EHop-016

Cas No.:	1380432-32-5
Chemical Name:	4-N-(9-Ethylcarbazol-3-yl)-2-N-(3-morpholin-4-ylpropyl)pyrimidine-2,4-diamine
Synonyms:	EHop-016;4-N-(9-ethylcarbazol-3-yl)-2-N-(3-morpholin-4-ylpropyl)pyrimidine-2,4-diamine;EHop016;N4-(9-ETHYL-9H-CARBAZOL-3-YL)-N2-(3-MORPHOLIN-4-YL-PROPYL)-PYRIMIDINE-2,4-DIAMINE;N4-(9-Ethyl-9H-carbazol-3-yl)-N2-[3-(4-morpholinyl)propyl]-2,4-pyrimidinediamine;EHop 016;N4-(9-Ethyl-9H-carbazol-3-yl)-N2-(3-morpholinopropyl)pyrimidine-2,4-diamine;C25H30N6O;SYN5172;AOB1274;HMS3653G12;BCP09978;s7319;BDBM50007190;SB19476;AK474016;BC600318;X5938;SW219568-1;A12740;rel-N-[(1R,2S)-2-Phenylcyclopropyl]-4-piperidinamine
SMILES:	O1C([H])([H])C([H])([H])N(C([H])([H])C1([H])[H])C([H])([H])C([H])([H])C([H])([H])N([H])C1=NC([H])=C([H])C(=N1)N([H])C1C([H])=C([H])C2=C(C=1[H])C1=C([H])C([H])=C([H])C([H])=C1N2C([H])([H])C([H])([H])[H]
Formula:	C25H30N6O
M.Wt:	430.5453
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

EHop-016 is specific for Rac1 and Rac3 at concentrations of ≤5 μM. At higher concentrations, EHop-016 inhibits the close homolog Cdc42. In MDA-MB-435 cells that demonstrate high active levels of the Rac GEF Vav2, EHop-016 inhibits the association of Vav2 with a nucleotide-free Rac1(G15A), which has a high affinity for activated GEFs. EHop-016 also inhibits the Rac activity of MDA-MB-231 metastatic breast cancer cells and reduces Rac-directed lamellipodia formation in both cell lines. EHop-016 decreases Rac downstream effects of PAK1 (p21-activated kinase 1) activity and directed migration of metastatic cancer cells. Moreover, at effective concentrations (<5 μM), EHop-016 does not affect the viability of transformed mammary epithelial cells (MCF-10A) and reduces viability of MDA-MB-435 cells by only 20%. Therefore, EHop-016 holds promise as a targeted therapeutic agent for the treatment of metastatic cancers with high Rac activity. Rac inhibition by EHop-016 increases the activity of the closely related Rho GTPase RhoA by a compensatory mechanism. . For the detailed information of EHop-016, the solubility of EHop-016 in water, the solubility of EHop-016 in DMSO, the solubility of EHop-016 in PBS buffer, the animal experiment (test) of EHop-016, the cell expriment (test) of EHop-016, the in vivo, in vitro and clinical trial test of EHop-016, the EC50, IC50,and affinity,of EHop-016, Please contact DC Chemicals.