839706-07-9
BenzaMide, N-[3-[1,4-dihydro-1-Methyl-7-[(6-Methyl-3-pyridinyl)aMino]-2-oxopyriMido[4,5-d]pyriMidin-3(2H)-yl]-4-Methylphenyl]-3-(trifluoroMethyl)-
CAS: 839706-07-9
Molecular Formula: C28H24F3N7O2
839706-07-9 - Names and Identifiers
839706-07-9 - Physico-chemical Properties
| Molecular Formula | C28H24F3N7O2 |
| Molar Mass | 547.53 |
| Density | 1.404±0.06 g/cm3(Predicted) |
| pKa | 12.82±0.70(Predicted) |
| Storage Condition | 2-8℃ |
| In vitro study | GNF-7 potently inhibits wild-type Bcr-Abl (IC 50 <5 nM) and Bcr-Abl mutants such as T315I (IC 50 =11 nM), G250E (IC 50 <5 nM), E255V (IC 50 =10 nM), F317L (IC 50 <5 nM) and M351T (IC 50 <5 nM) in cellular assays. GNF-7 (1 μM; 2 hours) suppresses AKT/mTOR signaling and GCK downstream. GNF-7 (1 μM; 24 hours) induces of apoptosis and cell cycle arrest in NRAS mutant cell lines. Western Blot Analysis Cell Line: Ba/F3-NRAS-G12D cells, OCI-AML3 cells Concentration: 1 μM Incubation Time: 2 hours Result: Caused a decreased level of phosphorylation of p70S6K1, AKT (S473), JNK, and p38. Apoptosis Analysis Cell Line: OCI-AML3 cells Concentration: 1 μM Incubation Time: 24 hours Result: Increased the levels of both cleaved PARP and cleaved caspase 3 and diminished bcl-2 and MCL1. Cell Cycle Analysis Cell Line: OCI-AML3 cells Concentration: 1 μM Incubation Time: 24 hours Result: Induced of G0-G1 arrest. |
| In vivo study | GNF-7 (10-20 mg/kg; o.p.; daily; for 7 days) displays significant in vivo efficacy against T315I Bcr-Abl in the bioluminescent xenograft mouse model. GNF-7 exhibits moderate oral bioavailability (mice 36%) and C max (mice 3616 nM) following oral administration (mice 20 mg/kg). GNF-7 exhibits terminal elimination half-lives (mice 3.8 h) due to high plasma clearance (8.6 mL/min/kg) following intravenous injection (mice 5 mg/kg). Animal Model: 6-8 weeks old SCID beige female mice, with Ba/F3-T315I-Bcr-Abl cells xenograft Dosage: 10 mg/kg, 20 mg/kg Administration: Oral administration, daily, for 7 days Result: Effectively inhibited tumor growth of T315I-Bcr-Abl-Ba/F3 cells in mice at low doses (10 mg/kg). Animal Model: 5-6 weeks old male Balb/c mice (20-25 g) Dosage: 5 mg/kg for i.v.; 20 mg/kg for i.g. (Pharmacokinetic Analysis) Administration: Intravenous injection and oral gavage Result: Oral bioavailability (36%), C max (3616 nM), T 1/2 (3.2 h). |
839706-07-9 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.826 ml | 9.132 ml | 18.264 ml |
| 5 mM | 0.365 ml | 1.826 ml | 3.653 ml |
| 10 mM | 0.183 ml | 0.913 ml | 1.826 ml |
| 5 mM | 0.037 ml | 0.183 ml | 0.365 ml |
Last Update：2024-01-02 23:10:35
839706-07-9 - Reference Information
| biological activity | GNF-7 is a multiple kinase inhibitor. GNF-7 are Bcr-Abl inhibitors with IC50 values for Bcr-AblWT and Bcr-AblT315I effects of 133 nM and 61 nM, respectively. GNF-7 also has inhibitory activity on ACK1 and GCK, with IC50 of 25 nM and 8 nM respectively. GNF-7 can be used for the study of hematological malignancies. |
| target | IC50: 133 nM (Bcr-Abl WT ), 61 nM (Bcr-Abl T315I ), 25 nM (ACK1), 8 nM (GCK) |
| in vitro study | GNF-7 potently inhibits wild-type Bcr-Abl (IC 50 <5 nM) and Bcr-Abl mutants such as T315I (IC 50=11 nM), G250E (IC 50 <5 nM), E255V (IC 50=10 nM), f317L (IC 50 <5 nM) and M351T (IC 50 <5 nM) in cellular assays. GNF-7 (1 μ M; 2 hours) suppresses AKT/mTOR signaling and GCK downstream. GNF-7 (1 μ M; 24 hours) induces of apoptosis and cell cycle arrest in NRAS mutant cell lines. Western Blot Analysis Cell Line: Ba/F3-NRAS-G12D cells, OCI-AML3 cells Concentration: 1 μM Incubation Time: 2 hours result: used a decreased level of phosphorylation of p70S6K1, AKT (S473), JNK, and p38. Apoptosis Analysis Cell Line: OCI-AML3 cells Concentration: 1 μM Incubation Time: 24 hours result: Increased the levels of both cleaved PARP and cleaved caspase 3 and diminished bcl-2 and MCL1. Cell Cycle Analysis Cell Line: OCI-AML3 cells Concentration: 1 μM Incubation Time: 24 hours Result: Induced of G0-G1 arrest. |
| Cell Line: | Ba/F3-NRAS-G12D cells, OCI-AML3 cells OCI-AML3 cells OCI-AML3 cells |
| Concentration: | 1 μM 1 μM 1 μM |
| Incubation Time: | 2 hours 24 hours 24 hours |
| Result: | used a decreased level of phosphorylation of p70S6K1, AKT (S473), JNK, and p38. Increased the levels of both cleaved PARP and cleaved caspase 3 and diminished bcl-2 and MCL1. Induced of G0-G1 arrest. Effectively inhibited tumor growth of T315I-Bcr-Abl-Ba/F3 cells in mice at low doses (10 mg/kg). Oral bioavailability (36%), C max (3616 nM), T 1/2 (3.2 h). |
| in vivo study | GNF-7 (10-20 mg/kg; o.p.; daily; for 7 days) displays significant in vivo efficacy against T315I Bcr-Abl in the bioluminescent xenograft mouse model. GNF-7 exhibits moderate oral bioavailability (mice 36%) and C max (mice 3616 nM) following oral administration (mice 20 mg/kg). GNF-7 exhibits terminal elimination half-lives (mice 3.8 h) due to high plasma clearance (8.6 mL/min/kg) following intravenous injection (mice 5 mg/kg). Animal Model: 6-8 weeks old SCID beige female mice, with Ba/F3-T315I-Bcr-Abl cells xenograft Dosage: 10 mg/kg, 20 mg/kg Administration: Oral administration, daily, for 7 days Result: Effectively inhibited tumour growth of T315I-Bcr-Abl-Ba/F3 cells in mice at low doses (10 mg/kg). Animal Model: 5-6 weeks old male balb/c mice (20-25g) Dosage: 5 mg/kg for I. v.; 20 mg/kg for I. g. (Pharmacokinetic Analysis) Administration: Intravenous injection and oral gavage result: oral bioavailability (36%), C max (3616 nM), T 1/2 (3.2 h). |
| Animal Model: | 6-8 weeks old SCID beige female mice, with Ba/F3-T315I-Bcr-Abl cells xenograft 5-6 weeks old male Balb/c mice (20-25 g) |
| Dosage: | 10 mg/kg, 20 mg/kg 5 mg/kg for I .v.; 20 mg/kg for I .g. (Pharmacokinetic Analysis) |
| Administration: | Oral administration, daily, for 7 days Intravenous injection and oral gavage |
Last Update：2024-04-09 21:04:16
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Product Name: BenzaMide, N-[3-[1,4-dihydro-1-Methyl-7-[(6-Methyl-3-pyridinyl)aMino]-2-oxopyriMido[4,5-d]pyriMidin-3(2H)-yl]-4-Methylphenyl]-3-(trifluoroMethyl)- Visit Supplier Webpage Request for quotation
CAS: 839706-07-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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CAS: 839706-07-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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