PTC-209 HBr( PTC-209 | PTC 209 | PTC209 Hydrobromide )

Catalog No. M17199 CAS No. 1217022-63-3

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HNMR

HPLC

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Product Name

PTC-209 HBr
Note

Research use only, not for human use.
Brief Description

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).
Description

PTC-209 Hydrobromide is a novel potent BMI1-inhibitor, modulating the RE1.
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.PTC-209 (1-2.5 μM) inhibits STAT3 phosphorylation in A549 lung cancer cells and MDA-MB-231 breast cancer cells. Cell Viability Assay 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. Animal Model:Nude mice (male, aged 8-10 weeks, HCT1116 cell-derived tumor)Dosage:60 mg/kg body weight Administration:Subcutaneously; once a day for 11 days Result:Significantly reduced tumor volume.
Synonyms

PTC-209 | PTC 209 | PTC209 Hydrobromide
Pathway

Membrane Transporter/Ion Channel
Target

NADPH
Recptor

BMI-1
Research Area

Cancer
Indication

——

CAS Number

1217022-63-3
Formula Weight

576.1
Molecular Formula

C17H13Br2N5OS·HBr
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 100 mg/mL (173.58 mM)
SMILES

Br.COC1=CC(Br)=C(NC2=NC(=CS2)C2=C(C)N=C3N=CC=CN23)C(Br)=C1
Chemical Name

N-(2,6-Dibromo-4-methoxyphenyl)-4-(2-methylimidazo[1,2-a]pyrimidin-3-yl)-2-thiazolamine hydrobromide

1. Kreso A, et al. Nat Med. 2014, 20(1), 29-36.

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