CG-806

Modify Date: 2024-01-09 11:53:27

CG-806 Structure
CG-806 structure
Common Name CG-806
CAS Number 1370466-81-1 Molecular Weight 509.455
Density 1.5±0.1 g/cm3 Boiling Point 686.2±55.0 °C at 760 mmHg
Molecular Formula C26H19F4N5O2 Melting Point N/A
MSDS N/A Flash Point 368.8±31.5 °C

 Use of CG-806


CG-806 is a pan FLT3/BTK Multi-Kinase inhibitor.

 Names

Name CG-806
Synonym More Synonyms

 CG-806 Biological Activity

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

[1]. Weiguo Zhang, et al. CG0806, a First-in-Class FLT3/BTK Inhibitor, Exerts Superior Potency against AML Cells Harboring ITD, TKD and Gatekeeper Mutated FLT3 or Wild-Type FLT3.

 Chemical & Physical Properties

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℃

 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
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Price: ¥7285/10 mM * 1 mL in DMSO

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