in vivo
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Gilteritinib

in vivo
Product Name
Gilteritinib
CAS No.
1254053-43-4
Chemical Name
Gilteritinib
Synonyms
Gilteritinib;CS-2849;ASP-2215;Geritinib;mobcertinib;Giliteritinib;ASP2215(Gilteritinib);Gilteritinib (ASP2215);Gilteritinib Impurity;Gilteritinib(free base)
CBNumber
CB82725626
Molecular Formula
C29H44N8O3
Formula Weight
552.71
MOL File
1254053-43-4.mol
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Gilteritinib Property

Melting point:
>157°C (dec.)
Boiling point:
696.9±55.0 °C(Predicted)
Density 
1.242±0.06 g/cm3(Predicted)
storage temp. 
-20°C
solubility 
Soluble in DMSO (25 mg/ml)
pka
14.39±0.50(Predicted)
form 
solid
color 
Off-white to pale pink
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
21503
Product name
Gilteritinib
Purity
≥98%
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
21503
Product name
Gilteritinib
Purity
≥98%
Packaging
5mg
Price
$116
Updated
2024/03/01
Cayman Chemical
Product number
21503
Product name
Gilteritinib
Purity
≥98%
Packaging
10mg
Price
$214
Updated
2024/03/01
Cayman Chemical
Product number
21503
Product name
Gilteritinib
Purity
≥98%
Packaging
25mg
Price
$381
Updated
2024/03/01
Usbiological
Product number
451193
Product name
Gilteritinib
Packaging
10mg
Price
$425
Updated
2021/12/16
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Gilteritinib Chemical Properties,Usage,Production

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

Description

Gilteritinib is an inhibitor of FMS-related tyrosine kinase 3 (FLT3; IC50 = 5 nM for the wild-type enzyme). It inhibits mutant forms of FLT3, including FLT3 with the internal tandem duplication mutation (FLT3-ITD), FLT3-ITD expressing the F691L mutation, and FLT3 with various tyrosine kinase domain mutations (FLT3-TKD; IC50s =1.4-1.8, 12.2, and 0.7-2 nM, respectively). Gilteritinib also inhibits Axl and c-Kit with IC50 values of 41 and 102 nM, respectively. It decreases the viability of blast cells isolated from patients with relapsed acute myeloid leukemia (AML) in a concentration-dependent manner. Formulations containing gilteritinib have been used in the treatment of AML.

Uses

Gilteritinib is an AXL inhibitor in cancer.

Definition

ChEBI: Gilteritinib is a member of the class of pyrazines that is pyrazine-2-carboxamide which is substituted by {3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}nitrilo, (oxan-4-yl)nitrilo and ethyl groups at positions 3,5 and 6, respectively. It is a potent inhibitor of FLT3 and AXL tyrosine kinase receptors (IC50 = 0.29 nM and 0.73 nM, respectively). Approved by the FDA for the treatment of acute myeloid leukemia in patients who have a FLT3 gene mutation. It has a role as an apoptosis inducer, an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor and an antineoplastic agent. It is a N-methylpiperazine, a member of piperidines, a secondary amino compound, a monomethoxybenzene, a member of pyrazines, a primary carboxamide, an aromatic amine and a member of oxanes.

brand name

Xospata

General Description

Class: receptor tyrosine kinase; Treatment: AML, SM; Other name: ASP-2215; Oral bioavailability > 61%; Elimination half-life = 113 h; Protein binding = 94%

target

FLT3, AXL

References

Lee et al. (2017) Preclinical studies of gilteritinib, a next-generation FLT3 inhibitor; Blood?129 257 Thomas et al. (2021) Gilteritinib Inhibits Glutamine Uptake and Utilization in FLT-3-ITD-Positive AML; Cancer Ther.?20 2207

Gilteritinib Preparation Products And Raw materials

Raw materials

Preparation Products

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Gilteritinib Suppliers

China 146 India 5 United States 15 Global 166
SynZeal Research Pvt Ltd
Tel
--
Fax
--
Email
standards@synzeal.com
Country
India
ProdList
6514
Advantage
58
Pharmaffiliates Analytics and Synthetics P. Ltd
Tel
--
Fax
--
Email
mktg@pharmaffiliates.com
Country
India
ProdList
6739
Advantage
58
CHEMSWORTH
Tel
--
Fax
--
Email
info@chemsworth.com
Country
India
ProdList
6700
Advantage
30
A.J Chemicals
Tel
--
Fax
--
Email
sales@ajchem.in
Country
India
ProdList
6100
Advantage
58
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View Lastest Price from Gilteritinib manufacturers

Nanjing Fred Technology Co., Ltd
Product
Gilteritinib 1254053-43-4
Price
US $0.00-0.00/kg
Min. Order
0.1kg
Purity
99%(HPLC)
Supply Ability
100kg
Release date
2023-12-12
shandong perfect biotechnology co.ltd
Product
Gilteritinib 1254053-43-4
Price
US $0.00/g
Min. Order
1g
Purity
98% HPLC
Supply Ability
1kg
Release date
2023-08-02
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
Product
Gilteritinib 1254053-43-4
Price
US $0.00/g
Min. Order
1g
Purity
More Than 99%
Supply Ability
100kg/Month
Release date
2024-08-09

1254053-43-4, GilteritinibRelated Search:

9-Cyclopentyl-2-[[2-methoxy-4-[(1-methylpiperidin-4-yl)oxy]-phenyl]amino]-7-methyl-7,9-dihydro-8H-purin-8-one Dequalinium chloride Volasertib (BI 6727) NORFLUOXETINE HYDROCHLORIDE SGI 7079 N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide ABX-1431 N2-[2-Methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-1,3,5-triazine-2,4-diamine UNC2541

  • ASP2215(Gilteritinib)
  • ASP-2215
  • Gilteritinib
  • 2-Pyrazinecarboxamide, 6-ethyl-3-[[3-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-5-[(tetrahydro-2H-pyran-4-yl)amino]-
  • 6-Ethyl-3-[[3-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-5-[(tetrahydro-2H-pyran-4-yl)amino]-2-pyrazinecarboxamide
  • 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
  • Gilteritinib (ASP2215)
  • 6-Ethyl-3-((3-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)-amino)-5-((tetrahydr
  • Gilteritinib(free base)
  • CS-2849
  • mobcertinib
  • Giliteritinib
  • 6-Ethyl-3-[[3-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidyl]phenyl]amino]-5-[(tetrahydropyran-4-yl)amino]pyrazine-2-carboxamide
  • 6-ethyl-3- (3-methoxy-4- (4- (4-methylpiperazin-1-yl) piperidin-1-yl) phenyl) amino) -5- (tetrahydro-2H-pyran-4-yl) amino) pyrazin-2-formamide
  • Geritinib
  • Gilteritinib Impurity
  • 1254053-43-4
  • C29H44N8O3
  • API