| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
GANT 58 (NSC 75503), a tetrapyridinylthiophene compound, is a novel, cell-permeable and potent Gli antagonist that inhibits GLI1-induced transcription with IC50 of 5 μM. GANT58 acts as downstream Hedgehog (Hh) pathway blocker and targets Gli-mediated gene transactivation (IC50 ~ 5 µM in SAG-stimulated Shh-L2 cells).
| Targets |
Gli(IC50= 5 μM)
|
|---|---|
| ln Vitro |
Hh signaling is inhibited downstream by GANT58. Indeed, GANT58 inhibits Hh signaling by blocking Smo and Sufu. Because transcription induced by GLI1 with a mutated nuclear export signal is still blocked, GANT58 primarily functions at the nuclear level. GANT58 successfully inhibits the growth of tumor cells in vitro in a manner that is dependent on GLI. This is achieved by using human prostate cancer cells that have downstream activation of the Hh pathway to block cell growth[1].
It has been demonstrated that GANT58 (NSC75503) prevents GLI1 (as well as the other GLI species) from activating transcription. It has been demonstrated that GANT58 inhibits GLI transactivation[2]. |
| ln Vivo |
Tumors (median size ≈250 mm3) are created by injecting GLI1-positive 22Rv1 prostate cancer cells subcutaneously into nude mice. Every day, n = 4–5 injections of solvent alone, GANT61, GANT58, or cyclopamine at a dose of 50 mg/kg are given to naked mice. But after three days, the animals receiving cyclopamine showed signs of severe ulcerations at the injection sites. Consequently, the treatment plan was modified to include injections only once every two days.This protocol is also introduced for the GANTs so that all compounds can be compared, even though the mice treated with these compounds did not exhibit any toxicity. Every injection is made two to three centimeters away from the tumors. For all compounds, there is suppression of tumor cell growth during the course of an 18-day treatment period. The administration of GANT58 or cyclopamine inhibits the growth of additional xenografts and restricts the growth of tumors[1].
|
| References |
| Molecular Formula |
C24H16N4S
|
|---|---|
| Molecular Weight |
392.47564
|
| Exact Mass |
392.11
|
| Elemental Analysis |
C, 73.45; H, 4.11; N, 14.28; S, 8.17
|
| CAS # |
64048-12-0
|
| Appearance |
Solid powder
|
| SMILES |
C1(C2=CC=NC=C2)=C(C3=CC=NC=C3)C(C4=CC=NC=C4)=C(C5=CC=NC=C5)S1
|
| InChi Key |
USWLOKMMUTWFMD-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C24H16N4S/c1-9-25-10-2-17(1)21-22(18-3-11-26-12-4-18)24(20-7-15-28-16-8-20)29-23(21)19-5-13-27-14-6-19/h1-16H
|
| Chemical Name |
2,3,4,5-Tetra(4-pyridyl)thiophene
|
| Synonyms |
NSC75503; NSC-75503; NSC 75503; GANT 58; GANT-58.
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
Ethanol : ~20 mg/mL (~50.96 mM)
DMSO : ~9.09 mg/mL (~23.16 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (5.10 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear EtOH stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2 mg/mL (5.10 mM) (saturation unknown) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.91 mg/mL (2.32 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 0.91 mg/mL (2.32 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 9.1 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 5: ≥ 0.91 mg/mL (2.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 9.1 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 6: 10% EtOH+40% PEG300+5% Tween-80+45% Saline: 2 mg/mL (5.10 mM) Solubility in Formulation 7: 5 mg/mL (12.74 mM) in 45% PEG300 5% Tween-80 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
|
|
|
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
