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;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)-;N-(2,6-Dibromo-4-methoxyphenyl)-4-(2-methylimidazo[1,2-a]pyrimidin-3-yl)-2-thiazolamine PTC-209
- CBNumber:
- CB02682264
- Molecular Formula:
- C17H13Br2N5OS
- Molecular Weight:
- 495.19
- MDL Number:
- MFCD02110649
- MOL File:
- 315704-66-6.mol
- MSDS File:
- SDS
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. |
CAS DataBase Reference | 315704-66-6 |
PTC-209 (PTC209 price More Price(27)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | SML1143 | PTC-209 ≥98% (HPLC) | 315704-66-6 | 5mg | $118 | 2024-03-01 | Buy |
Sigma-Aldrich | SML1143 | PTC-209 ≥98% (HPLC) | 315704-66-6 | 25mg | $476 | 2024-03-01 | Buy |
Sigma-Aldrich | 5.30154 | BMI-1 Expression Inhibitor, PTC-209 - CAS 315704-66-6 - Calbiochem A cell-permeable compound that downregulates cellular BMI-1 levels by inhibiting BMI-1 transcription. | 315704-66-6 | 10MG | $265 | 2024-03-01 | Buy |
Cayman Chemical | 16277 | PTC-209 ≥95% | 315704-66-6 | 1mg | $29 | 2024-03-01 | Buy |
Cayman Chemical | 16277 | PTC-209 ≥95% | 315704-66-6 | 5mg | $109 | 2024-03-01 | Buy |
PTC-209 (PTC209 Chemical Properties,Uses,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
PTC 209 is a compound involved in thedown-reglation of NOTCH signaling and aids in suppressing acute leukemia cells.
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 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.
storage
Store at -20°C
References
Kreso et al. (2013), Self-renewal as a therapeutic target in human colorectal cancer; Nat. Med. 20 29 Srinivasan et al. (2017), Downregulation of Bmi1 in breast cancer stem cells suppresses tumor growth and proliferation; Oncotarget. 8 38731 Wang et al. (2017), Pharmacological inhibition of Bmi1 by PTC-209 impaired tumor growth in head neck squamous cell carcinoma; Cancer Cell Int. 17 107 Kong et al. (2018), Targeting of BMI-1 with PTC-209 inhibits glioblastoma development; Cell Cycle 17 1199 Elango et al. (2019), Concurrent targeting of BMI1 and CDK4/6 abrogates tumor growth in vitro and in vivo; Sci. Rep. 9 13696 Shields et al. (2021), Epigenetic regulator BMI1 promotes alveolar rhabdomyosarcoma proliferation and constitutes a novel therapeutic target; Mol. Oncol. 1002/1878-0261.12914 Guo et al. (2019), Chemical suppression of specific C-C chemokine signaling pathways enhances cardiac reprogramming; J. Biol. Chem. 294 9134 Testa et al.. (2020),Bmi1 inhibitor PTC-209 promotes Chemically-induced Direct Cardiac Reprogramming of cardiac fibroblasts into cardiomyocytes; Sci. Rep. 10 7129
PTC-209 (PTC209 Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
SHANGHAI T&W PHARMACEUTICAL CO., LTD. | +86-021-61551413 +8618813727289 | contact@trustwe.com | China | 5738 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
Golden Pharma Co., Limited | +undefined18958062155 | sales@zjgoldpharm.com | China | 5905 | 58 |
ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
GIHI CHEMICALS CO.,LIMITED | +8618058761490 | info@gihichemicals.com | China | 49999 | 58 |
View Lastest Price from PTC-209 (PTC209 manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
---|---|---|---|---|---|---|---|---|
2020-01-10 | PTC-209 (PTC209
315704-66-6
|
US $9.80 / KG | 1KG | ≥98% | 20 tons | Career Henan Chemical Co |
- PTC-209 (PTC209
315704-66-6
- US $9.80 / KG
- ≥98%
- Career Henan Chemical Co