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  3. HhAntag

HhAntag 

Cat. No.: HY-15412 Purity: 98.70%
Handling Instructions

HhAntag is a specific, potent and orally active small molecule SMO antagonist of the Hh pathway.

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

HhAntag Chemical Structure

HhAntag Chemical Structure

CAS No. : 496794-70-8

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 325 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 325 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 295 In-stock
Estimated Time of Arrival: December 31
10 mg USD 516 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1850 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2712 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

HhAntag is a specific, potent and orally active small molecule SMO antagonist of the Hh pathway[1].

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 IC50 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 IC50 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 IC50 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.
Molecular Weight

450.92

Formula

C₂₄H₂₃ClN₄O₃

CAS No.
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: 

DMSO : ≥ 100 mg/mL (221.77 mM)

*"≥" means soluble, but saturation unknown.

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 3 mg/mL (6.65 mM); Clear solution

  • 2.

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

    Solubility: ≥ 3 mg/mL (6.65 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
HhAntag
Cat. No.:
HY-15412
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