1. Protein Tyrosine Kinase/RTK
  2. FLT3
    Btk
  3. CG-806

CG-806 

Cat. No.: HY-112646 Purity: 98.07%
Handling Instructions

CG-806 is an orally active, potent and non-covalent pan-FLT3/pan-BTK inhibitor with an IC50 of 0.08 µM for FLT3. CG-806 has an IC50 of 11 nM against FLT3 wild type (WT)-transfected Ba/F3 cells.

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
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
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

CG-806 is an orally active, potent and non-covalent pan-FLT3/pan-BTK inhibitor with an IC50 of 0.08 µM for FLT3[1][2]. CG-806 has an IC50 of 11 nM against FLT3 wild type (WT)-transfected Ba/F3 cells[3].

IC50 & Target

FLT3/BTK[1].

In Vitro

In FLT3-ITD AML cells, CG-806 induces apoptosis through inhibition of FLT3 signaling (decreases phospho-FLT3, -STAT5 and -ERK) and promotion of G0/G1 cell cycle arrest. In FLT3-WT AML cell lines, or Ba/F3 cells transfected with FLT3-WT, D835Y, ITD+D835Y, or ITD+F691L, CG-806 markedly decreases phosphorylation of BTK, aurora kinases (AURK) and H3S10, resulting in G2/M arrest or polyploidy, and apoptosis with less or no effect on FLT3-WT activity. CG-806 decreases BTK phosphorylation in all malignant B cell lines tested and inhibits cell proliferation and colony formation.CG-806 equivalently inhibits BTK-WT and BTK-C481S in HEK293 transfected cells[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

CG-806 (0-120 mg/kg; oral administration; for 28 days; CD-1 mice) treatment suppresses leukemia growth at all doses tested throughout the 28-day period of dosing, and has no adverse CG-806-related effects on body weight, ophthalmic, respiratory or neurological examinations, clinical pathology (coagulation, clinical chemistry, or urinalysis), organ weight or macroscopic evaluations in the subcutaneous MV4-11 xenograft model[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CD-1 mice with MV4-11[1]
Dosage: 0 mg/kg, 30 mg/kg, 60 mg/kg or 120 mg/kg
Administration: Oral administration; for 28 days
Result: Suppressed leukemia growth at all doses tested throughout the 28-day period of dosing.
Clinical Trial
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 7.2 mg/mL (14.13 mM; Need ultrasonic)

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

Purity: 98.07%

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Keywords:

CG-806CG806CG 806FLT3BtkCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Bruton tyrosine kinaseInhibitorinhibitorinhibit

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