1. Protein Tyrosine Kinase/RTK
  2. Btk
    FLT3

CG-806 

Cat. No.: HY-112646 Purity: 98.02%
Handling Instructions

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

For research use only. We do not sell to patients.

CG-806 Chemical Structure

CG-806 Chemical Structure

CAS No. : 1370466-81-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 729 In-stock
Estimated Time of Arrival: December 31
5 mg USD 650 In-stock
Estimated Time of Arrival: December 31
10 mg USD 950 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1950 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2950 In-stock
Estimated Time of Arrival: December 31
100 mg USD 4400 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & 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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9629 mL 9.8145 mL 19.6290 mL
5 mM 0.3926 mL 1.9629 mL 3.9258 mL
10 mM 0.1963 mL 0.9815 mL 1.9629 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

509.45

Formula

C₂₆H₁₉F₄N₅O₂

CAS No.

1370466-81-1

SMILES

O=C(NC1=CC=CC(C(F)(F)F)=C1)NC2=CC=C(C3=CC=C(C4=NC=C(C)N4)C5=C3CNC5=O)C(F)=C2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
CG-806
Cat. No.:
HY-112646
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CG-806

Cat. No.: HY-112646