[CAS NO. 315704-66-6]  PTC-209

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PRODUCTS SPECIFICATIONS [315704-66-6]

Catalog
HY-15888
Brand
MCE
CAS
315704-66-6

DESCRIPTION [315704-66-6]

Overview

MDLMFCD02110649
Molecular Weight495.19
Molecular FormulaC17H13Br2N5OS
SMILESCC1=C(C2=CSC(NC3=C(Br)C=C(OC)C=C3Br)=N2)N4C=CC=NC4=N1

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


Summary

PTC-209 is a specific BMI-1 inhibitor with an IC 50 of 0.5 μM in HEK293T cell line. PTC-209 irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 shows potent anti-myeloma activity and impairs the tumor microenvironment [1] [2] .


IC50 & Target

IC50: 0.5 μM (BMI-1, in HT1080 tumor cells) [1]


In Vitro

PTC-209 (0.01-10 µM; 24-72 hours) induces a concentration- and time-dependent decrease in the cellular viability of all cell lines tested [2] .
PTC-209 (1-2.5 μM) inhibits STAT3 phosphorylation in A549 lung cancer cells and MDA-MB-231 breast cancer cells [2] .

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

Cell Viability Assay [2]

Cell Line: Lung (LNM35, A549 cells), breast (MDA-MB-231 and T47D cells), and colon (HT-29, HCT-116, and HCT8/S11 cells)
Concentration: 0.01-10 µM
Incubation Time: 24, 48, and 72 hour
Result: Induced a concentration- and time-dependent decrease in the cellular viability of all cell lines tested.

In Vivo

PTC-209 (60 mg/kg body weight; subcutaneously; once a day for 11 days) significantly reduces tumor volume [1] .

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

Animal Model: Nude mice (male, aged 8-10 weeks, HCT1116 cell-derived tumor) [1]
Dosage: 60 mg/kg body weight
Administration: Subcutaneously; once a day for 11 days
Result: Significantly reduced tumor volume

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 : ≥ 32 mg/mL ( 64.62 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0194 mL 10.0971 mL 20.1943 mL
5 mM 0.4039 mL 2.0194 mL 4.0389 mL
10 mM 0.2019 mL 1.0097 mL 2.0194 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: 2.5 mg/mL (5.05 mM); Suspended solution; Need ultrasonic

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