ChemicalBook > CAS DataBase List > Lestaurtinib
Lestaurtinib
Lestaurtinib
- CAS No.111358-88-4
- Chemical Name:Lestaurtinib
- CBNumber:CB3506750
- Molecular Formula:C26H21N3O4
- Formula Weight:439.47
- MOL File:111358-88-4.mol
Lestaurtinib Property
- Melting point 215-220°C
- Boiling point 723.0±60.0 °C(Predicted)
- Density 1.70±0.1 g/cm3(Predicted)
- storage temp. Desiccate at -20°C
- solubility DMSO: >10mg/mL
- form white powder
- pka 13.37±0.40(Predicted)
- color White or off-white
- Stability Photosensitive
- NCI Dictionary of Cancer Terms apalutamide; CEP-701; lestaurtinib
- FDA UNII DO989GC5D1
- NCI Drug Dictionary apalutamide
- ATC code L02BB05
- UNSPSC Code 12352200
- NACRES NA.77
Safety
-
Symbol(GHS)
- Signal wordWarning
- Hazard statements H315-H319-H335
- Precautionary statements P271-P261-P280
Lestaurtinib Price
More Price(2)
- Brand: Sigma-Aldrich(India)
- Product number: C7869
- Product name : CEP-701 hydrate
- Purity: ≥98% (HPLC)
- Packaging: 1MG
- Price: ₹18380.85
- Updated: 2022/06/14
- Buy: Buy
- Brand: Sigma-Aldrich(India)
- Product number: C7869
- Product name : CEP-701 hydrate
- Purity: ≥98% (HPLC)
- Packaging: 5MG
- Price: ₹73458.45
- Updated: 2022/06/14
- Buy: Buy
Lestaurtinib Chemical Properties,Usage,Production
- Description Lestaurtinib (111358-88-4) is a potent and selective FLT3 inhibitor (IC50= 2 nM).1,2?Inhibits RET and RET phosphorylation in medullary thyroid carcinoma cells.3?Suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders.4?Potent Trk inhibitor.5?Cell permeable.
- Chemical Properties Lestaurtinib is Off-White Solid
- Uses Lestaurtinib is used for the treatment of pancreatic cancer and acute myelogenous leukaemia (AML)
- Uses It is used for the treatment of pancreatic cancer and acute myelogenous leukaemia (AML).
-
Uses
CEP-701 hydrate has been used as a tyrosine kinase inhibitor:
- to study its effects on early growth response protein (EGR) genes and nerve growth factor (NGF) stimulation in human epithelial cells
- as a supplement in reservoir solution for co-crystallization studies with human receptor-interacting?protein kinase?4 (RIPK4)
- as an FMS-like tyrosine kinase 3 (FLT3) inhibitor-gold nanoparticle conjugate to study its effects on acute myeloid leukemia
- Definition ChEBI: LSM-1231 is an indolocarbazole.
- Biological Activity Potent JAK2, FLT3 and TrkA inhibitor (IC 50 values are 0.9, 3 and < 25 nM respectively) that prevents STAT5 phosphorylation (IC 50 = 20 - 30 nM). Exhibits antiproliferative activity in vitro (IC 50 = 30 - 100 nM in HEL92.1.7 cells) and is effective against myeloproliferative disorders in vivo .
- Biochem/physiol Actions CEP-701 hydrate, also known as Lestaurtinib, can repress Janus kinase 2/signal transducer and activator of transcription 5 (JAK2/STAT5) signaling by the specific inhibition of JAK2.
- storage -20°C (desiccate)
- References 1) Levis?et al. (2003),?Novel FLT3 tyrosine kinase inhibitors; Expert Opin. Investig. Drugs,?12?1951 2) Chen?et al.?(2005),?FLT3/ITD Mutation Signaling Includes Suppression of SHP-1; J. Biol. Chem.,?280?5361 3) Strock?et al. (2003),?CEP-701 and CEP-751 Inhibit Constitutively Activated RET Tyrosine Kinase Activity and Block Medullary Thyroid Carcinoma Cell Growth; Cancer Res.,?63?5559 4) Hexner?et al. (2008),?Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders; Blood,?111?5663 5) Ruggeri?et al. (1999),?Role of neurotrophin-trk interactions in oncology: the anti-tumor efficacy of potent and selective trk tyrosine kinase inhibitors in pre-clinical tumor models; Curr. Med. Chem.,?6?845
Lestaurtinib Preparation Products And Raw materials
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- Pharmaceuticals
- Intermediates & Fine Chemicals
- Inhibitor
- 信号转导通路激酶抑制剂
- 抑制剂
- 原料药及中间体
- 医药原料
- C26H21N3O4
- (5R,7S,8S)-7-羟基-7-(羟甲基)-8-甲基-5,6,7,8,13,14-六氢-15H-16-氧杂-4B,8A,14-三氮杂-5,8-甲二苯并[B,H]环八[JKL]环戊[E]-AS-茚-15-酮
- LESTAURTINIB 来他替尼
- 来他替尼
- 来他替尼 CEP-701, LESTAURTINIB
- 来他替尼、CEP-701
- 来他替尼LESTAURTINIB,CEP-701
- 111358-88-4
- ritatinib
- Lestaurtinib USP/EP/BP
- KT5555-Lestaurtinib
- 9,12-Epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one, 2,3,9,10,11,12-hexahydro-10-hydroxy-10-(hydroxymethyl)-9-methyl-, (9S,10S,12R)-
- LESTAURTINIB (CEP-701;KT-5555)
- (15S,16S,18R)-16-HYDROXY-16-(HYDROXYMETHYL)-15-METHYL-28-OXA-4,14,19-TRIAZAOCTACYCLO[12.11.2.1^{15,18}.0^{2,6}.0^{7,27}.0^{8,13}.0^{19,26}.0^{20,25}]OCTACOSA-1(26),2(6),7(27),8,10,12,20,22,24-NONAEN-3-ONE
- CS-1165
- Lestaurtinib (KT-5555
- SP 924
- KT 5555
- CEP 701
- (9S,10S,12R)-2,3,9,10,11,12-Hexahydro-10-hydroxy-10-(hydroxymethyl)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:321kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one
- A 154475.0
- Lestaurtinib hydrate
- KT-5555 hydrate
- CEP-701 hydrate
- SPM-924
- (9S-(9α,10β,12α))-2,3,9,10,11,12-hexahydro-10-hydroxy-10-(hydroxyMethyl)-9-Methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one
- lestaurtinib