5-Amino-1-(3,5-dichloro-4-(4-chlorobenzoyl)benzyl)-1H-1,2,3-triazole-4-carboxamide
- CAS No.99519-84-3
- Chemical Name:5-Amino-1-(3,5-dichloro-4-(4-chlorobenzoyl)benzyl)-1H-1,2,3-triazole-4-carboxamide
- CBNumber:CB5501698
- Molecular Formula:C17H12Cl3N5O2
- Formula Weight:424.67
- MOL File:99519-84-3.mol
- Melting point 200-202 °C
- Boiling point 685.5±65.0 °C(Predicted)
- Density 1.65±0.1 g/cm3(Predicted)
- storage temp. Store at +4°C
- solubility DMSO: soluble10mg/mL (clear solution)
- pka 14.16±0.50(Predicted)
- form powder
- color white to beige
- FDA UNII 6ST3ZF52WB
- NCI Dictionary of Cancer Terms carboxyamidotriazole
- NCI Drug Dictionary carboxyamidotriazole
- UNSPSC Code 12352200
- NACRES NA.77
-
Symbol(GHS)
- Signal wordDanger
- Hazard statements H301
- Precautionary statements P301+P310
- Brand: Sigma-Aldrich(India)
- Product number: SML0408
- Product name : Carboxyamidotriazole
- Purity: ≥98% (HPLC)
- Packaging: 5MG
- Price: ₹10846.65
- Updated: 2022/06/14
- Buy: Buy
- Brand: Sigma-Aldrich(India)
- Product number: SML0408
- Product name : Carboxyamidotriazole
- Purity: ≥98% (HPLC)
- Packaging: 25MG
- Price: ₹43830.43
- Updated: 2022/06/14
- Buy: Buy
5-Amino-1-(3,5-dichloro-4-(4-chlorobenzoyl)benzyl)-1H-1,2,3-triazole-4-carboxamide Chemical Properties,Usage,Production
- Uses Carboxyamidotriazole is an orally active calcium channel blocker. Carboxyamidotriazole also exhibits inhibition of pro-inflammatory cytokines in tumor associated macrophages as potential anti-cancer m echanism.
- Biological Activity Orally active Ca 2+ channel blocker; inhibits K + - and carbachol-stimulated Ca 2+ influx (IC 50 values are 500 and 935 nM respectively). Exhibits antiproliferative, antiangiogenic and antimetastatic activity in vivo and displays selectivity towards numerous mismatch repair-deficient tumor cell lines in vitro .
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in vivo
Carboxyamidotriazole (30 mg/kg; i.g.; daily; 19 days) combined with 2-deoxyglucose retards the growth of LLC tumors in C57BL/6 mice[4].
Carboxyamidotriazole (10-40 mg/kg; i.g.; once daily; from day 12 to day 26 after arthritis induction) reduces the severity of arthritis, inhibits hind paw swelling, decreases the infiltration of joint pathological inflammatory cells in the adjuvant arthritis model of Lewis rats induced by complete Freund's adjuvant[9].
Carboxyamidotriazole (30 mg/kg; i.g.; once daily; from day 7 to day 29 after inoculation of tumor cells) inhibits tumor growth, enhances the weights of gastrocnemius muscle and epididymal adipose tissue in the C57BL/6J mouse model inoculated with Lewis lung carcinoma cells[10].
Carboxyamidotriazole (30 mg/kg; i.g.; once daily; for 29 days) combined with low-dose Sorafenib (HY-10201) synergistically inhibits tumor growth in the C57BL/6J mouse model inoculated with Lewis lung carcinoma cells[11].
Carboxyamidotriazole (20 mg/kg; i.g.; once daily) combined with 1-MT or DMF, increases the number of CD8+ T cells in tumor-infiltrating lymphocytes (TILs), enhances the anti-tumor immune response of T cells, inhibits tumor growth, and prolongs the survival in the C57BL/6, BALB/c or RAG1 KO mouse models inoculated with B16, C26, 4T1 or B16-OVA tumor cells[12].
Carboxyamidotriazole (40 mg/kg, p.o., once daily, 14 days) reduces Bleomycin (HY-108345)-induced lung injury in mice[13].Animal Model: C57BL/6 mice (weight: 18-22 g) + LLC xenograft model[4] Dosage: Carboxyamidotriazole (30 mg/kg, dissolved in PEG 400), 2-DG (450 mg/kg) Administration: Carboxyamidotriazole was administered intragastrically daily, and 2-DG was administered intraperitoneally daily for 19 days Result: Caused no obvious changes in the animal body weight and behaviors.
Resulted in slower tumor growth than in the groups treated with Carboxyamidotriazole or 2-DG alone.Animal Model: C57BL/6J male mice (weight: 18-22 g, 6-8 weeks old) inoculated with Lewis lung carcinoma cells[11] Dosage: 30 mg/kg Administration: Intragastric administration, once daily, 29 days Result: Synergistically inhibited tumor growth in combination with low-dose Sorafenib.
Showed comparable efficacy to high-dose Sorafenib monotherapy.
Alleviated weight loss during cancer progression and inhibited NANOG expression in tumor tissues. - storage Store at +4°C
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- Benzoyl peroxide Chlorantraniliprole Benzyl chloride Benzyl acetate Sodium carboxymethyl cellulose 1H-Benzotriazole N,N-Dimethylformamide Benzyl alcohol 1,2,4-Triazole Formamide Benzyl benzoate Benzyl 4-ISOCYANATO-1-(TRIFLUOROACETYL)PIPERIDINE 2-Chloro-4-methylbenzaldehyde 2',6'-Dichloroacetophenone 3-Chloro-4-methylbenzylamine 2,4'-Dichlorobenzophenone 4-METHYL-1-PHENYLMETHYL-1H-1,2,3-TRIAZOLE
- 化学试剂
- 医用原料
- 抑制剂
- 药靶配体
- C17H12Cl3N5O2
- 羧基酰胺
- 羧胺三唑-[13C6]/精确称量
- 化合物 CARBOXYAMIDOTRIAZOLE
- L-651,582,CA2 +通道阻滞剂
- 化合物 T14872
- 羧胺三唑对照品
- 羧胺三唑
- 5-氨基-1-(3,5-二氯-4-(4-氯苯甲酰基)苄基)-1H-1,2,3-三氮唑-4-甲酰胺
- 99519-84-3
- 5-AMINO-1-[[3,5-DICHLORO-4-(4-CHLORO-BENZOYL)-PHENYL]METHYL]-1H-1,2,3-TRIAZOLE-4-CARBOXAMIDE
- 5-amino-1-[4-(4-chlorobenzoyl)-3,5-dichlorobenzyl]-1,2,3-triazole-4-carboxamide
- NSC 609974
- MERCK L651582
- Merck L651582 5-aMino-1-[3,5-dichloro-4-(4-chloro-benzoyl)-benzyl]-1H-[1,2,3]triazole-4-carboxylic acid aMide
- carboxyaMido-triazole(5-AMino-1-(3,5-dichloro-4-(4-chlorobenzoyl)benzyl)-1H-1,2,3-triazole-4-carboxaMide)
- L-651582
- 5-Amino-1-[4-(4-chlorobenzoyl)-3,5-dichlorobenzyl]-1H-1,2,3-triazole-4-carboxamide
- 1-[3,5-Dichloro-4-(4-chlorobenzoyl)benzyl]-5-amino-1H-1,2,3-triazole-4-carboxamide
- 5-Amino-1-(3,5-dichloro-4-(4-chlorobenzoyl)benzyl)-1H-1,2,3-triazole-4-carboxamide
- carboxyamido-triazole
- 1H-1,2,3-TRIAZOLE-4-CARBOXAMIDE-5-AMINO-1-[[3,5-DICHLORO-4-(4-CHLOROBENZOYL)PHENYL]METHYL]
- 5-Amino-1-[3,5-dichloro-4-(4-chlorobenzoyl)benzyl]-1H-[1,2,3]triazole-4-carboxylic acid amide