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Cat.No.S8140
| Related Targets | EGFR VEGFR JAK PDGFR FGFR Src HIF FLT FLT3 HER2 |
|---|---|
| Other Bcr-Abl Inhibitors | Degrasyn (WP1130) Bafetinib GNF-5 Rebastinib (DCC-2036) GNF-2 Berbamine Olverembatinib (GZD824) dimesylate PD173955 Radotinib Risvodetinib |
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In vitro |
DMSO
: 20 mg/mL
(36.52 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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| Molecular Weight | 547.53 | Formula | C28H24F3N7O2 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 839706-07-9 | Download SDF | Storage of Stock Solutions |
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| Synonyms | N/A | Smiles | CC1=C(C=C(C=C1)NC(=O)C2=CC(=CC=C2)C(F)(F)F)N3CC4=CN=C(N=C4N(C3=O)C)NC5=CN=C(C=C5)C | ||
| Targets/IC50/Ki |
M351T
<5 nM
T315I
61 nM
E255V
122 nM
c-Abl
133 nM
G250E
136 nM
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|---|---|
| In vitro |
GNF-7 shows potent antiproliferative activity against wild-type and mutant Bcr-Abl Ba/F3 cells with IC50 less than 11 nM. In human colon cancer cells (Colo205 and SW620), this compound also displays excellent growth inhibitory activity with IC50 of 5 nM and 1 nM, respectively. It potently and selectively inhibits NRAS-dependent acute myelogenous leukemia and acute lymphoblastic leukemia cells through combined inhibition of ACK1/AKT and GCK.
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| In vivo |
GNF-7 exhibits excellent pharmacokinetic parameters in mice. In a bioluminescent xenograft mouse model using a transformed T315I-Bcr-Abl-Ba/F3 cell line, this compound (10 mg/kg, p.o.) effectively inhibits tumor growth. In NSG mice bearing human mutant NRAS-expressing MOLT-3-luc+ tumors, this compound (15 mg/kg, p.o.) significantly decreases disease burden, prolongs overall survival, and causes strong suppression of phospho-AKT and phospho-RPS6.
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References |
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