[CAS NO. 307543-71-1]  STF-083010

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PRODUCTS SPECIFICATIONS [307543-71-1]

Catalog
HY-15845
Brand
MCE
CAS
307543-71-1

DESCRIPTION [307543-71-1]

Overview

MDLMFCD02332975
Molecular Weight317.38
Molecular FormulaC15H11NO3S2
SMILESO=S(C1=CC=CS1)(/N=C/C2=C3C=CC=CC3=CC=C2O)=O

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


Summary

STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.


IC50 & Target

Ire1 [1]


In Vitro

STF-083010 shows cytostatic and cytotoxic activity in a dose- and time-dependent manner. Treatment with STF-083010 shows significant antimyeloma activity in model human multiple myeloma (MM) xenografts. RPMI 8226 human MM cells grown as tumor xenografts are treated in NSG mice. Intraperitoneal injection of STF-083010 alone (day 1, day 8) significantly inhibits the growth of these tumors [1] . STF-083010 is an IRE1α-specific inhibitor. Four pancreatic cancer cell lines (Panc0403, Panc1005, BxPc3, MiaPaCa2) are treated with different combination of Bortezomib (10 or 50 nM) and STF (10 or 50 μM). The normalized isobologram analysis demonstrates synergistic activity between 10 μM STF and either 10 or 50 nM bortezomib in all four cell lines. Moreover, a higher concentration of STF (50 μM) attains synergy after addition of bortezomib either at a concentration of 10 nM when tested against BxPc3 cells, at a concentration of 50 nM against Panc1005 cells, and at either 10 or 50 nM against Panc0403 cells [2] . STF-083010 (50 μM) suppresses the growth of p53-deficient human cancer cells [3] .

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


In Vivo

Treatment with STF-083010 reduces the viability of HCT116 p53 -/- cells by approximately 20% compared with that of HCT116 p53 -/- cells. Administration of STF-083010 to tumors induced by HCT116 p53 -/- cells significantly reduces tumor volume and weight by 75% and 73% at the endpoint, respectively [3] .

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
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 315.08 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1508 mL 15.7540 mL 31.5080 mL
5 mM 0.6302 mL 3.1508 mL 6.3016 mL
10 mM 0.3151 mL 1.5754 mL 3.1508 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: ≥ 3.25 mg/mL (10.24 mM); Clear solution

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


Synonyms

2-Thiophenesulfonamide, N-[(2-hydroxy-1-naphthalenyl)methylene]-
N-[(2-Hydroxy-1-naphthalenyl)methylene]-2-thiophenesulfonamide
STF 083010
IRE 1 Inhibitor I