CGP-57380

  Cat. No.:  DC7381   Featured
Chemical Structure
522629-08-9
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Field of application
CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 (IC50 = 2.2 μM) with no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.
Cas No.: 522629-08-9
Chemical Name: N3-(4-Fluorophenyl)-1h-pyrazolo[3,4-d]pyrimidine-3,4-diamine
Synonyms: CGP 57380;3-N-(4-fluorophenyl)-2H-pyrazolo[3,4-d]pyrimidine-3,4-diamine;CGP-57380;CGP57380 N3-(4-fluorophenyl)-1h-pyrazolo[3,4-d]pyrimidine-3,4-diamine;N3-(4-fluorophenyl)-1h-pyrazolo[3,4-d]pyrimidine-3,4-diamine;MNK1 Inhibitor;CGP57380;C11H9FN6;4-Amino-5-(4-fluoroanilino)-pyrazolo[3,4-d]pyrimidine;GTPL6010;HMS3653G22;HMS3269P13;HMS3677D16;HMS3263L14;HMS3229K20;HMS3648M14;HMS3413D16;Tox21_501256;BDBM50130693;2314AH;NSC741567;s7421;IN1236;BDBM50
SMILES: FC1C([H])=C([H])C(=C([H])C=1[H])N([H])C1=C2C(N([H])[H])=NC([H])=NC2=NN1[H]
Formula: C11H9FN6
M.Wt: 244.2278
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 with IC50 of 2.2 μM, but has no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.
In Vivo: CGP57380 (40 mg/kg/d i.p.) potently extinguishes the ability of BC CML cells to serially transplant-immunodeficient mice and function as LSCs[4].
In Vitro: CGP57380 inhibits phosphorylation of eIF4E in cellular assays with IC50 of about 3 μM. CGP57380 causes dephosphorylation of eIF4E, and induces a further increase in the cap-dependent reporter in 293 cells[1]. CGP57380 results in dose-dependent decreases in Ang II-stimulated phosphorylation of eIF4E, protein synthesis, and VSMC hypertrophy[2]. CGP57380 sensitizes wild-type cells for serum-withdrawal induced apoptosis in mouse embryo fibroblasts (MEFs)[3]. CGP57380 prevents the serial replating function of BC progenitors[4].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC7381 CGP-57380 CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 (IC50 = 2.2 μM) with no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.
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