Molecular Weight(MW): 552.71
Gilteritinib(ASP2215) is a small-molecule FLT3/AXL inhibitor with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL, respectively. It inhibits FLT3 at an IC50 value that was approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM).
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|Description||Gilteritinib(ASP2215) is a small-molecule FLT3/AXL inhibitor with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL, respectively. It inhibits FLT3 at an IC50 value that was approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM).|
Gilteritinib demonstrates potent inhibitory activity against the internal tandem duplication (FLT3-ITD) and FLT3-D835Y point mutations in cellular assays using MV4-11 and MOLM-13 cells as well as Ba/F3 cells expressing mutated FLT3. Gilteritinib decreases the phosphorylation levels of FLT3 and its downstream targets in both cellular and animal models. Gilteritinib inhibits the activity of eight of the 78 tested kinases by over 50% at concentrations of either 1 nM (FLT3, LTK, ALK, and AXL) or 5 nM (TRKA, ROS, RET, and MER). Gilteritinib treatment for 48h results in an induction of apoptosis in MV4-11 cells as determined by an increase in annexin V-positive cells. Gilteritinib also decreases the expression of anti-apoptotic proteins such as MCL-1, BCL2L10, and survivin, which are reported to be important in chemotherapy sensitivity, following 24h treatment.
|In vivo||In vivo, gilteritinib is distributed at high levels in xenografted tumors after oral administration. The decreased FLT3 activity and high intratumor distribution of gilteritinib translates to tumor regression and improved survival in xenograft and intra-bone marrow transplantation models of FLT3-driven AML. This antitumor activity is associated with a durable inhibition of phospho-FLT3 and phospho-STAT5. Furthermore, treatment with gilteritinib decreases the leukemic burden and prolongs survival in a mouse IBMT model. No overt toxicity is seen in mouse models treated with gilteritinib.|
|In vitro||DMSO||100 mg/mL (180.92 mM)|
|Ethanol||85 mg/mL (153.78 mM)|
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Molecular Weight Calculator
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03730012||Recruiting||Drug: gilteritinib|Drug: atezolizumab||Acute Myeloid Leukemia (AML)|Acute Myeloid Leukemia With FMS-like Tyrosine Kinase (FLT3) Mutation||Astellas Pharma Global Development Inc.|Astellas Pharma Inc||June 19 2019||Phase 1|Phase 2|
|NCT03964038||Completed||Drug: gilteritinib|Drug: gilteritinib mini tablet||Healthy Volunteer||Astellas Pharma Global Development Inc.|Astellas Pharma Inc||May 21 2019||Phase 1|
|NCT02456883||Completed||Drug: gilteritinib|Drug: 14C-labeled gilteritinib||Advanced Solid Tumors|Pharmacokinetics of 14C-labeled Gilteritinib||Astellas Pharma Global Development Inc.|Astellas Pharma Inc||March 4 2016||Phase 1|
|NCT02571816||Completed||Drug: ASP2215||Hepatic Impairment|Healthy||Astellas Pharma Global Development Inc.|Astellas Pharma Inc||October 23 2015||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
Do you have recommendations for the formulation of giltertinib (ASP-2215) in mice (for in vivo studies)?
You can use "5% DMSO+40% PEG 300+5% Tween 80+ddH2O" clear at 5mg/ml as a IP formula.