Home Protein Tyrosine Kinase FLT3 inhibitor - Axl inhibitor Gilteritinib (ASP2215)

Gilteritinib (ASP2215)

Catalog No.S7754

For research use only.

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 (ASP2215) Chemical Structure

CAS No. 1254053-43-4

Selleck's Gilteritinib (ASP2215) has been cited by 16 publications

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Biological Activity

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).
Targets
FLT3 [1]
(Cell-free assay)		 Axl [1]
(Cell-free assay)
0.29 nM 0.73 nM
In vitro

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)[1]. 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[2].
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MV4-11 cells MkSzR4VtdCCleXPs[UBie3OjeR?= MUixMEA{NCBzMDygZY5lKDNyIH7N NUXQ[FRMOjRiaB?= M2XCUXRp\SCvZXHuJJBzd3CxcoTpc44hd2ZiTW[0MVEyKGOnbHzzJIlvKEdzIIDoZZNmKHencnWgd4lodmmoaXPhcpRtgSCrbnPy[YF{\WRiYYSg[4ltfGW{aYTpcoljKGOxbnPlcpRz[XSrb37zJI9nKDNiKE[5MlAmQyCSPECuNFEqKGGwZDCxNEBvVSBqN{CuO{U8KFB:MD6wNFEqNg>? MnjNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzFyNkmwNVUoRjNzME[5NFE2RC:jPh?=
MOLM-13 cells NW\tRYxKSXCxcITvd4l{KGG|c3H5 M3u2fFEtKDNuIEGwMEA{OCxiYX7kJFExOCCwTR?= MoPUOFghcA>? NF3EdXZ{cWewaX\pZ4FvfCCrbnPy[YF{\XNiaX6geIhmKHCncnPlcpRi\2Vib3[gZY5v\XirbjDWMZBwe2m2aY\lJINmdGy|IHH0JINwdmOnboTyZZRqd26|IH;mJFMxKG6PIDizNk4xLSliYX7kJFExOCCwTTCoOVIvPCVrII\ldpN2eyClb370do9tKCh2LkGlLS=> NIPZe4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUC2PVAyPSd-M{GwOlkxOTV:L3G+
32D/TKD cells NWrFV3dnTnWwY4Tpc44h[XO|YYm= MnvLOVAhdk4EoB?= Mk\rOkBp MVXJcohq[mm2b36gc4YhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBb5Qhd25iVEOwPC=> M{DudVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUC3OlYxLz5{OUWwO|Y3ODxxYU6=
TF-1 cells MVHGeY5kfGmxbjDhd5NigQ>? NGP2XG0xNCB{MDygPFAtKDJyMDDhcoQhPTByIH7N NIjpdZYyKGh? NGX0fIhocWy2ZYLpeIlvcWJiaHHzJIFvKEmFNUCgZYdicW6|dDD3bYxlNXS7cHWgZ{1McXRib3[gNVAzKG6P NUK0XJdtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5NFg5QDFpPkK3PVA5QDhzPD;hQi=>
BA/F3 M3[xXGZ2dmO2aX;uJIF{e2G7 M4mybWlvcGmkaYTpc44hSXO|YYm6JGEhemWlb33ibY5idnRicnX0do93cXK3czD3ZZMh[3KnYYTl[EBnem:vIHX4dJJme3Orb36gdIxie22rZDDGUGFINUWPTEStRWxMfjFxcF3YMYlz\XOFREigbY4hf2irY3igZ2RPSSCob4KgSW1NSS2DTFug[pV{cW:wIIDyc5RmcW5idkGge4F{KGmwdHXndoF1\WRuIHHu[EBqdmqnY4Tl[EBqdnSxIH3veZNmKGy7bYDoc4llKGOnbHygcIlv\SCEQT;GN{Bk\Wyucz6gWZNqdmdiYTDtZYdv\XSrYzDi[YFlKHKnYXflcpQh\ixiSVO1NEA:KDBwMECxOUDPxE1w NUjjNItqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzNyMU[yNk8oRkOqRV3CUFww[T5?
BA/F3 M13sfGZ2dmO2aX;uJIF{e2G7 M1fDT2lvcGmkaYTpc44hSXO|YYm6JGEhemWlb33ibY5idnRicnX0do93cXK3czD3ZZMh[3KnYYTl[EBnem:vIHX4dJJme3Orb36gdIxie22rZDDGUGFINUWPTEStRWxMfjFxcF3YMYlz\XOFREigbY4hf2irY3igZ2RPSSCob4KgSW1NSS2DTFug[pV{cW:wIIDyc5RmcW5idkGge4F{KGmwdHXndoF1\WRuIHHu[EBqdmqnY4Tl[EBqdnSxIH3veZNmKGy7bYDoc4llKGOnbHygcIlv\SCEQT;GN{Bk\Wyucz6gWZNqdmdiYTDtZYdv\XSrYzDi[YFlKHKnYXflcpQh\ixiSVO1NEA:KDBwMECxOUDPxE1w MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyzN|AyPjJ{Lze+R4hGVUKOPD;hQi=>
Vero NWDqeJNCSW62aY\pdoFtKGG|c3H5 M17YVVI1KGi{ MXvBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDTRXJUNUOxVj2yJEh3cXKjbDD0bZRmeilibXXhd5Vz\WRiYomgdIxieXWnIHHzd4F6KGmwIG\ldo8h[2WubIOgZZQhVU:LIECuNFEzPSCjZoTldkAzPCCqcjygTWM2OCB;IE[uO|Yh|ryPLh?= Mnz5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|MxOTZ{Mj:nQmNpTU2ETEyvZV4>
Vero NGXyS4tE\WyuII\pZYJqdGm2eTDhd5NigQ>? MUi3NkBpeg>? NIfQd4RE\WyuII\pZYJqdGm2eTDt[YF{fXKnZDDifUBE\WyuVHn0[ZIuT2yxIHHzd4F6KGmwIG\ldo8h[2WubIOgZZQhVU:LIECuNFUh[W[2ZYKgO|JpeixiQ1O1NEA:KDN5LkG2JO69VS5? NEm5PYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{OzBzNkKyM{c,S2iHTVLMQE9iRg>?
Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot p-STAT5 / STAT5 / p-AKT / AKT / p-ERK / ERK ; p-c-kit / c-kit ; p-FLT3(Y591) / FLT3 28516360 27908881 30344940
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[1].

Protocol (from reference)

Cell Research:

[1]
  • Cell lines: MV4-11 cells
  • Concentrations: 0.1 nM, 1 nM, and 10 nM
  • Incubation Time: 2 h
  • Method:

    MV4-11 cells are treated with DMSO or increasing concentrations of gilteritinib for 2 hours. Immunoprecipitation and immunoblot for phosphorylated FLT3 and total FLT3 are performed.

  • (Only for Reference)
Animal Research:

[1]
  • Animal Models: MV4-11 xenografted mice (Nude mice)
  • Dosages: 1 mg/kg, 6 mg/kg, and 10 mg/kg
  • Administration: oral
  • (Only for Reference)

Solubility (25°C)

In vitro

 DMSO 100 mg/mL
(180.92 mM)
Water Insoluble
Ethanol '85 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 552.71
Formula

C29H44N8O3
CAS No. 1254053-43-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC1=C(N=C(C(=N1)C(=O)N)NC2=CC(=C(C=C2)N3CCC(CC3)N4CCN(CC4)C)OC)NC5CCOCC5

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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04699877 Recruiting Drug: Gilteritinib Renal Impaired|Gilteritinib|Normal Renal Function|Pharmacokinetics of ASP2215 Astellas Pharma Global Development Inc.|Astellas Pharma Inc January 28 2021 Phase 1
NCT04140487 Recruiting Drug: Azacitidine|Drug: Gilteritinib|Drug: Venetoclax Recurrent Acute Myeloid Leukemia|Recurrent Chronic Myelomonocytic Leukemia|Recurrent Myelodysplastic/Myeloproliferative Neoplasm|Refractory Acute Myeloid Leukemia|Refractory Chronic Myelomonocytic Leukemia|Refractory Myelodysplastic/Myeloproliferative Neoplasm M.D. Anderson Cancer Center December 17 2019 Phase 1|Phase 2
NCT03730012 Completed 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

(data from https://clinicaltrials.gov, updated on 2021-09-06)

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