Gilteritinib

ChemicalBook > CAS DataBase List > 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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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