Home Angiogenesis FLT3 inhibitor SKLB4771 (FLT3-IN-1)

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SKLB4771 (FLT3-IN-1) FLT3 inhibitor

Cat.No.S1099

SKLB4771 (FLT3-IN-1) is a potent and selective inhibitor of human receptor-type tyrosine-protein kinase FLT3 with an IC50 of 10 nM.
SKLB4771 (FLT3-IN-1) FLT3 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 537.66

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S109901 DMSO]50 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.10%
99.10

Chemical Information, Storage & Stability

Molecular Weight 537.66 Formula

C25H27N7O3S2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1370256-78-2 -- Storage of Stock Solutions

Synonyms N/A Smiles CC1=CC=C(C=C1)NC(=O)NC2=NN=C(S2)SC3=NC=NC4=C3C=CC(=C4)OCCCN5CCOCC5

Solubility

In vitro
Batch:

DMSO : 50 mg/mL ( (92.99 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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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.

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Mechanism of Action

Targets/IC50/Ki
FLT3 [1]
(Cell-free assay)
10 nM
In vitro

SKLB4771 (FLT3-IN-1) just weakly inhibits Aurora A, FMS, FLT4, and c-Kit (IC50s: 1.5 μM, 2.8 μM, 3.7 μM, and 6.8 μM, respectively). It displays almost no inhibitory activity against the other 13 selected protein kinases. This compound potently inhibits the growth of MV4-11 cells that express FLT3-ITD, with an IC50 value of 0.006 μM. It just exhibits very weak inhibitory activity against human T lymphoma Jurkat cells, human Burkitt’s lymphoma Ramos cells, human lung cancer PC-9 and H292 cells, and human epithelial carcinoma A431 cells (IC50: 3.05 μM, 6.25 μM, 3.72 μM, 6.94 μM, and 8.91 μM, respectively).[1].
In vivo

In the MV4-11 xenograft model, treatment with SKLB4771 (FLT3-IN-1) at 100 mg/kg/d results in rapid and complete tumor regression in all mice of this group. At doses of 20 mg/kg/d and 40 mg/kg/d, it significantly slows down tumor growth, with inhibition rates of 66% and 84%, respectively. Throughout the experiment, no significant weight loss or other obvious signs of toxicity were observed in any of the treated mice. Tumor tissues from groups receiving this compound showed significantly fewer Ki67 (tumor mitotic index)-positive cells. TUNEL data indicated a time-dependent increase in the percentage of apoptotic cells.[1]
References

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