Gilteritinib
- CAS No.
- 1254053-43-4
- Chemical Name:
- Gilteritinib
- Synonyms
- Gilteritinib;CS-2849;ASP-2215;mobcertinib;Giliteritinib;2H5]-Gilteritinib;ASP2215(Gilteritinib);Gilteritinib (ASP2215);Gilteritinib(free base);6-Ethyl-3-((3-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)-amino)-5-((tetrahydr
- CBNumber:
- CB82725626
- Molecular Formula:
- C29H44N8O3
- Molecular Weight:
- 552.71
- MDL Number:
- MFCD28144685
- MOL File:
- 1254053-43-4.mol
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) | GHS07 |
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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 |
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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 |
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.
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
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
Xi'an Yutbon Pharmaceutical Technology Co., Ltd | 029-81140587 +8618717328141 | sales@yutbon.com | China | 437 | 58 |
shandong perfect biotechnology co.ltd | +86-53169958659; +8618596095638 | sales@sdperfect.com | China | 294 | 58 |
Hangzhou FandaChem Co.,Ltd. | 008657128800458; +8615858145714 | fandachem@gmail.com | China | 9348 | 55 |
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
ANHUI WITOP BIOTECH CO., LTD | +8615255079626 | eric@witopchemical.com | China | 23556 | 58 |
Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
Alfa Chemistry | +1-5166625404 | Info@alfa-chemistry.com | United States | 21317 | 58 |
Related articles
- The Pharmacodynamics and Synthetic method of Gilteritinib
- Gilteritinib, an oral inhibitor of FMS‐like tyrosine kinase 3 (FLT3), is a standard treatment for FLT3‐mutated acute myeloid l....
- Dec 28,2023
View Lastest Price from Gilteritinib manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
---|---|---|---|---|---|---|---|---|
2024-03-12 | Gilteritinib
1254053-43-4
|
US $0.00 / g | 1g | 98% HPLC | 1kg | shandong perfect biotechnology co.ltd | ||
2023-12-12 | Gilteritinib
1254053-43-4
|
US $0.00-0.00 / kg | 0.1kg | 99%(HPLC) | 100kg | Nanjing Fred Technology Co., Ltd | ||
2022-09-23 | ASP-2215
1254053-43-4
|
US $0.00-0.00 / KG | 1KG | 98% | 1ton | Henan Aochuang Chemical Co.,Ltd. |
- Gilteritinib
1254053-43-4
- US $0.00 / g
- 98% HPLC
- shandong perfect biotechnology co.ltd
- Gilteritinib
1254053-43-4
- US $0.00-0.00 / kg
- 99%(HPLC)
- Nanjing Fred Technology Co., Ltd
- ASP-2215
1254053-43-4
- US $0.00-0.00 / KG
- 98%
- Henan Aochuang Chemical Co.,Ltd.