Description
JAK2/FLT3-IN-1 (TFA) is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 (TFA) has anti-cancer activity.
Product information
CAS Number: 2928093-29-0
Molecular Weight: 581.61
Formula: C27H35F4N7O3
Chemical Name: 2-({1-[2-fluoro-4-({5-methyl-4-[1-(propan-2-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl}amino)phenyl]piperidin-4-yl}(methyl)amino)ethan-1-ol; trifluoroacetic acid
Smiles: CN(CCO)C1CCN(CC1)C1=CC=C(C=C1F)NC1=NC(C2C=NN(C=2)C(C)C)=C(C)C=N1.OC(=O)C(F)(F)F
InChiKey: WIIIAEPAIQXSFK-UHFFFAOYSA-N
InChi: InChI=1S/C25H34FN7O.C2HF3O2/c1-17(2)33-16-19(15-28-33)24-18(3)14-27-25(30-24)29-20-5-6-23(22(26)13-20)32-9-7-21(8-10-32)31(4)11-12-34;3-2(4,5)1(6)7/h5-6,13-17,21,34H,7-12H2,1-4H3,(H,27,29,30);(H,6,7)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
JAK2/FLT3-IN-1 (0.008-1 μM; for 2 hours) (TFA) down-regulates p-FLT3 in a dose-dependent manner. JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) (TFA) has a dose-dependent effect on the induction of apoptosis in the MV4-11 cells. JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) (TFA) strongly induces cell cycle arrest with a G1/G0 percentage of 85% at 100 nM in the MV4-11 cells.
In Vivo:
JAK2/FLT3-IN-1 (30 and 60 mg/kg/day; p.o.; for 14 days) (TFA) exhibits significant antitumor effects.
Products are for research use only. Not for human use.
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