Gilteritinib
in vivo- Product Name
- Gilteritinib
- CAS No.
- 1254053-43-4
- Chemical Name
- Gilteritinib
- Synonyms
- Gilteritinib;CS-2849;ASP-2215;mobcertinib;Giliteritinib;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;6-Ethyl-3-[[3-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidyl]phenyl]amino]-5-[(tetrahydropyran-4-yl)amino]pyrazine-2-carboxamide
- CBNumber
- CB82725626
- Molecular Formula
- C29H44N8O3
- Formula Weight
- 552.71
- MOL File
- 1254053-43-4.mol
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.
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..…
N-Bromosuccinimide Price
- Product number
- 21503
- Product name
- Gilteritinib
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 21503
- Product name
- Gilteritinib
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $116
- Updated
- 2024/03/01
- Product number
- 21503
- Product name
- Gilteritinib
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $214
- Updated
- 2024/03/01
- Product number
- 21503
- Product name
- Gilteritinib
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $381
- Updated
- 2024/03/01
- Product number
- 451193
- Product name
- Gilteritinib
- Packaging
- 10mg
- Price
- $425
- Updated
- 2021/12/16
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.
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
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View Lastest Price from Gilteritinib manufacturers
- Product
- Gilteritinib 1254053-43-4
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- 98% HPLC
- Supply Ability
- 1kg
- Release date
- 2023-08-02
- 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
- Product
- ASP-2215 1254053-43-4
- Price
- US $0.00-0.00/KG
- Min. Order
- 1KG
- Purity
- 98%
- Supply Ability
- 1ton
- Release date
- 2022-09-22