Flumatinib

Research use only, not for human use.

Flumatinib is an orally bioavailable tyrosine kinase inhibitor flumatinib, with potential antineoplastic activity.

Flumatinib is an orally bioavailable tyrosine kinase inhibitor flumatinib, with potential antineoplastic activity.(In Vitro):Flumatinib (HH-GV-678) can predominantly inhibit the autophosphorylation of Bcr-Abl in K562 cell. In higher concentration, Flumatinib can inhibit the phosphorylation of c-Kit in Mo7e cell and the phosphorylation of PDGFR in Swiss3T3 cell, however, Flumatinib has no or little effect on other tyrosine kinase including EGFR, KDR, c-Src and HER2 . Flumatinib (HHGV678) effectively overcame the drug resistance of certain KIT mutants with activation loop mutations (i.e., D820G, N822K, Y823D, and A829P) .

Flumatinib (HH-GV-678) can predominantly inhibit the autophosphorylation of Bcr-Abl in K562 cell. In higher concentration, Flumatinib can inhibit the phosphorylation of c-Kit in Mo7e cell and the phosphorylation of PDGFR in Swiss3T3 cell, however, Flumatinib has no or little effect on other tyrosine kinase including EGFR, KDR, c-Src and HER2 . Flumatinib (HHGV678) effectively overcame the drug resistance of certain KIT mutants with activation loop mutations (i.e., D820G, N822K, Y823D, and A829P) .

——

HHGV678

GPCR/G Protein

cAMP

c-Abl|PDGFRβ|c-Kit|

Cancer

——

895519-90-1

562.6

C29H29F3N8O

>98% (HPLC)

DMSO : ≥ 32 mg/mL; 56.88 mM

CC1=C(C=C(C=N1)NC(=O)C2=CC(=C(C=C2)CN3CCN(CC3)C)C(F)(F)F)NC4=NC=CC(=N4)C5=CN=CC=C5

——

(-20℃)

With Ice Pack

≥ 2 years