PTC-209

Catalog No.S7372

For research use only.

PTC-209 is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM in HEK293T cell line, and results in irreversible reduction of cancer-initiating cells (CICs).

PTC-209 Chemical Structure

CAS No. 315704-66-6

Selleck's PTC-209 has been cited by 17 publications

Purity & Quality Control

Choose Selective BMI-1 Inhibitors

Biological Activity

Description PTC-209 is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM in HEK293T cell line, and results in irreversible reduction of cancer-initiating cells (CICs).
Features BMI-1-selective inhibitor targeting self-renewal of cancer cells.
Targets
BMI-1 [1]
(HEK293T cells)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 MXnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M4[xOFczKGi{cx?= M4joO2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTBiPTCwMlAxODZ3IN88UU4> NWLBRZl7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C0Nlk6PTNpPkOwOFI6QTV|PD;hQi=>
HCT8 MUXBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NVj0cWRGPzJiaILz M17QfGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUPEBk\WyuczDh[pRmeiB5MjDodpMh[nliU2LCJIF{e2G7LDDJR|UxKD1iMD61PUDPxE1w MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODR{OUm1N{c,OzB2Mkm5OVM9N2F-
HT-29 M4fpSmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MkLOO|IhcHK| MnLWRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczDh[pRmeiB5MjDodpMh[nliU2LCJIF{e2G7LDDJR|UxKD1iMD62NUDPxE1w MmPaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB2Mkm5OVMoRjNyNEK5PVU{RC:jPh?=
HCT116 NYD5ZXlQTnWwY4Tpc44h[XO|YYm= NF;IR5g5KGi{cx?= NGnmNXNKdmirYnn0bY9vKG:oIFLtbVEheHKxdHXpckBmgHC{ZYPzbY9vKGmwIHj1cYFvKEiFVEGxOkBk\WyuczDh[pRmeiB6IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYOsJGlEPTBiPTCwMlch|ryPLh?= MmewQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB2Mkm5OVMoRjNyNEK5PVU{RC:jPh?=
HCT116 NHfy[I9HfW6ldHnvckBie3OjeR?= NWfRSWh6OC5zIITvJFAvPCC3TR?= Mn\KO{Bl[Xm| MVLJcohq[mm2aX;uJI9nKGOxbH;ufUBnd3KvYYTpc44hcW5iaIXtZY4hUEOWMUG2JINmdGy|IHH0JFAvOSC2bzCwMlQhfU1iYX\0[ZIhPyCmYYnzJIJ6KGO{eYP0ZYwhfmmxbHX0JJN1[WmwaX7nJIJie2WmIHHzd4F6 M2\ISlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNEK5PVU{Lz5|MESyPVk2OzxxYU6=
HCT116 NWHx[o03SW62aYT1cY9zKGG|c3H5 MV2xNEBu\y:tZz;kZZk> NX\qcXF3OThiZHH5dy=> NHvCSIVCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMhgGWwb3fyZYZ1\WRiaX6gcpVl\SCvb4Xz[UBie3Onc4Pl[EBieyC2dX3vdkBoem:5dHigbY5pcWKrdHnvckBifCBzMDDt[{9s\y:mYYmsJIlxKG[xcjCxPEBl[Xm| NEC1R4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MESyPVk2Oyd-M{C0Nlk6PTN:L3G+
HCT116 M{W5SWFvfGm2dX3vdkBie3OjeR?= NE\nOXgyOCCvZz;r[{9l[Xl? M3foTVE5KGSjeYO= NWnOVZZ7SW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KHinbn;ndoFnfGWmIHnuJI52\GVibX;1d4Uh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJGtqPjdiZYjwdoV{e2mxbjDpckB1fW2xcjDheEAyOCCvZz;r[{9l[XluIHnwJIZweiBzODDkZZl{KGK7IFnIR{BidmGueYPpdy=> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODR{OUm1N{c,OzB2Mkm5OVM9N2F-
HCT116 Mof6SpVv[3Srb36gZZN{[Xl? M2\4b|ExKG2pL3vnM4RigQ>? MonuNVgh\GG7cx?= MV3E[YNz\WG|ZTDpckBDdWlzIHX4dJJme3Orb36gbY4hfHWvb4LzJI9nKG63ZHWgcY92e2VieHXuc4dz[W[2ZXSge4l1cCCqdX3hckBJS1RzMU[gZ4VtdHNiYYSgNVAhdWdxa3ev[IF6NCCrcDDmc5IhOThiZHH5d{BjgSCLSFOgZY5idHm|aYO= M1zVOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNEK5PVU{Lz5|MESyPVk2OzxxYU6=
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]

Protocol (from reference)

Kinase Assay:[1]
  • 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.

Cell Research:[1]
  • Cell lines: Human lymphoma U937 and HT1080 tumor cells, primary human peripheral blood mononuclear cells and human hematopoietic stem cells.
  • Concentrations: ~10 μM
  • Incubation Time: 4 days
  • Method: To determine whether pretreatment with the inhibitor affects tumor cell growth, cells are plated with the inhibitor for 4 d in vitro and plated in limiting doses in vitro without adding further inhibitor. Trypan blue exclusion is used to count viable cells. The in vitro sphere-initiating cell frequency is calculated after inhibitor treatment by evaluating the number of wells containing spheres. For the experiments where LDAs are set up following recovery of PTC-209 treated cells, 6-well plates were seeded with 1E6 cells per well and incubated overnight. Cells are subsequently treated for 4 d in triplicate with either DMSO vehicle or PTC-209 (0.01, 0.1, 1 and 10 μM). Drug treatments are washed off and 4 mL fresh suspension medium added to all wells. To assess cell viability following the 4 d treatment window, cells are trypsinized and counted at 0, 24, 72 and 120 h after removal of the drug. Long-lasting effects of the drug treatment on sphere-forming ability are assessed by plating LDAs (50,000, 10,000, 1,000,100, 10 and 1 cell per well) using the cells obtained 120 h after the 4-d drug treatment.
Animal Research:[1]
  • Animal Models: Primary human colon cancer xenograft, human colon cancer cell lines LIM1215 and HCT116 xenografts in nude mice.
  • Dosages: ~60 mg/kg/day
  • Administration: s.c.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 495.19
Formula

C17H13Br2N5OS

CAS No. 315704-66-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(N2C=CC=NC2=N1)C3=CSC(=N3)NC4=C(C=C(C=C4Br)OC)Br

In vivo Formulation Calculator (Clear solution)

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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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Tech Support

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