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  2. Cell Cycle/DNA Damage Cytoskeleton
  3. Mps1
  4. TC-Mps1-12

TC-Mps1-12 是一種高效、選擇性的 Mps1 抑制劑，其 IC50 值為 6.4 nM。

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TC-Mps1-12 Chemical Structure

TC-Mps1-12 Chemical Structure

CAS No. : 1206170-62-8

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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

TC-Mps1-12 is a potent and selective monopolar spindle 1 (Mps1) inhibitor, with an IC50 of 6.4 nM[1].

IC50 & Target

IC50: 6.4 nM (Mps1)[1]
細胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.84 μM
Compound: 12
Antiproliferative activity against human A549 cells after 72 hrs by WST8 assay
Antiproliferative activity against human A549 cells after 72 hrs by WST8 assay
[PMID: 24900510]
A549 IC50
840 nM
Compound: 14; TC Mps1 12
Antiproliferative activity against human A549 cells by MTT assay
Antiproliferative activity against human A549 cells by MTT assay
[PMID: 31121430]
HCT-116 IC50
0.56 μM
Compound: 6
Inhibition of Myc-tagged wild type MPS1 autophosphorylation in human HCT116 cells after 2 hrs in presence of proteosome inhibitor MG132
Inhibition of Myc-tagged wild type MPS1 autophosphorylation in human HCT116 cells after 2 hrs in presence of proteosome inhibitor MG132
[PMID: 24256217]
HCT-116 GI50
1.6 μM
Compound: 6
Growth inhibition in human HCT116 cells after 72 hrs by MTT assay
Growth inhibition in human HCT116 cells after 72 hrs by MTT assay
[PMID: 24256217]
RERF-LC-AI IC50
131 nM
Compound: 12
Inhibition of FLAG-tagged Mps1 autophosphorylation in human RERF-LC-AI cells expressing Tet-suppressible promotor after 3 hrs by immunoblotting
Inhibition of FLAG-tagged Mps1 autophosphorylation in human RERF-LC-AI cells expressing Tet-suppressible promotor after 3 hrs by immunoblotting
[PMID: 24900510]
Sf9 IC50
0.011 μM
Compound: 6
Inhibition of N-terminal 6XHis-tagged/GST-tagged full length human MPS1 expressed in recombinant baculovirus infected sf9 insect cells using 5FAM-DHTGFLTEYVATRCONH2 as substrate after 60 to 90 mins by fluorescence assay
Inhibition of N-terminal 6XHis-tagged/GST-tagged full length human MPS1 expressed in recombinant baculovirus infected sf9 insect cells using 5FAM-DHTGFLTEYVATRCONH2 as substrate after 60 to 90 mins by fluorescence assay
[PMID: 24256217]
體外研究
(In Vitro)

TC-Mps1-12 inhibits the growth of pMps1 cell lines with IC50 values of 131 nM in autophosphorylation assay[1].
TC-Mps1-12 (72 hours) inhibits the growth of cells in a dose-dependent manner and with an IC50 values of 0.84 μM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: 549 cells
Concentration:
Incubation Time: 72 hours
Result: Inhibited the growth of cells in a dose-dependent manner and with an IC50 values of 0.84 μM.
體內(nèi)研究
(In Vivo)

TC-Mps1-12 (25-100 mg/kg; p.o.; daily; for 19 days) inhibits the growth of A549 cells in a dose-dependent manner in vivo. At a dose of 100 mg/kg, TC-Mps1-12 exhibits 47% tumor growth inhibition without body weight loss[1].
TC-Mps1-12 shows good PK properties with a Cmax of 3542 ng/mL and AUC of 6604 ng h/mL at an oral dose of 25 mg/kg[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: A549 mouse xenograft model[1]
Dosage: 25 mg/kg, 50 mg/kg, 100 mg/kg
Administration: Oral administration; once daily; for 19 days
Result: Inhibited the growth of A549 cells in a dose-dependent manner.
Animal Model: A549 mouse xenograft model (pharmacokinetic )[1]
Dosage: 25 mg/kg
Administration: Oral administration
Result: Cmax = 3542 ng/mL, AUC = 6604 ng h/mL
分子量

324.38

Formula

C17H20N6O
CAS 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
純度 & 產(chǎn)品資料
參考文獻

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