ChemicalBook > CAS DataBase List > PTC-209 (PTC209

PTC-209 (PTC209

Product Name
PTC-209 (PTC209
CAS No.
315704-66-6
Chemical Name
PTC-209 (PTC209
Synonyms
PTC-209;CS-1315;PTC 209 NEW;PTC-209, >=98%;PTC-209 (PTC209;PTC-209 free base;BMI-1 Expression Inhibitor, PTC-209;N-(2,6-Dibromo-4-methoxyphenyl)-4-(2-methylimidazo[1,2-a]pyrimidin-3-yl)-2-thiazolamine;N-(2,6-dibroMo-4-Methoxyphenyl)-4-(2-MethyliMidazo[1,2-a]pyriMidin-3-yl)thiazol-2-aMine;2-THIAZOLAMINE, N-(2,6-DIBROMO-4-METHOXYPHENYL)-4-(2-METHYLIMIDAZO[1,2-A]PYRIMIDIN-3-YL)-
CBNumber
CB02682264
Molecular Formula
C17H13Br2N5OS
Formula Weight
495.19
MOL File
315704-66-6.mol
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PTC-209 (PTC209 Property

Density 
1.86±0.1 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
DMSO: soluble20mg/mL, clear
pka
3.77±0.30(Predicted)
form 
powder
color 
white to brown
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
InChI
InChI=1S/C17H13Br2N5OS/c1-9-15(24-5-3-4-20-16(24)21-9)13-8-26-17(22-13)23-14-11(18)6-10(25-2)7-12(14)19/h3-8H,1-2H3,(H,22,23)
InChIKey
XVOOCQSWCCRVDY-UHFFFAOYSA-N
SMILES
S1C=C(C2N3C(=NC=2C)N=CC=C3)N=C1NC1=C(Br)C=C(OC)C=C1Br
CAS DataBase Reference
315704-66-6
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Safety

Hazard Codes 
T
Risk Statements 
25
Safety Statements 
45
RIDADR 
UN 2811 6.1 / PGIII
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H301Toxic if swalloed

Precautionary statements

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML1143
Product name
PTC-209
Purity
≥98% (HPLC)
Packaging
5mg
Price
$121
Updated
2025/07/31
Sigma-Aldrich
Product number
SML1143
Product name
PTC-209
Purity
≥98% (HPLC)
Packaging
25mg
Price
$489
Updated
2025/07/31
Sigma-Aldrich
Product number
5.30154
Product name
BMI-1 Expression Inhibitor, PTC-209 - CAS 315704-66-6 - Calbiochem
Purity
A cell-permeable compound that downregulates cellular BMI-1 levels by inhibiting BMI-1 transcription.
Packaging
10MG
Price
$231
Updated
2025/07/31
Cayman Chemical
Product number
16277
Product name
PTC-209
Purity
≥95%
Packaging
1mg
Price
$29
Updated
2024/03/01
Cayman Chemical
Product number
16277
Product name
PTC-209
Purity
≥95%
Packaging
5mg
Price
$109
Updated
2024/03/01
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PTC-209 (PTC209 Chemical Properties,Usage,Production

Description

PTC-209 (315704-66-6) is an inhibitor of BMI-1 (IC50 = 500 nM), part of the polycomb repressive complex 1 (PCR1).1? It inhibited endogenous BMI-1 expression in human colorectal HCT116 and human fibrosarcoma HT1080 tumor cells resulting in reduced tumor volume as well as reduced cancer initiating cell (CIC) number.?? PTC-209 displayed potent in vivo antitumor effects in several cancer models including breast2, head and neck3, glioblastoma4, prostate5, colon5, and rhabdomyosarcoma6. It also promoted chemically-induced direct cardiac reprogramming of cardiac fibroblasts into cardiac myocytes.7,8

Uses

Polycomb complex protein BMI-1 is a polycomb ring finger oncogene that regulates the p16 and p19 cell cycle inhibitor genes. It is necessary for efficient self-renewing cell divisions of stem cells in several tissues and can be over-expressed in tumors. PTC-209 is a BMI-1 inhibitor (IC50 = ~ 0.5 μM) that irreversibly impairs colorectal cancer-initiating cell (CIC) growth. It reduces tumor growth in CIC xenograft assays and abrogates colorectal cancer cell self-renewal in vivo, reducing their tumorigenic potential.[Cayman Chemical]

Uses

PTC 209 is a compound involved in thedown-reglation of NOTCH signaling and aids in suppressing acute leukemia cells.

Uses

PTC-209 has been used as a B lymphoma Mo-MLV insertion region 1 homolog (BMI1) inhibitor to study its effects on:

  • the cell viability of canine osteosarcoma (OSA) cell lines
  • lipidated microtubule-associated protein 1 light chain 3 (LC3B-II) and Sequestosome 1 (SQSTM1) protein levels in ovarian cancer (OvCa) cells
  • cardiac reprogramming efficiency in mouse embryonic fibroblasts (MEF)

Biochem/physiol Actions

PTC-209 inhibits the expression of the oncogene BMI-1 (B lymphoma Mo-MLV insertion region 1 homolog), which encodes a polycomb group RING finger protein involved in cell cycle. PTC-209 lowers the self-renewal properties of colorectal cancer-initiating cells (CICs) The compound inhibits tumor growth, and reduces the levels of CICs present in colon cancer tumor xenografts in mice.

in vivo

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

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

storage

Store at -20°C

References

[1] ANTONIJA KRESO. Self-renewal as a therapeutic target in human colorectal cancer[J]. Nature Medicine, 2013, 20 1: 29-36. DOI:10.1038/nm.3418
[2] MATHANGI SRINIVASAN. Downregulation of Bmi1 in breast cancer stem cells suppresses tumor growth and proliferation.[J]. Oncotarget, 2017: 38731-38742. DOI:10.18632/oncotarget.16317
[3] QIONG WANG. Pharmacological inhibition of Bmi1 by PTC-209 impaired tumor growth in head neck squamous cell carcinoma.[J]. Cancer Cell International, 2017: 107. DOI:10.1186/s12935-017-0481-z
[4] YU KONG. Targeting of BMI-1 with PTC-209 inhibits glioblastoma development.[J]. Cell Cycle, 2018, 17 10: 1199-1211. DOI:10.1080/15384101.2018.1469872
[5] R. ELANGO. Concurrent targeting of BMI1 and CDK4/6 abrogates tumor growth in vitro and in vivo[J]. Scientific Reports, 2019. DOI:10.1038/s41598-019-50140-0
[6] CARA E SHIELDS. Epigenetic regulator BMI1 promotes alveolar rhabdomyosarcoma proliferation and constitutes a novel therapeutic target.[J]. Molecular Oncology, 2021, 15 8: 2156-2171. DOI:10.1002/1878-0261.12914
[7] YIJING GUO. Chemical suppression of specific C-C chemokine signaling pathways enhances cardiac reprogramming.[J]. The Journal of Biological Chemistry, 2019, 294 23: 9134-9146. DOI:10.1074/jbc.ra118.006000
[8] GIANLUCA TESTA. Bmi1 inhibitor PTC-209 promotes Chemically-induced Direct Cardiac Reprogramming of cardiac fibroblasts into cardiomyocytes.[J]. Scientific Reports, 2020: 7129. DOI:10.1038/s41598-020-63992-8

PTC-209 (PTC209 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from PTC-209 (PTC209 manufacturers

Career Henan Chemical Co
Product
PTC-209 (PTC209 315704-66-6
Price
US $9.80/KG
Min. Order
1KG
Purity
≥98%
Supply Ability
20 tons
Release date
2020-01-09

315704-66-6, PTC-209 (PTC209Related Search:


  • PTC-209 (PTC209
  • PTC-209
  • N-(2,6-dibroMo-4-Methoxyphenyl)-4-(2-MethyliMidazo[1,2-a]pyriMidin-3-yl)thiazol-2-aMine
  • N-(2,6-Dibromo-4-methoxyphenyl)-4-(2-methylimidazo[1,2-a]pyrimidin-3-yl)-2-thiazolamine
  • N-(2,6-Dibromo-4-methoxyphenyl)-4-(2-methylimidazo[1,2-a]pyrimidin-3-yl)-2-thiazolamine PTC-209
  • PTC-209, >=98%
  • 2-THIAZOLAMINE, N-(2,6-DIBROMO-4-METHOXYPHENYL)-4-(2-METHYLIMIDAZO[1,2-A]PYRIMIDIN-3-YL)-
  • PTC-209 free base
  • PTC 209 NEW
  • CS-1315
  • BMI-1 Expression Inhibitor, PTC-209
  • 315704-66-6
  • C17H13Br2N5OS
  • Inhibitors