GANT61(NSC 136476)

Cas No.:	500579-04-4
Chemical Name:	2-[[3-[[2-(Dimethylamino)phenyl]methyl]-2-pyridin-4-yl-1,3-diazinan-1-yl]methyl]-N,N-dimethylaniline
Synonyms:	GANT 61;2,2'-((2-(Pyridin-4-yl)dihydropyrimidine-1,3(2H,4H)-diyl)bis(methylene))bis(N,N-dimethylaniline);2-[[3-[[2-(dimethylamino)phenyl]methyl]-2-pyridin-4-yl-1,3-diazinan-1-yl]methyl]-N,N-dimethylaniline;GANT 61 (NSC 136476);GANT-61;NSC 136476;2,2′-[[Dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis[N,N-dimethyl-benzenamine;GANT61;NSC136476;GNT61;GANT 61(NSC 136476);C27H35N5;NCIStruc1_001747;NCIStruc2_001814;BCP08050;NCGC00014352;NCI136476;2423AH;BDBM5024
SMILES:	N1(C([H])([H])C2=C([H])C([H])=C([H])C([H])=C2N(C([H])([H])[H])C([H])([H])[H])C([H])([H])C([H])([H])C([H])([H])N(C([H])([H])C2=C([H])C([H])=C([H])C([H])=C2N(C([H])([H])[H])C([H])([H])[H])C1([H])C1C([H])=C([H])N=C([H])C=1[H]
Formula:	C27H35N5
M.Wt:	429.6003
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	GANT 61 is an inhibitor of Gli1 and Gli2 targeting the Hedgehog/GLI pathway.
In Vivo:	GANT-61 (40 mg/kg, i.p., three days per week) inhibits CSC tumor growth in NOD/SCID IL2Rγ null mice[2]. GANT61 (50 mg/kg, p.o.) enhances the effects of chemotherapeutic drugs used in the treatment of neuroblastoma in an additive or synergistic manner and reduces the growth of established neuroblastoma xenografts in nude mice[3].
In Vitro:	GANT61 (20 μM) induces greater cell death than targeting Smo (cyclopamine). GANT61 (0, 5, 10, 20 μM) inhibits clonogenic survival of human colon carcinoma cell lines. GANT61 (20 μM, 0-72 hr) down-regulates Gli1 and Gli2 expression in HT29 cells. GANT61 (0, 10 μM or 20 μM) differentially regulates genes involved in the balance between cell death and cell survival[1]. GANT-61 inhibits cell viability and induces apoptosis in pancreatic CSCs. GANT-61 inhibits expression of downstream targets of Shh pathway, decreases Gli-DNA interaction, Gli transcriptional activity and Gli nuclear translocation in pancreatic CSCs. GANT-61 differentially regulates genes involved in cell survival, cell death and pluripotency. GANT-61 inhibits motility, invasion and migration of CSCs[2]. GANT61 sensitivity positively correlates to GLI1 and negatively to MYCN expression in the neuroblastoma cell lines tested. GANT61 downregulates GLI1, c-MYC, MYCN and Cyclin D1 expression and induces apoptosis of neuroblastoma cells[3].