[CAS NO. 496794-70-8] HhAntag
PRODUCTS SPECIFICATIONS [496794-70-8]
DESCRIPTION [496794-70-8]
Overview
| MDL | MFCD25976715 |
|---|---|
| Molecular Weight | 450.92 |
| Molecular Formula | C24H23ClN4O3 |
| SMILES | O=C(NC1=CC=C(Cl)C(C2=NC3=CC=C(N(C)C)C=C3N2)=C1)C4=CC(OC)=CC(OC)=C4 |
Summary
In Vitro
HhAntag (2-30 µM; 72 hours) demonstrates to be 10-times more potent than the natural product SMO antagonist, cyclopamine, at inhibiting Hh pathway activity and it inhibits Hh signalling pathway sensitivitive cells with IC
50
values ranging from 2 µM to >30 µM
[1]
.
HhAntag inhibits AsPC-1, BXPC-3, CFPAC, HPAC, HPAF-II, KP4, Panc 03.27, PA-TU-8902, PSN-1, SU.86.86 cells with IC
50
values of 30 µM, 5.4 µM, 5.8 µM, 2.7 µM, 6.2 µM,10.3 µM, 2.5 µM, 2.9 µM, 5.8 µM and 2.7 µM, respectively
[1]
.
HhAntag (100 nM) is needed to completely inhibit Hh signalling in a Hh-responsive human mesenchymal cell line (HEPM) expressing a GLI luciferase reporter construct (HEPM-rep), the IC
50
of 5 nM 400-times lower than that required to inhibit cell growth by 50% in the most sensitive cancer cell line (1.9 μM)
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
HhAntag (oral administraion; 75 mg/kg or 100 mg/kg; twice daily; 25 days) results in significant growth delay in HT55 and HT-29 colorectal cell line xenografts models, with average tumour growth inhibitions of 29% and 48%, respectively. Whereas HhAntag had no effect on the growth of DLD-1 xenografts
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Primary human xenografts in female CD1 nu/nu mice of 6–8 weeks (DLD-1, HT55 and HT-29 cells) [1] |
| Dosage: | 75 mg/kg or 100 mg/kg |
| Administration: | Oral administraion; twice daily; 25 days |
| Result: | Resulted in growth delay of HT55 and HT-29 xenografts, but had no effects on DLD-1 xenografts. |
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
DMSO : ≥ 100 mg/mL ( 221.77 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2177 mL | 11.0884 mL | 22.1769 mL |
| 5 mM | 0.4435 mL | 2.2177 mL | 4.4354 mL |
| 10 mM | 0.2218 mL | 1.1088 mL | 2.2177 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 3 mg/mL (6.65 mM); Clear solution