Volasertib trihydrochloride
Modify Date: 2024-01-07 00:46:32
Volasertib trihydrochloride structure
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Common Name | Volasertib trihydrochloride | ||
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| CAS Number | 946161-17-7 | Molecular Weight | 728.19500 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C34H53Cl3N8O3 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Volasertib trihydrochlorideVolasertib (BI 6727) trihydrochloride is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib trihydrochloride inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis. Volasertib trihydrochloride, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models[1][2]. |
| Name | N-[4-[4-(cyclopropylmethyl)piperazin-1-yl]cyclohexyl]-4-[[(7R)-7-ethyl-5-methyl-6-oxo-8-propan-2-yl-7H-pteridin-2-yl]amino]-3-methoxybenzamide,trihydrochloride |
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| Synonym | More Synonyms |
| Description | Volasertib (BI 6727) trihydrochloride is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib trihydrochloride inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis. Volasertib trihydrochloride, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models[1][2]. |
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| Related Catalog | |
| In Vitro | Volasertib trihydrochloride (BI 6727 trihydrochloride; 0.01-10000 nM; 72 hours) has EC50 values of 11 to 37 nmol/L in multiple cell lines[1]. Volasertib trihydrochloride (10-1000 nM; 24 hours) results accumulation of cells with 4N DNA content, indicative of a cell cycle block in G2-M phase[1]. Volasertib trihydrochloride (100 nM; 24-72 hours) induces cell apoptosis at 48 hours[1]. Cell Proliferation Assay[1] Cell Line: Multiple cell lines Concentration: 0.01-10000 nM Incubation Time: 72 hours Result: Inhibited proliferation of multiple cell lines derived from various cancer tissues, including carcinomas of the colon (HCT 116, EC50=23 nmol/L) and lung (NCI-H460, EC50=21 nmol/L), melanoma (BRO, EC50=11 nmol/L), and hematopoietic cancers (GRANTA-519, EC50=15 nmol/L; HL-60, EC50=32 nmol/L; THP-1, E50=36 nmol/L and Raji, EC50=37 nmol/L) with EC50 values of 11 to 37 nmol/L. Apoptosis Analysis[1] Cell Line: NCI-H460 cells Concentration: 100 nM Incubation Time: 24, 48, 72 hours Result: G2-M arrest at 24 hours was followed by induction of apoptosis at 48 hours. Cell Cycle Analysis[1] Cell Line: NCI-H460 cells Concentration: 10, 30, 100, 300, 1000 nM Incubation Time: 24 hours Result: Resulted in accumulation of cells with 4N DNA content, indicative of a cell cycle block in G2-M phase. |
| In Vivo | Volasertib trihydrochloride (BI 6727 trihydrochloride; A total weekly dose of 50 mg/kg; Oral; once a week, twice a week, or daily; for 40 days) shows comparable efficacy in human colon carcinoma xenograft models[1]. Volasertib trihydrochloride (15, 20, or 25 mg/kg/day; i.v.; 2 consecutive days per week; for 40 days) leads to significant tumor growth delay and even tumor regression in human colon carcinoma xenograft models [1]. Volasertib trihydrochloride (70 mg/kg given once weekly or 10 mg/kg daily; oral) significantly delays tumor growth in a non-small cell lung carcinoma xenograft model derived from NCI-H460 cells[1]. Volasertib (a single dose of 40 mg/kg; iv) causes a significant (13-fold) increase in mitotic cells in HCT 116 tumor-bearing nude mice[1]. Volasertib has high volume of distribution and a long terminal half-life in mice (Vss=7.6 L/kg, t1/2=46 h) and rats (Vss=22 L/kg, t1/2=54 h)[1]. Animal Model: Female BomTac:NMRI-Foxn1nu mice (Taconic) were grafted s.c. with HCT 116 human colon carcinoma cells (ATCC CCL-247)[1] Dosage: A total weekly dose of 50 mg/kg Administration: Oral; once a week, twice a week, or daily; for 40 days Result: Showed comparable efficacy and were well tolerated. Animal Model: Female BomTac:NMRI-Foxn1nu mice and male Wistar rats of the strain Crl:WI[1] Dosage: 35 mg/kg (mice) or 10 mg/kg (rat) (Pharmacokinetic Analysis) Administration: IV 5-minute infusion; a single dose 5-minute infusion Result: Had high volume of distribution and a long terminal half-life in mice (Vss=7.6 L/kg, t1/2=46 h) and rats (Vss=22 L/kg, t1/2=54 h). |
| Molecular Formula | C34H53Cl3N8O3 |
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| Molecular Weight | 728.19500 |
| Exact Mass | 726.33100 |
| PSA | 109.66000 |
| LogP | 7.32680 |
| bi 6727 cl3 |
| volasertib trihydrochloride |