Home Cell Cycle BMI-1 inhibitor PTC-209 HBr

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PTC-209 HBr BMI-1 inhibitor

Cat.No.S7539

PTC-209 HBr is the hydrobromide salt of PTC-209, which is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM, and results in irreversible reduction of cancer-initiating cells (CICs).
PTC-209 HBr BMI-1 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 576.10

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S753901 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.02%
99.02

Chemical Information, Storage & Stability

Molecular Weight 576.10 Formula

C17H13Br2N5OS.HBr

 Storage (From the date of receipt)
CAS No. 1217022-63-3 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=C(N2C=CC=NC2=N1)C3=CSC(=N3)NC4=C(C=C(C=C4Br)OC)Br.Br

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (173.58 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Features
BMI-1-selective inhibitor, targeting the BMI-1 self-renewal machinery.
Targets/IC50/Ki
BMI-1 [1]
0.5 μM
In vitro
PTC-209 inhibits both the UTR-mediated reporter expression and endogenous BMI-1 expression in human colorectal HCT116 and human fibrosarcoma HT1080 tumor cells. PTC-209 decreases colorectal tumor cell growth in a BMI-1-dependent way. In addition, PTC-209 impairs colorectal cancer-initiating cells (CICs) through irreversible growth inhibition. [1]
Kinase Assay
Untranslated region-mediated luciferase reporter expression
HEK293 cells are transfected with a GEMS reporter vector that contains the luciferase open-reading frame flanked by and under post-transcriptional control of the BMI-1 5′ and 3′ UTRs. The resulting stable cells (F8) are treated with PTC-209 or vehicle control overnight, and then luciferase reporter activity is determined using Bright-Glo assays. The assays are run in triplicate for each point, and the percentage of inhibition was calculated against vehicle control.
In vivo
PTC-209 (60 mg/kg/day, s.c.) effectively inhibits BMI-1 production in tumor tissue, and halts growth of preestablished tumors in mice bearing primary human colon cancer xenograft, human colon cancer cell lines LIM1215 or HCT116 xenografts. PTC-209 also reduces the frequency of functional colorectal CICs in vivo. [1]
References

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