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[CAS NO. 500579-04-4] GANT61

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Catalog:	HY-13901
Brand:	MCE
CAS:	500579-04-4

Overview

MDL	MFCD14635408
Molecular Weight	429.60
Molecular Formula	C27H35N5
SMILES	CN(C)C1=CC=CC=C1CN2C(C3=CC=NC=C3)N(CC4=CC=CC=C4N(C)C)CCC2

For research use only. We do not sell to patients.

46 Publications Citing Use of MCE

[1]Cell Res. 2022 Mar;32(3):288-301.
[2]Blood. 2016 Dec 8;128(23):2642-2654.
[3]Nat Commun. 2017 Jun 12;8:15773
[4]J Clin Invest. 2020 Dec 1;130(12):6354-6365.
[5]Cell Death Differ. 2021 Jul;28(7):2221-2237.
[6]ACS Appl Mater Interfaces. 2021 Jul 20.
[7]ACS Appl Mater Interfaces. 2017 Dec 13;9(49):42544-42555.
[8]Cell Rep. 2020 Apr.
[9]Br J Pharmacol. 2021 Sep;178(17):3428-3447.
[10]Cancer Lett. 2018 Apr 28;420:195-207.
[11]Cancer Lett. 2017 Jan 28;385:128-136.
[12]J Exp Clin Cancer Res. 2020 Jan 28;39(1):22.
[13]J Exp Clin Cancer Res. 2020 Jan 28;39(1):22.
[14]Stem Cells. 2020 Feb;38(2):261-275.
[15]Cell Prolif. 2021 Mar 23;e13026.
[16]Cell Proliferat. 2020 May;53(5):e12810.
[17]Cell Oncol. 2023 Jan 4.
[18]Stem Cell Res Ther. 2019 Jul 5;10(1):198.
[19]Cancer Sci. 2017 May;108(5):918-930.
[20]J Am Heart Assoc. 2022 Sep 14;e026365.
[21]J Cell Mol Med. 2021 Jun 2.
[22]FEBS J. 2020 Dec 13.
[23]Phytomedicine. 4 February 2022, 153972.
[24]Front Pharmacol. 2018 Jun 26;9:674.
[25]J Transl Med. 2022 Jun 25;20(1):286.
[26]Stem Cells Int. 15 Aug 2021.
[27]Life Sci. 2017 Dec 15;191:82-89.
[28]Cancer Med. 2018 Nov;7(11):5704-5715.
[29]Oncol Rep. 2020 Dec;44(6):2610-2620.
[30]Oncol Rep. 2019 May;41(5):2689-2702.
[31]Toxicol Appl Pharmacol. 2020 Jan 15;387:114853.
[32]Brain Sci. 2021 Jan 8;11(1):77.
[33]Prostate. 2020 Nov;80(15):1328-1340.
[34]Environ Toxicol. 2021 Feb;36(2):194-203.
[35]Biochem Bioph Res Co. 2020 Dec 17;533(4):770-778.
[36]Breast Cancer. 2017 Sep;24(5):683-693.
[37]Asian J Androl. 2018 Nov-Dec;20(6):608-614.
[38]Mech Dev. 2018 Dec;154:219-239.
[39]Cancer Biother Radiopharm. 2021 Dec 31.
[40]Chemotherapy. 2021 Nov 9.
[41]Int J Pharmacol. 2020 Jan.
[42]Hong Kong Polytechnic University. Department of Applied Biology and Chemical Technology. 2022 Feb.
[43]Research Square Preprint. 2021 Sep.
[44]Chinese Pharmacological Bulletin. 2018, 34(9): 1235-1242.
[45]Birla Institute of Technology, University of Colorado. 2016 Aug.
[46]Oncotarget. 2015 Nov 3;6(34):36700-12.

Summary

GANT 61 is an inhibitor of Gli1 and Gli2 targeting the Hedgehog/GLI pathway.

IC50 & Target

Gli1/2 ^[1]

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] .

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

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] .

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

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

Ethanol : 66.67 mg/mL ( 155.19 mM ; Need ultrasonic)

DMSO : 25 mg/mL ( 58.19 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3277 mL	11.6387 mL	23.2775 mL
5 mM	0.4655 mL	2.3277 mL	4.6555 mL
10 mM	0.2328 mL	1.1639 mL	2.3277 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% EtOH >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 5 mg/mL (11.64 mM); Clear solution
2.

Add each solvent one by one: 10% EtOH >> 90% (20% SBE-β-CD in saline)

Solubility: 5 mg/mL (11.64 mM); Suspended solution; Need ultrasonic
3.

Add each solvent one by one: 10% EtOH >> 90% corn oil

Solubility: ≥ 5 mg/mL (11.64 mM); Clear solution
4.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution
5.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (5.82 mM); Suspended solution; Need ultrasonic
6.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution
7.

Add each solvent one by one: 5% DMSO >> 40% PEG300 >> 5% Tween-80 >> 50% saline

Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution
8.

Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (5.82 mM); Suspended solution; Need ultrasonic

* All of the co-solvents are available by MCE.

References

[1] Mazumdar T, et al. Hedgehog signaling drives cellular survival in human colon carcinoma cells. Cancer Res. 2011 Feb 1;71(3):1092-102.
[2] Fu J, et al. GANT-61 inhibits pancreatic cancer stem cell growth in vitro and in NOD/SCID/IL2R gamma null mice xenograft. Cancer Lett. 2013 Mar 1;330(1):22-32.
[3] Wickstrom M, et al. Targeting the hedgehog signal transduction pathway at the level of GLI inhibits neuroblastoma cell growth in vitro and in vivo. Int J Cancer. 2013 Apr 1;132(7):1516-24.

Synonyms

Benzenamine, 2,2′-[[dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis[N,N-dimethyl-

2,2′-[[Dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis[N,N-dimethylbenzenamine]

NSC 136476

GANT 61

2-[[3-[[2-(Dimethylamino)phenyl]methyl]-2-pyridin-4-yl-1,3-diazinan-1-yl]methyl]-N,N-dimethylaniline

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