[CAS NO. 64048-12-0] GANT58

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PRODUCTS SPECIFICATIONS [64048-12-0]

Catalog

HY-13282

Brand

MCE

CAS

64048-12-0

DESCRIPTION [64048-12-0]

Overview

MDL	MFCD01103196
Molecular Weight	392.48
Molecular Formula	C24H16N4S
SMILES	C1(C2=C(C(C3=CC=NC=C3)=C(S2)C4=CC=NC=C4)C5=CC=NC=C5)=CC=NC=C1

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

3 Publications Citing Use of MCE

Summary

GANT 58 (NSC 75503) is a potent GLI antagonist that inhibits GLI1-induced transcription with IC ₅₀ of 5 μM ^[1] .

IC50 & Target

IC50: 5 μM (Gli) ^[1]

In Vitro

GANT58 is a downstream inhibitor of Hh signaling. GANT58 is an indeed inhibitor of Hh signaling downstream of Smo and Sufu. GANT58 mainly acts at the nuclear level because transcription induced by GLI1 with a mutated nuclear export signal is still blocked. GANT58 efficiently inhibits in vitro tumor cell proliferation in a GLI-dependent manner and successfully blocks cell growth using human prostate cancer cells harboring downstream activation of the Hh pathway ^[1] . GANT58 (NSC75503) has been shown to inhibit transcriptional activation by GLI1 (as well as by the other GLI species). GANT58 has been shown to inhibit GLI transactivation ^[2] .

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

In Vivo

Nude mice are injected s.c. with GLI1-positive 22Rv1 prostate cancer cells, and tumors are established (median size ≈250 mm ³ ). Nude mice are treated with daily s.c. injections at a concentration of 50 mg/kg of cyclopamine, GANT61, GANT58, or solvent only (n=4-5 for each group). However, after 3 days, cyclopamine-treated animals presented with severe ulcerations at the injection sites. Therefore, changing the treatment regimen to injections only every second day. To be able to compare all compounds, this protocol is also introduced for the GANTs, although mice treated with these compounds showed no such signs of toxicity. All injections are done 2-3 cm away from the tumors. During an 18-day treatment period, suppression of tumor cell growth is observed for all compounds. Treatment with cyclopamine or GANT58 results in the inhibition of additional xenograft growth and limited the increase in tumor size ^[1] .

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 : 20 mg/mL ( 50.96 mM ; Need ultrasonic)

DMSO : 9.09 mg/mL ( 23.16 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5479 mL	12.7395 mL	25.4790 mL
5 mM	0.5096 mL	2.5479 mL	5.0958 mL
10 mM	0.2548 mL	1.2740 mL	2.5479 mL

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

In Vivo:

1.

Add each solvent one by one: 45% PEG300 >> 5% Tween-80 >> 50% saline

Solubility: 5 mg/mL (12.74 mM); Suspended solution; Need ultrasonic
2.

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

Solubility: 2 mg/mL (5.10 mM); Clear solution; Need ultrasonic
3.

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

Solubility: 2 mg/mL (5.10 mM); Clear solution; Need ultrasonic
4.

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

Solubility: ≥ 0.91 mg/mL (2.32 mM); Clear solution
5.

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

Solubility: ≥ 0.91 mg/mL (2.32 mM); Clear solution
6.

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

Solubility: ≥ 0.91 mg/mL (2.32 mM); Clear solution

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