(S)-1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)-1H-1,2,4-triazole-3,5-diamine
1-(6,7-Dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-[(7S)-6,7,8,9-tetrahydro-7-(1-pyrrolidinyl)-5H-benzocyclohepten-2-yl]-1H-1,2,4-triazole-3,5-diamine
CAS: 1037624-75-1
Molecular Formula: C30H34N8
(S)-1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)-1H-1,2,4-triazole-3,5-diamine - Names and Identifiers
(S)-1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)-1H-1,2,4-triazole-3,5-diamine - Physico-chemical Properties
| Molecular Formula | C30H34N8 |
| Molar Mass | 506.64 |
| Density | 1.41±0.1 g/cm3(Predicted) |
| Melting Point | >211°C (dec.) |
| Boling Point | 799.6±70.0 °C(Predicted) |
| Solubility | Soluble in DMSO (up to at least 25 mg/ml) |
| Appearance | Form Yellow powder, color Yellow |
| Color | Yellow |
| pKa | 10.34±0.20(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| Physical and Chemical Properties | Bioactive Bemcentinib (R428, BGB324) is an Axl inhibitor with IC50 of 14 nM. The selectivity for Axl is more than 100 times higher than for Abl. The selectivity of Axl is also higher than that of Mer and Tyro3 (50 to 100 times higher) and InsR, EGFR, HER2, and PDGFRβ (100 times higher). |
| Use | Use R428 is an AXL tyrosine kinase inhibitor and is considered an anticancer drug. |
| In vitro study | R428 blocks the catalytic and cancer-promoting activity of Axl. Nanomolar R428 inhibits Axl activity and blocks Axl-dependent processes including Akt phosphorylation, breast cancer cell invasion, and pro-inflammatory cytokine production. A recent study showed that the Axl inhibitor R428 on primary CLL B cells after 24 hours of treatment, the average IC50 is about 2.0 μm, while the normal B cells under similar conditions, T cells and natural killer cells (NK) there was no significant cell death at the concentration of R428 (2.5 μm). |
| In vivo study | Pharmacological studies have shown that oral R428 treatment can reduce the expression of macrophage colony stimulating factor and transcriptional regulator Snail of epithelial mesenchymal transition in tumor, which is dose dependent. R428 inhibits angiogenesis in corneal microcapsules and tumor models, supporting a previous study. In MDA-MB-231 intracardiac and 4T1 orthotopic breast cancer metastasis mouse models, R428 treatment reduced the metastatic burden of cancer cells and prolonged survival (median survival greater than 80 days compared to 52 days in the control group, P<0.05). |
(S)-1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)-1H-1,2,4-triazole-3,5-diamine - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.974 ml | 9.869 ml | 19.738 ml |
| 5 mM | 0.395 ml | 1.974 ml | 3.948 ml |
| 10 mM | 0.197 ml | 0.987 ml | 1.974 ml |
| 5 mM | 0.039 ml | 0.197 ml | 0.395 ml |
Last Update：2024-01-02 23:10:35
(S)-1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)-1H-1,2,4-triazole-3,5-diamine - Reference Information
| introduction | R428 (BGB324) is an Axl inhibitor with IC50 of 14nM, which is more than 100 times more selective on Axl than on Abl. The selectivity of Axl is also higher than that of Mer and Tyro3 (50 to 100 times higher) and InsR, EGFR, HER2 and PDGFRβ (more than 100 times higher). |
| In vivo studies | Pharmacological studies have shown that oral R428 treatment can reduce the expression of macrophage colony stimulating factor and epithelial-mesenchymal transition transcription regulator Snail in tumors. This effect has dose-dependent properties. R428 inhibits angiogenesis in corneal microcapsules and tumor models, which supports a previous study. In MDA-MB-231 intracardiac and 4T1 orthotopic mouse models of breast cancer metastasis, R428 treatment can reduce the burden of cancer cell metastasis and prolong survival (median survival is greater than 80 days compared with 52 days in the control group, P<0.05). |
| use | R428 is an AXL tyrosine kinase inhibitor, which is considered an anti-cancer drug. |
| biological activity | Bemcentinib (R428, BGB324) is an Axl inhibitor with IC50 of 14 nM, which is more than 100 times more selective on Axl than on Abl. The selectivity of Axl is also higher than that of Mer and Tyro3 (50 to 100 times higher) and InsR, EGFR, HER2, and PDGFRβ (100 times higher). |
| target | TargetValue axl (cell-free say) 14 nM |
| Target | Value |
| Axl (Cell-free assay) | 14 nM |
| in vitro study | R428 blocks the catalytic and cancer-promoting activities of Axl. The nanomolar R428 inhibits Axl activity and blocks Axl-dependent processes, including Akt phosphorylation, breast cancer cell invasion, and proinflammatory cytokine production. A recent study showed that Axl inhibitor R428 had an average IC50 of about 2.0 μM after 24 hours of treatment of primary CLL B cells, while normal B cells, T cells and natural killer cells (NK) had no obvious cell death at R428 (2.5 μM) concentration under similar conditions. |
Last Update：2024-04-10 22:29:15
(S)-1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)-1H-1,2,4-triazole-3,5-diamine - Nature
| Solubility | Soluble in DMSO (up to at least 25 mg/ml) |
Last Update：2024-04-10 22:29:15
(S)-1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)-1H-1,2,4-triazole-3,5-diamine - Uses and synthesis methods
Introduction
R428 (BGB324) is an Axl inhibitor with an IC50 of 14nM. The selectivity for Axl is more than 100 times higher than for Abl. The selectivity of Axl is also higher than that of Mer and Tyro3 (50 to 100 times higher) and InsR, EGFR, HER2 and PDGFRβ (more than 100 times higher).
In vivo studies
Pharmacological studies have shown that oral R428 treatment can reduce the expression of macrophage colony-stimulating factor and the transcription regulator Snail of epithelial-mesenchymal transition in tumors. This effect has dose-dependent properties. R428 inhibits angiogenesis in corneal microcapsules and tumor models, which supports a previous study. In MDA-MB-231 intracardial and 4T1 orthotopic mouse models of breast cancer metastasis, R428 treatment can reduce the burden of cancer metastasis and prolong survival (median survival is greater than 80 days compared with 52 days in the control group, P<0.05).
Target
Target Value
Axl
(Cell-free assay) 14 nM
in vitro studies
R428 blocks the catalytic and cancer-promoting activity of Axl. The nanomolar R428 inhibits Axl activity and blocks Axl-dependent processes, including Akt phosphorylation, breast cancer cell invasion, and proinflammatory cytokine production. A recent study showed that Axl inhibitor R428 had an average IC50 of about 2.0 μM after 24 hours of treatment of primary CLL B cells, while normal B cells, T cells and natural killer cells (NK) had no obvious cell death at R428 (2.5 μM) concentration under similar conditions.
Last Update：2024-04-09 21:54:55
![(S)-1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)-1H-1,2,4-triazole-3,5-diamine](http://res.chembk.com/assets/images/structure/300378.gif)
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Spot supply
Product Name: R428 (BGB324) Visit Supplier Webpage Request for quotationCAS: 1037624-75-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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