| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
The most prevalent cancer types' cells show antiproliferative activity when exposed to antitumor agent-81 (0–20 µM; 72 h)[1]. In HCT-116 cells, antitumor agent-81 (1, 2, 5 µM; 24 h) impairs HR (homologous recombination)-mediated DSB repair[1]. In HCT-116 cells, antitumor agent-81 tethers the relationship between P62 and RNF168[1]. In HCT-116 cells, antitumor agent-81 inhibits RNF168's catalytic activity as well as RNF168 E3 ligase activity[1].
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|---|---|
| ln Vivo |
Tumor volumes are suppressed in mice by antitumor agent-81 (5, 10 mg/kg; ip; once every three days for 22 days) in a dose-dependent manner[1]. 1.19 Antitumor agent-81 pharmacokinetic parameters in female BALB/c nude mice[1]. IP (5 mg/kg) 16.17 26.10 215.69 19647.83 IP (10 mg/kg) 31.00 39.87 408.18 16554.30 IP (20 mg/kg) 22.10 52.23 1003.58 14669.81 Dose T1/2 (h) Cmax (ng/mL) AUC0-t (h㻿ng/mL) CL ((mL/h)/kg)
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: A549, HCT-116, A375, HeLa, HepG2, MCF-7, MDA-MB-231, MGC-803, U2OS and MCF-10A cells Tested Concentrations: 0 -20 µM Incubation Duration: 72 h Experimental Results: Inhibited A549, HCT-116, A375, HeLa, HepG2, MCF-7, MDA-MB-231, MGC-803, U2OS and MCF-10A cells, with IC50 values of 1.18, 0.36, 1.93, 2.48, 19.61, 2.79, 1.17, 1.88, 3.64 and 6.98, respectively. Cell Cycle Analysis[1] Cell Types: HCT-116 cells Tested Concentrations: 1, 2, 5 µM Incubation Duration: 24 h Experimental Results: Induced a G2/M arrest but no significant accumulation of sub-G1 phase. Compromised both HR(homologous recombination)- and NHEJ (non-homologous end joining)- mediated DSB repair in a dose-dependent manner, but HR was the more severely impacted process . |
| Animal Protocol |
Animal/Disease Models: Female BALB/c nude mice (xenograft tumor model)[1].
Doses: 5, 10 mg/kg Route of Administration: intraperitoneal (ip) injection; single every 3 days for 22 days Experimental Results: Suppressed tumor growth by promoting apoptosis in xenografted tumorigenesis. Animal/Disease Models: Female BALB/c nude mice[1]. Doses: 5, 10, 20 mg/kg Route of Administration: intraperitoneal (ip) injection; single Experimental Results: demonstrated plasma concentration peaked 1 h after administration. demonstrated a relatively high maximum concentration (Cmax= 52.23 ng/mL) and exposure (AUC0-t= 1003.58 h·ng/mL) at a dose of 20 mg/kg. |
| References |
| Molecular Formula |
C19H19N7O3
|
|---|---|
| Molecular Weight |
393.399262666702
|
| Exact Mass |
393.154
|
| CAS # |
2765180-17-2
|
| PubChem CID |
163214076
|
| Appearance |
Off-white to light yellow solid powder
|
| LogP |
1.8
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
29
|
| Complexity |
530
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
SWULRQWLALOGFO-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H19N7O3/c1-27-15-7-11(8-16(28-2)17(15)29-3)26-9-14(24-25-26)10-4-5-13-12(6-10)18(20)23-19(21)22-13/h4-9H,1-3H3,(H4,20,21,22,23)
|
| Chemical Name |
6-[1-(3,4,5-trimethoxyphenyl)triazol-4-yl]quinazoline-2,4-diamine
|
| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5419 mL | 12.7097 mL | 25.4194 mL | |
| 5 mM | 0.5084 mL | 2.5419 mL | 5.0839 mL | |
| 10 mM | 0.2542 mL | 1.2710 mL | 2.5419 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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