- Shanghai Nianxing Industrial Co., Ltd
- China
- Product Name: CG-806
- Price:
- Purity: 98.0%
- Stocking Period: 10 Day
- Contact: Huang
- DC Chemicals Limited
- China
- Product Name: CG-806
- Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
- Purity: 98.0%
- Stocking Period: 3 Day
- Contact: Tony Cao
- ShangHai DC Chemicals Co.,Ltd
- China
- Product Name: CG-806
- Price: ￥Inquiry/1g
- Purity: 98.9%
- Stocking Period: 1 Day
- Contact: Tony Lai
1370466-81-1
1370466-81-1 structure
- Name: CG-806
- Chemical Name: CG-806
- CAS Number: 1370466-81-1
- Molecular Formula: C26H19F4N5O2
- Molecular Weight: 509.455
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Btk
- Create Date: 2018-11-18 15:40:26
- Modify Date: 2024-01-09 11:53:27
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CG-806 is a pan FLT3/BTK Multi-Kinase inhibitor.
| Name | CG-806 |
|---|---|
| Synonyms |
1-{3-Fluoro-4-[7-(4-methyl-1H-imidazol-2-yl)-1-oxo-2,3-dihydro-1H-isoindol-4-yl]phenyl}-3-[3-(trifluoromethyl)phenyl]urea
Urea, N-[4-[2,3-dihydro-7-(4-methyl-1H-imidazol-2-yl)-1-oxo-1H-isoindol-4-yl]-3-fluorophenyl]-N'-[3-(trifluoromethyl)phenyl]- Cg-026806 |
| Description | CG-806 is a pan FLT3/BTK Multi-Kinase inhibitor. |
|---|---|
| Related Catalog | |
| Target |
FLT3/BTK[1]. |
| In Vitro | CG-806 (CG'806) is a small molecule multi-kinase inhibitor against FLT3 and BTK kinases that is under development to treat FLT3-driven AML. CG-806 exerts potent picomolar IC50 anti-proliferative activity against human AML cells and against Ba/F3 mouse AML cells with FLT3-ITD mutations (about 50 to 250-fold higher activity compared to quizartinib or gilteritinib). Specifically, compared to second-generation FLT3 inhibitors quizartinib or gilteritinib, CG-806 shows much more pronounced anti-proliferative effects in leukemia cells with D835 mutations, the ITD plus F691L/Y842D/D835 mutations, or in FLT3 wild-type cells (IC50s are 0.17, 0.82, 9.49, 0.30, 8.26, 9.72, and 0.43 nM for human ITD-mutated AML cells MV4-11, MOLM13, murine ITD mutated leukemia cells Ba/F3 WT, Ba/F3-ITD, Ba/F3-D835Y, Ba/FLT3-ITD+D835Y, and “gatekeeper” mutation Ba/F3-ITD+F691L cells, respectively). Furthermore, CG-8066 triggers profound apoptosis in cell lines. Mechanistically, CG-806 profoundly suppresses FLT3 and its downstream MAPK/AKT signaling, as well as phospho-Aurora, and/or phospho-BTK proteins, suggesting the ability of CG-806 to inhibit various kinases that function in AML signaling and appear to contribute to its effectiveness[1]. |
| In Vivo | CG-806 demonstrates in vivo tumor eradication without toxicity when administered orally, once daily for 14 d as a single agent in the MV4:11 AML murine xenograft model, and demonstrates sustained micromolar plasma drug levels in mice after a single oral administration. CG-806 can be considered not only a pan-FLT3 inhibitor for targeting FLT3 wild type and ITD-mutant AML, but also a one-of-a-kind agent killing leukemia cells with TKD or dual TKD plus ITD mutations, which are frequently associated with resistance/relapse in FLT3-mutant AML patients. CG-806 exerts a robust therapeutic window in animal xenograft studies. Thus, CG-806 warrants further investigation for the treatment of newly diagnosed and relapsed/refractory patients with FLT3-mutated AML[1]. |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Boiling Point | 686.2±55.0 °C at 760 mmHg |
| Molecular Formula | C26H19F4N5O2 |
| Molecular Weight | 509.455 |
| Flash Point | 368.8±31.5 °C |
| Exact Mass | 509.147491 |
| LogP | 5.30 |
| Vapour Pressure | 0.0±2.1 mmHg at 25°C |
| Index of Refraction | 1.655 |
| Storage condition | 2-8℃ |