プラルセチニブ化学構造式

プラルセチニブ

化学名:プラルセチニブ

CAS番号.2097132-94-8

英語名:Pralsetinib

CBNumberCB04632289

MFC27H32FN9O2

MW533.6

MOL File2097132-94-8.mol

别名

N-[(1S)-1-[6-(4-フルオロピラゾール-1-イル)ピリジン-3-イル]エチル]-1-メトキシ-4-{4-メチル-6-[(5-メチル-1H-ピラゾール-3-イル)アミノ]ピリミジン-2-イル}シクロヘキサン-1-カルボキサミド

N-[(1S)-1-[6-(4-フルオロ-1H-ピラゾール-1-イル)ピリジン-3-イル]エチル]-1-メトキシ-4-{4-メチル-6-[(5-メチル-1H-ピラゾール-3-イル)アミノ]ピリミジン-2-イル}シクロヘキサン-1-カルボキサミド

プラルセチニブ

プラルセチニブ物理性質

沸点	799.1±60.0 °C(Predicted)
比重(密度)	1.40±0.1 g/cm3(Predicted)
貯蔵温度	Store at 4°C
溶解性	DMSO : ≥ 100 mg/mL (187.41 mM);Water : < 0.1 mg/mL (insoluble)
外見	Solid
酸解離定数(Pka)	14.33±0.10(Predicted)
色	White to off-white
InChIKey	GBLBJPZSROAGMF-BATDWUPUSA-N
SMILES	[C@]1(OC)(C(N[C@H](C2=CC=C(N3C=C(F)C=N3)N=C2)C)=O)CC[C@H](C2=NC(NC3C=C(C)NN=3)=CC(C)=N2)CC1

危険有害性情報のコード(GHS)

プラルセチニブ化学特性,用途語,生産方法

説明
Pralsetinib is a potent, selective RET inhibitor, and was optimized from a hit compound identified from a compound library that included more than 60 chemical scaffolds. However, as of 2020, detailed medicinal chemistry on the optimization process has yet to be published. Pralsetinib proved to be more potent and selective than cabozantinib or vandertanib against both wild-type and abnormal RET. The agent also showed a level of selectivity against RET relative to VEGFR2, whereas previous agents showed very little selectivity. On September 4, 2020, the Food and Drug Administration granted accelerated approval to pralsetinib (GAVRETO®, Blueprint Medicines Corporation) for adult patients with metastatic RET fusion-positive non-small cell lung cancer (NSCLC) as detected by an FDA-approved test.
使用
Pralsetinib is a highly potent and selective RET inhibitor designed for RET-driven cancers.
適応症
Pralsetinib is the second selective RET inhibitor approved by the FDA (following Lilly's selpercatinib) for the treatment of adult patients with metastatic RET (rearranged during transfection) fusion-positive non-small cell lung cancer (NSCLC); (2) adult and pediatric patients >=12 years of age with advanced or metastatic RET-mutant medullary thyroid cancer (MTC) who require systemic therapy; and (3) adult and pediatric patients >=12 years of age with advanced or metastatic RET fusion-positive thyroid cancer who require systemic therapy and who are radioactive iodine-refractory.
brand name
Gavreto
Synthesis Reference(s)
[1] GAIKWAD RAJENDRA. Green One-Pot Chemo-Enzymatic Synthesis of a Key Chiral Amine Intermediate: Useful to Pralsetinib Synthesis[J]. ChemistrySelect, 2023. DOI:10.1002/slct.202204409.
[2] HUGHES* D L. Review of Synthetic Routes and Crystalline Forms of the Oncology Drugs Capmatinib, Selpercatinib, and Pralsetinib[J]. Organic Process Research & Development, 2021. DOI:10.1021/acs.oprd.1c00282.
副作用
Pralsetinib may cause side effects: Nausea, vomiting, loss of appetite, diarrhea, constipation, extreme tiredness, dizziness, weakness, night sweats, rapid heartbeat, heartburn, shortness of breath, headache, sores in the mouth, confusion, changes in vision, fever, cough, chills, nosebleeds, pale skin, rash, itching, hives, weight changes, hair loss, back pain, muscle pain, joint pain, bone pain, unusual bruising or bleeding, blood in the urine or stool, bloody or black tarry stools, difficulty falling asleep or staying asleep, unusual vaginal bleeding, and other less common effects.
Mode of action
Kinase inhibitor of wild-type RET, oncogenic RET fusions, and select mutations. Pralsetinib may also inhibit other pathways including those through FLT3, JAK1-2, PDGFRB, VEGFR-2, and FGFR1. RET fusion proteins and activating point mutations can act as oncogenic drivers by promoting cell proliferation of tumor cell lines and pralsetinib inhibits this process.

プラルセチニブ生産企業

2097132-94-8, プラルセチニブキーワード

Send Inquriy

プラルセチニブ

危険有害性情報のコード(GHS)

プラルセチニブ 化学特性,用途語,生産方法

プラルセチニブ 生産企業

2097132-94-8, プラルセチニブ キーワード

プラルセチニブ化学特性,用途語,生産方法

プラルセチニブ生産企業

2097132-94-8, プラルセチニブキーワード