Gilteritinib hemifumarate
- Product Name
- Gilteritinib hemifumarate
- CAS No.
- 1254053-84-3
- Chemical Name
- Gilteritinib hemifumarate
- Synonyms
- Gilteritinib fumarate;ASP 2215 hemifumarate;Gilteritinib hemifumarate;UJOUWHLYTQFUCU-WXXKFALUSA-N;6-Ethyl-3-((3-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)-5-((tetrahydro-2H-pyran-4-yl)amino)pyrazine-2-carboxamide hemifumarate;2-Pyrazinecarboxamide, 6-ethyl-3-[[3-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-5-[(tetrahydro-2H-pyran-4-yl)amino]-, (2E)-2-butenedioate (2:1);6-Ethyl-3-((3-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)-5-((tetrahydro-2H-pyran-4-yl)amino)pyrazine-2-carboxamide hemifumarate , Gilteritinib hemifumarate
- CBNumber
- CB53038520
- Molecular Formula
- C33H48N8O7
- Formula Weight
- 668.8
- MOL File
- 1254053-84-3.mol
Gilteritinib hemifumarate Property
- storage temp.
- Store at -20°C
- solubility
- Water: 2 mg/mL (3.27 mM); DMSO: 1.74 mg/mL (2.85 mM and warming)
- form
- Solid
- color
- White to yellow
- InChIKey
- RXDWJNODTRVCER-WLHGVMLRSA-N
- SMILES
- C(/C(=O)O)=C\C(=O)O.N(C1C=CC(N2CCC(N3CCN(C)CC3)CC2)=C(OC)C=1)C1=NC(NC2CCOCC2)=C(CC)N=C1C(=O)N
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-0011363
- Product name
- Gilteritinibhemifumarate
- Purity
- 99.75%
- Packaging
- 5mg
- Price
- $100
- Updated
- 2021/12/16
- Product number
- CS-0011363
- Product name
- Gilteritinibhemifumarate
- Purity
- 99.75%
- Packaging
- 10mg
- Price
- $150
- Updated
- 2021/12/16
- Product number
- CS-0011363
- Product name
- Gilteritinibhemifumarate
- Purity
- 99.75%
- Packaging
- 50mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CS-0011363
- Product name
- Gilteritinibhemifumarate
- Purity
- 99.75%
- Packaging
- 100mg
- Price
- $550
- Updated
- 2021/12/16
Gilteritinib hemifumarate Chemical Properties,Usage,Production
Uses
Gilteritinib (ASP2215) hemifumarate is a potent and ATP-competitive FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively.
Mechanism of action
Gilteritinib hemifumarate, also known as ASP2215, is a potent FLT3/AXL inhibitor, which showed potent antileukemic activity against AML with either or both FLT3-ITD and FLT3-D835 mutations. In invitro, among the 78 tyrosine kinases tested, ASP2215 inhibited FLT3, LTK, ALK, and AXL kinases by over 50% at 1 nM with an IC50 value of 0.29 nM for FLT3, approximately 800-fold more potent than for c-KIT, the inhibition of which is linked to a potential risk of myelosuppression. ASP2215 inhibited the growth of MV4-11 cells, which harbor FLT3-ITD, with an IC50 value of 0.92 nM, accompanied with inhibition of pFLT3, pAKT, pSTAT5, pERK, and pS6. ASP2215 decreased tumor burden in bone marrow and prolonged the survival of mice intravenously transplanted with MV4-11 cells. ASP2215 may have potential use in treating AML.
in vivo
In MV4-11 xenografted-mice, the concentration of Gilteritinib (ASP2215) in tumors is more than 20-fold higher than that in plasma with oral administration of Gilteritinib at 10 mg/kg for 4 days. Treatment of Gilteritinib for 28 days results in dose-dependent inhibition of MV4-11 tumor growth and induces complete tumor regression at more than 6 mg/kg. Further, Gilteritinib decreases tumor burden in bone marrow and prolonged the survival of mice intravenously transplanted with MV4-11 cells[1].
IC 50
Axl
References
[1] ASP2215, a novel FLT3/AXL inhibitor: Preclinical evaluation in acute myeloid leukemia (AML). 2014 ASCO Annual Meeting.
[2] Mori M, et al. Gilteritinib, a FLT3/AXL inhibitor, shows antileukemic activity in mouse models of FLT3 mutated acute myeloid leukemia. Invest New Drugs. 2017 Oct;35(5):556-565. DOI:10.1007/s10637-017-0470-z
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View Lastest Price from Gilteritinib hemifumarate manufacturers
- Product
- Gilteritinib hemifumarate 1254053-84-3
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- More Than 99%
- Supply Ability
- 100kg/Month
- Release date
- 2024-07-03