IITZ-01|cas 1807988-47-1|DC Chemicals

Cas No.:	1807988-47-1
Chemical Name:	IITZ-01
Synonyms:	IITZ-01;N2-(4-(1H-benzo[d]imidazol-2-yl)phenyl)-N4-(4-fluorophenyl)-6-morpholino-1,3,5-triazine-2,4-diamine;IITZ01;BCP29968;s8764;D80590;4-N-[4-(1H-benzimidazol-2-yl)phenyl]-2-N-(4-fluorophenyl)-6-morpholin-4-yl-1,3,5-triazine-2,4-diamine;AUTOPHAGY INHIBITOR;IITZ 01;Autophagy inhibitor IITZ-01;AUTOPHAGY INHIBITOR IITZ-01;CS-2857;1,3,5-Triazine-2,4-diamine, N2-[4-(1H-benzimidazol-2-yl)phenyl]-N4-(4-fluorophenyl)-6-(4-morpholinyl)-;N-[4-(1H-Benzimidazol-2-yl)phenyl]-N'-(4-fluorophenyl)-6-(4-morpholinyl)-1,3,5-triazine-2,4-diamine
SMILES:	FC1C=CC(=CC=1)NC1N=C(NC2C=CC(=CC=2)C2=NC3C=CC=CC=3N2)N=C(N=1)N1CCOCC1
Formula:	C₂₆H₂₃FN₈O
M.Wt:	482.523
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ.
In Vivo:	Tumors after reaching ~100 mm3, vehicle, 45 mg/kg of IITZ-01, is administered through intraperitoneal (i.p.) route on every alternate day for 4 weeks. IITZ-01 reduces the active tumor burden around 8.8-fold, when compared with control group as determined by tumor photon counts. Moreover, tumor volume measurements have demonstrated that IITZ-01 has significantly inhibited average tumor growth when compared with control from third day of treatment. Significant reduction in average tumor weights is observed after treatment with IITZ-01 compared with control. This treatment schedule of both compounds is well tolerated in mice for the total duration of administration with no significant changes in their body weights[1].
In Vitro:	IITZ-01 shows negligible inhibition toward PI3Kγ (IC50: 2.62μM). Time-course immunoblotting experiment with IITZ-01-treated cells also displays significant elevation in SQSTM1 levels, indicating the autophagy inhibitory nature of the compound. In addition to that, both compounds IITZ-01 has demonstrated potent autophagy inhibitory activity in other breast, lung, and colon cancer cells[1].
References:	[1]. Guntuku L, et al. IITZ-01, a novel potent lysosomotropic autophagy inhibitor, has single-agent antitumor efficacy in triple-negative breast cancer in vitro and in vivo. Oncogene. 2018 Aug 30.

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