7]  BF738735

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PRODUCTS SPECIFICATIONS [1436383-95-7]

Catalog
HY-U00426
Brand
MCE
CAS
1436383-95-7

DESCRIPTION [1436383-95-7]

Overview

MDL-
Molecular Weight426.46
Molecular FormulaC21H19FN4O3S
SMILESOC1=CC=C(C2=C(C)N=C3C(NCC4=CC=CC(S(=O)(C)=O)=C4)=NC=CN32)C=C1F

For research use only. We do not sell to patients.

1 Publications Citing Use of MCE


Summary

BF738735 is a phosphatidylinositol 4-kinase III beta ( PI4KIIIβ ) inhibitor with an IC 50 of 5.7 nM.


IC50 & Target

PI4KIIIβ

5.7 nM (IC 50 )

PI4KIIIα

1.7 μM (IC 50 )


In Vitro

BF738735 (Compound 1) strongly inhibits PI4KIIIβ activity in vitro, with an IC 50 of 5.7 nM. BF738735 also impairs PI4KIIIα, but only at an ~300-fold-higher concentration (IC 50 of 1.7 μM). In addition, the activity of BF738735 is analyzed on a set of 150 cellular kinases, including 13 lipid kinases at a concentration of 10 μM. For all kinases, the inhibition is less than 10%, indicating that BF738735 specifically inhibits PI4KIIIβ in vitro. BF738735 exhibits a broad spectrum of antiviral activity, as it inhibits all tested species of enteroviruses and rhinoviruses, with 50% effective concentrations ranging between 4 and 71 nM. BF738735 potently inhibits all viruses tested, with EC 50 s ranging between 4 and 71 nM. The cytotoxicity of BF738735, determined in parallel with the EC 50 and using the same culture conditions for 3 to 4 days, is low, with CC 50 values ranging from 11 to 65 μM, resulting in high selectivity indices. Low concentrations of BF738735 reduce the amount of luciferase to GuaHCl-treated levels, suggesting that the BF738735 blocks viral RNA replication. The EC 50 of BF738735 in this assay is 77 nM, which is comparable to the inhibition observed in the multicycle assay for coxsackievirus serotype B3 (CVB3) [1] .

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


In Vivo

BF738735 is well tolerated by specimens with good plasma levels of the antiviral in circulation and a complete inhibition with 25 mg/kg and some inhibition with 5 mg/kg dose is observed [2] .

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


Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL ( 293.11 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3449 mL 11.7244 mL 23.4489 mL
5 mM 0.4690 mL 2.3449 mL 4.6898 mL
10 mM 0.2345 mL 1.1724 mL 2.3449 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution

* All of the co-solvents are available by MCE.