1. GPCR/G Protein
  2. Ras

1A-116 

Cat. No.: HY-104064 Purity: 99.28%
Handling Instructions

1A-116 is a specific Rac1 inhibitor.

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

1A-116 Chemical Structure

1A-116 Chemical Structure

CAS No. : 1430208-73-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 211 In-stock
Estimated Time of Arrival: December 31
5 mg USD 192 In-stock
Estimated Time of Arrival: December 31
10 mg USD 312 In-stock
Estimated Time of Arrival: December 31
25 mg USD 660 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1128 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1920 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

1A-116 is a specific Rac1 inhibitor.

IC50 & Target

Rac1[1]

In Vitro

1A-116 shows lesser effect on MCF7::pcDNA.3 cells than on MCF7::C1199 cells. 1A-116 treatment decreases phospho-PAK1 levels in a time-dependent manner. The presence of 1A-116 reverts the PAK1 phosphorylation induced by 4-hydroxytamoxifen (Tam). The presence of 1A-116 also effectively reverts Rac1-PAK1-mediated estrogen receptor (ER) phosphorylation at Ser305[1]. 1A-116 shows a significant increase in antiproliferative activity on F3II cells, showing an IC50 value of 4 µM. A-116 also dramatically impairs Rac1 activation at low micromolar range (1 µM)[2].

In Vivo

Daily treatment of mice with compound 1A-116 at 3mg/kg body weight/day reduces about 60% the formation of total metastatic lung colonies. A significant antitumor activity is obtained for macronodules (more than 1 mm in diameter) by treatment with 1A-116 in this highly aggressive breast cancer model. The treatment with 1A-116 reduces the total lung weight compare to the control group, leading to a total weight similar to the average pulmonary weight of Balb/c mice[2].

References
Cell Assay
[1]

5×103 MCF7::pcDNA.3 and MCF7::C1199 cells are plated in 96-wells plates and 24 hours later are treated for 72 hours with different concentrations of 17-β-Estradiol to evaluate hormone response. To evaluate the reversion of 4-hydroxytamoxifen (Tam) resistance by 1A-116, MCF7::C1199 cells are treated with Tam (0.01 μM, 0.1 μM and 1 μM), 1A-116 (4 μM) or combination of both for 72 hours. Cell growth is measured by colorimetric crystal violet assay. The analysis of hormone-dependent growth and Tam resistance reversion is determined using PRISM 6, Version 6.01. Results shown correspond to the average of three independent experiments[1].

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

Animal Administration
[2]

Specific pathogen-free female BALB/c inbred mice with an age of 8 to 10 weeks and an average weight of 20 g, are used. They are housed in plastic cages under standard conditions and have access to rodent chow and water ad libitum. On day 0, 2×105 viable F3II cells in 0.3 mL Dulbecco’s modified Eagle medium (DMEM) are injected into the lateral tail vein. Mice are injected i.p at daily doses of 3 mg/kg body weight 1A-116 or vehicle. Treatment is carried out from day 0 to day 21. On day 21 mice are sacrificed and lungs are excised and immediately fixed in Bouin’s solution. Superficial lung nodules are counted under dissection microscope[2].

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

References
Molecular Weight

307.31

Formula

C₁₆H₁₆F₃N₃

CAS No.

1430208-73-3

SMILES

N=C(NC1=CC=CC=C1C(F)(F)F)NC2=CC(C)=CC(C)=C2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
1A-116
Cat. No.:
HY-104064
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1A-116

Cat. No.: HY-104064