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CHMFL-FLT3-122

Chemical Structure : CHMFL-FLT3-122

CAS No.: 1839150-56-9

CHMFL-FLT3-122

Catalog No.: PC-24328Not For Human Use, Lab Use Only.

CHMFL-FLT3-122 is a potent, selective and orally active FLT3 kinase with IC50 of 40 nM, shows >10-fold selectivity over BTK (IC50=421 nM) and c-KIT (IC50=559 nM) kinases.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

CHMFL-FLT3-122 is a potent, selective and orally active FLT3 kinase with IC50 of 40 nM, shows >10-fold selectivity over BTK (IC50=421 nM) and c-KIT (IC50=559 nM) kinases.
CHMFL-FLT3-122 demonstrates 170-fold selectivity between FLT3 kinase and c-KIT kinase (GI50 = 11 nM versus 1900 nM) in the TEL-fusion isogenic BaF3 cells.
CHMFL-FLT3-122 induces apoptosis by arresting the cell cycle into the G0/G1 phase.
CHMFL-FLT3-122 significantly inhibits the proliferation of FLT3-ITD positive AML cancer cell lines MV4-11 (GI50 = 22 nM), MOLM13/14 (GI50 = 21 nM/42 nM).
CHMFL-FLT3-122 demonstrates a good bioavailability (30%) and significantly suppressed the tumor growth in MV4-11 cell inoculated xenograft model (50 mg/kg) without exhibiting obvious toxicity.

Physicochemical Properties

M.Wt 471.57
Formula C26H29N7O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-(dimethylamino)-ethanone

References

1. Li X, et al. J Med Chem. 2015 Dec 24;58(24):9625-38.

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