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Chemical Structure| 500579-04-4 Chemical Structure| 500579-04-4

Structure of GANT61
CAS No.: 500579-04-4

Chemical Structure| 500579-04-4

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

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Product Details of GANT61

CAS No. :500579-04-4
Formula : C27H35N5
M.W : 429.60
SMILES Code : CN(C)C1=CC=CC=C1CN2C(C3=CC=NC=C3)N(CC4=CC=CC=C4N(C)C)CCC2
MDL No. :MFCD14635408
InChI Key :KVQOGDQTWWCZFX-UHFFFAOYSA-N
Pubchem ID :421610

Safety of GANT61

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H319
Precautionary Statements:P305+P351+P338

Related Pathways of GANT61

Hedgehog

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
MCF7-Ctrl 10 µM 48 h Restores EMT marker expression, inhibits invasion Nat Commun. 2017 Jun 12;8:15773.
HMLER-Ctrl 10 µM 48 h Inhibits GLI signaling activation, reduces migration and invasion Nat Commun. 2017 Jun 12;8:15773.
AML cell lines 20 μM 24 h Induced apoptosis, resulting in approximately 30% of cells undergoing apoptosis J Hematol Oncol. 2017 Jan 21;10(1):26.
PANC-1 30 μM 3 days GANT61 had a more modest effect on the viability and sphere formation of PANC-1 cells, but still significantly reduced cell viability at 30 μM. Mol Cancer. 2016 Jun 27;15(1):49.
Capan-1 M9 20 μM 3 days Inhibition of the Hh pathway significantly reduced the expression of stem cell marker CD133 and sphere formation, demonstrating the suppression of CSC-like properties. GANT61 was more effective than the SMO inhibitor cyclopamine in reducing sphere formation and cell viability. Mol Cancer. 2016 Jun 27;15(1):49.
Human mesenchymal stem cells 10 μM 24-48 h To investigate the effect of GANT61 on mesenchymal stem cells from MPN patients and healthy donors, results showed that GANT61 significantly reduced the expression of α-SMA and Gli1, and induced apoptosis in MPN-MSCs. Cell Stem Cell. 2017 Jun 1;20(6):785-800.e8.
NCI-H1299 cells 10, 20, and 30 μM Inhibited the migration and invasion abilities of NCI-H1299 cells Acta Pharm Sin B. 2022 Oct;12(10):3877-3890.
HT29 cells 20 µM 72 h GANT61 induced accumulation of HT29 cells at G1/S and early S-phase, followed by entry into subG1, leading to cell death. Cancer Res. 2011 Sep 1;71(17):5904-14.
WB-F344 cells 2 μM 4 days Inhibition of Gli1 expression reduced the expression of KRT19 and Ki67, as well as proinflammatory cytokines including IL-6 and TNF-α, thereby suppressing the differentiation of HPCs into cholangiocytes. Theranostics. 2024 Mar 25;14(6):2379-2395.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Capan-1 M9 xenograft model Intraperitoneal injection 40 mg/kg 3 times a week for 25 days Combination treatment with GANT61 and the mTOR inhibitor rapamycin significantly inhibited tumor growth in the Capan-1 M9 xenograft model. Mol Cancer. 2016 Jun 27;15(1):49.
Mice Jak2(V617F)-induced myelofibrosis model Subcutaneous injection 50 mg/kg Every other day for 9 weeks To investigate the therapeutic effect of GANT61 on Jak2(V617F)-induced myelofibrosis, results showed that GANT61 significantly reduced the number of Gli1+ cells, inhibited the development of bone marrow fibrosis, and improved splenomegaly and hemoglobin levels. Cell Stem Cell. 2017 Jun 1;20(6):785-800.e8.
BALB/c nude mice NSCLC metastasis model Intraperitoneal injection 50 mg/kg Every two days for a total of 30 days GANT-61 significantly suppressed the lung and liver metastasis of NSCLC Acta Pharm Sin B. 2022 Oct;12(10):3877-3890.
Mice Breast cancer xenograft model Subcutaneous injection 50 mg/kg Every other day for 18 days Inhibits metastasis and growth of non-EMT cells Nat Commun. 2017 Jun 12;8:15773.
Mice Unilateral ureteral obstruction model Subcutaneous injection 50 mg/kg Administered on days 1, 2, 3, 5, 7, and 9 after surgery GANT61 reduced renal fibrosis by decreasing GLI1 and GLI2 protein levels. J Clin Invest. 2015 Aug 3;125(8):2935-51
Nude mice NSCLC xenograft model Intraperitoneal injection 50 mg/kg Every other day for 24 days To evaluate the effect of GANT61 on tumor angiogenesis and tumor growth in NSCLC, the results showed that GANT61 significantly inhibited tumor angiogenesis and tumor growth. J Exp Clin Cancer Res. 2024 Mar 16;43(1):83

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.64mL

2.33mL

1.16mL

23.28mL

4.66mL

2.33mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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