PTC-209
PTC-209 is a small-molecule inhibitor of BMI-1 with IC50 value of 0.5 μM [1].
PTC-209 is screened out by using gene expression modulation by small molecules (GEMS) technology. It can lower BMI-1 transcript levels. PTC-209 is demonstrated to inhibit not only the UTR-mediated expression but also endogenous BMI-1 expression in HCT116 cell line. For HEK293 and HT1080 cell lines, PTC-209 doesn’t show any inhibition of the growth, suggesting that PTC-209 has no cytotoxicity. And for tumor cells or stem cells, such as U937, HT1080 and human hematopoietic stem cells, PTC-209 can inhibit the proliferation of them. As BMI-1 plays its role through the PRC1 complex, PTC-209 reduces the ability of PRC1 selectively. It is also reported that PTC-209 suppresses the growth of colorectal tumor cells through irreversible growth inhibition of CICs [1].
References:
[1] Kreso A, van Galen P, Pedley NM, Lima-Fernandes E, Frelin C, Davis T, Cao L, Baiazitov R, Du W, Sydorenko N, Moon YC, Gibson L, Wang Y, Leung C, Iscove NN, Arrowsmith CH, Szentgyorgyi E, Gallinger S, Dick JE, O'Brien CA. Self-renewal as a therapeutic target in human colorectal cancer. Nat Med. 2014 Jan;20(1):29-36.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 495.19 |
| Cas No. | 315704-66-6 |
| Formula | C17H13Br2N5OS |
| Solubility | ≥24.75 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| Chemical Name | N-(2,6-dibromo-4-methoxyphenyl)-4-(2-methylimidazo[1,2-a]pyrimidin-3-yl)-1,3-thiazol-2-amine |
| SDF | Download SDF |
| Canonical SMILES | CC1=C(N2C=CC=NC2=N1)C3=CSC(=N3)NC4=C(C=C(C=C4Br)OC)Br |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Human colorectal HCT116 and human fibrosarcoma HT1080 tumor cells |
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Preparation method |
Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37°C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
37°C |
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Applications |
PTC-209 dose-dependently inhibits not only the UTR-mediated reporter expression but also endogenous BMI-1 expression in human colorectal HCT116 and human fibrosarcoma HT1080 tumor cells (IC50 = ~0.5 μM). PTC-209 (between 0.1 and 10 μM) also reduces BMI-1 protein levels in a dose-dependent manner with a concomitant reduction in cell growth. |
| Animal experiment [1]: | |
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Animal models |
Primary human colon cancer xenograft in nude mice |
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Dosage form |
Administered subcutaneously once a day at a dose of 60 mg per kg body weight |
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Applications |
For mice transplanted with cells from sample 01, 9 d following the initial drug administration, the tumor volume of the PTC-209–treated group is significantly reduced, continued treatment of animals with PTC-209 for an additional week did not affect the overall health of the mice, and tumors did not increase in size. Likewise, for mice given cells from sample 03, 9 d after PTC-209 initiation, the drug-treated tumors displays a significantly smaller tumor volume as compared to the control tumors. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: 1. Kreso A, van Galen P, Pedley NM et al. Self-renewal as a therapeutic target in human colorectal cancer. Nat Med. 2014 Jan;20(1):29-36. |
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| Description | PTC-209 is a small-molecule inhibitor of BMI-1 with IC50 value of 0.5 μM. | |||||
| Targets | BMI-1 | |||||
| IC50 | 0.5 μM | |||||
Quality Control & MSDS
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Chemical structure
