3-Arylisoquinolinamine derivative is a small molecule with antitumor activity. Its mechanism depends on the specific target, acting by binding to protein kinases, receptors, or enzymes to modulate signaling pathways, thereby affecting cell proliferation, differentiation, or metabolism.

3-Arylisoquinolinylamine derivative is a 3-arylisoquinolinylamine derivative that was taken out of compound 7b in reference [1]. The initial phase and its derivative (7b) of 3-arylisoquinolinylamine are the same. In comparison to paclitaxel, the more strong active cytotoxic anticancer medication paclitaxel is exhibited by the paclitaxel-resistant HCT-15 human colorectal cancer cell line. use of flow cytometry for the analysis of cell cycle dynamics. When 3-arylisoquinolinylamine derivatives (7b) are administered to human HCT-15 cells, they cause cell death and inhibit or impede the cells' transition from the G0/G1 phase into the S phase. In addition, treatment with 3-arylisoquinolinamine derivatives (7b) dramatically reduced tumor growth and improved tumor regression in an HCT-15 xenograft model resistant to paclitaxel. 3. With IC50 values ranging from 14 nM to 32 nM, 3-Arylisoquinolinylamine derivatives (7b) suppressed cell proliferation in tested human cancer cells. Using HCT-15 cells for cell cycle analysis, 1 nM treatment The 3-arylisoquinolinylamine derivative (7b) demonstrated a considerable rise in the G0/G1 phase and a decrease in the G2/M phase at 24 hours, but not the G0/G1 phase. The G1 phase did not significantly increase at 48 hours. The G0/G1 phase rose dramatically after 24 and 48 hours, the G2/M phase reduced, and a sub-G1 phase appeared at a greater concentration of 3-arylisoquinolinylamine derivative (7b) (10 nM). 3-Arylisoquinolinamine derivatives (7b) cause cell death by preventing or delaying the entry of cells from G0/G1 phase into S phase [1]. The 3-arylisoquinolinylamine derivative, or 3-arylisoquinolinylamine derivative 13, was taken from reference [1]. In colon cancer cells, a 3-arylisoquinolinamine derivative (compound 13) was evaluated, and its anticancer efficacy was contrasted with that of paclitaxel. Using IC50 values in the low nanomolar range, 3-Arylisoquinolinylamine derivatives (IC50: 15 nM in HCT-15 cells, 17 nM in HCT116 cells) shown strong antiproliferative activity in both cells. Additionally, on 15 colorectal cancer cells, paclitaxel-resistant HCT exhibited greater antitumor efficacy than paclitaxel [2].

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In vitro, 3-Arylisoquinolinamine derivative inhibits cell growth with IC50 values ranging from 14 nM to 32 nM in human cancer cells. It has demonstrated superior antitumor efficacy and is a potent compound with activity in the low nanomolar range.

In animal tests, the 3-arylisoquinolinamine derivative (compound 13) inhibits tumor growth more effectively than the control medication paclitaxel (48.8% inhibition) with a 69.2% inhibition rate [2].

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In vivo, 3-Arylisoquinolinamine derivative has demonstrated superior antitumor efficacy, achieving 69.2% inhibition of tumor growth in an animal model, outperforming the control drug Paclitaxel, which exhibited 48.8% inhibition.

In vitro enzyme/receptor binding assays for 3-Arylisoquinolinamine derivative are not well-defined. As a compound with antitumor activity, its mechanism likely involves binding to specific protein kinases or enzymes. Kinase inhibition assays could be used to identify its molecular target.

Cellular assays for 3-Arylisoquinolinamine derivative are conducted using human cancer cell lines to evaluate its antitumor activity. Cells are treated with the compound, and cell viability is measured to determine IC50 values, which range from 14 nM to 32 nM.

In vivo animal studies for 3-Arylisoquinolinamine derivative are conducted in xenograft models using human tumor cell lines. Tumor-bearing mice are treated with the compound, and tumor growth inhibition is measured. It has shown 69.2% tumor growth inhibition in an animal model.

The pharmacokinetic properties of 3-Arylisoquinolinamine derivative are characteristic of a small molecule. It has a molecular weight of 293.36 and a molecular formula of C18H19N3O. It is a heteroaromatic compound. Its exact PK parameters are not detailed in the provided literature.

The toxicological profile of 3-Arylisoquinolinamine derivative is not fully detailed. As a research compound with potent antitumor activity, its safety is evaluated in preclinical studies. It is for research use only and is not for human therapeutic use.

[1]. Synthesis, in vitro and in vivo evaluation of 3-arylisoquinolinamines as potent antitumor agents. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5277-81.

[2]. 5, 6, or 7-substituted-s- (hetero)arylisoquinolinamine derivatives as antitumor agents. WO 2008063548 A2.

3-Arylisoquinolinamine derivative is a compound with antitumor activity. It has demonstrated superior antitumor efficacy in an animal model, outperforming Paclitaxel. It is a small molecule that likely acts by modulating signaling pathways and is available for research use only.

293.153

1029008-71-6

24801853

Light yellow to yellow solid powder

4.139

1

4

3

22

362

0

CN(C)C1=CC2=C(N=C(C=C2C=C1)C3=CC(=CC=C3)OC)N

SSNNAZIMPALQIR-UHFFFAOYSA-N

InChI=1S/C18H19N3O/c1-21(2)14-8-7-12-10-17(20-18(19)16(12)11-14)13-5-4-6-15(9-13)22-3/h4-11H,1-3H3,(H2,19,20)

3-(3-methoxyphenyl)-7-N,7-N-dimethylisoquinoline-1,7-diamine

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ≥ 50 mg/mL (~170.44 mM)

Solubility in Formulation 1: ≥ 2.75 mg/mL (9.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% 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 27.5 mg/mL clear DMSO 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.

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 (Please use freshly prepared in vivo formulations for optimal results.)