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Gilteritinib

Gilteritinib Structure
Gilteritinib structure
CAS No.
1254053-43-4
Chemical Name:
Gilteritinib
Synonyms
Gilteritinib;CS-2849;ASP-2215;Geritinib;mobcertinib;Giliteritinib;2H5]-Gilteritinib;ASP2215(Gilteritinib);Gilteritinib (ASP2215);Gilteritinib Impurity
CBNumber:
CB82725626
Molecular Formula:
C29H44N8O3
Molecular Weight:
552.71
MDL Number:
MFCD28144685
MOL File:
1254053-43-4.mol
Last updated:2024-11-19 20:33:22
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Gilteritinib Properties

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)
form solid
pka 14.39±0.50(Predicted)
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.
FDA UNII 66D92MGC8M
NCI Drug Dictionary gilteritinib
ATC code L01EX13

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H315-H319-H335
Precautionary statements  P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P321-P362+P364-P332+P313-P337+P313-P403+P233-P405-P501
NFPA 704
0
2 0

Gilteritinib price More Price(17)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 21503 Gilteritinib ≥98% 1254053-43-4 1mg $32 2024-03-01 Buy
Cayman Chemical 21503 Gilteritinib ≥98% 1254053-43-4 5mg $116 2024-03-01 Buy
Cayman Chemical 21503 Gilteritinib ≥98% 1254053-43-4 10mg $214 2024-03-01 Buy
Cayman Chemical 21503 Gilteritinib ≥98% 1254053-43-4 25mg $381 2024-03-01 Buy
Usbiological 451193 Gilteritinib 1254053-43-4 10mg $425 2021-12-16 Buy
Product number Packaging Price Buy
21503 1mg $32 Buy
21503 5mg $116 Buy
21503 10mg $214 Buy
21503 25mg $381 Buy
451193 10mg $425 Buy

Gilteritinib Chemical Properties,Uses,Production

Physical Form

Pale-yellow to Yellow-brown Solid

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 synthesis

33024-60-1
1254053-43-4
Synthesis of Gilteritinib from 4-Aminotetrahydropyran hydrochloride

Gilteritinib Preparation Products And Raw materials

Raw materials

4-Aminotetrahydropyran hydrochloride

Preparation Products

Gilteritinib Suppliers

Global( 165)Suppliers
Supplier Tel Email Country ProdList Advantage
shandong perfect biotechnology co.ltd 		+86-53169958659 +86-13153181156 sales@sdperfect.com China 294 58
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. 		+86-18600796368 +86-18600796368 sales@sjar-tech.com China 456 58
Hangzhou FandaChem Co.,Ltd. 		+8615858145714 FandaChem@Gmail.com China 9087 55
ATK CHEMICAL COMPANY LIMITED 		+undefined-21-51877795 ivan@atkchemical.com China 32957 60
BOC Sciences 		+1-631-485-4226 inquiry@bocsci.com United States 19553 58
career henan chemical co 		+86-0371-86658258 +8613203830695 factory@coreychem.com China 29811 58
Xi'an Yutbon Pharmaceutical Technology Co., Ltd 		029-81140587 +8618717328141 sales@yutbon.com China 454 58
TargetMol Chemicals Inc. 		+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 32161 58
HANGZHOU CLAP TECHNOLOGY CO.,LTD 		86-571-88216897,88216896 13588875226 sales@hzclap.com CHINA 6312 58
ANHUI WITOP BIOTECH CO., LTD 		+8615255079626 eric@witopchemical.com China 23541 58
Supplier Advantage
shandong perfect biotechnology co.ltd 		58
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. 		58
Hangzhou FandaChem Co.,Ltd. 		55
ATK CHEMICAL COMPANY LIMITED 		60
BOC Sciences 		58
career henan chemical co 		58
Xi'an Yutbon Pharmaceutical Technology Co., Ltd 		58
TargetMol Chemicals Inc. 		58
HANGZHOU CLAP TECHNOLOGY CO.,LTD 		58
ANHUI WITOP BIOTECH CO., LTD 		58

Related articles

View Lastest Price from Gilteritinib manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Gilteritinib pictures 2024-12-23 Gilteritinib
1254053-43-4
 US $0.00 / g 1g More Than 99% 100kg/Month BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
Gilteritinib pictures 2024-11-26 Gilteritinib
1254053-43-4
 US $0.00-0.00 / kg 0.1kg 99%(HPLC) 100kg Nanjing Fred Technology Co., Ltd
Gilteritinib pictures 2024-11-19 Gilteritinib
1254053-43-4
 US $34.00-82.00 / mg 99.74% 10g TargetMol Chemicals Inc.
  • Gilteritinib pictures
  • Gilteritinib
    1254053-43-4
  • US $0.00 / g
  • More Than 99%
  • BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
  • Gilteritinib pictures
  • Gilteritinib
    1254053-43-4
  • US $0.00-0.00 / kg
  • 99%(HPLC)
  • Nanjing Fred Technology Co., Ltd
  • Gilteritinib pictures
  • Gilteritinib
    1254053-43-4
  • US $34.00-82.00 / mg
  • 99.74%
  • TargetMol Chemicals Inc.

Gilteritinib Spectrum

ASP-2215(1254053-43-4)1HNMR

1254053-43-4(Gilteritinib)Related 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

1of2

ASP-2215 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 ASP2215(Gilteritinib) Gilteritinib(free base) CS-2849 mobcertinib Gilteritinib Giliteritinib 2H5]-Gilteritinib 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