プラルセチニブ

プラルセチニブ 化学構造式
2097132-94-8
CAS番号.
2097132-94-8
化学名:
プラルセチニブ
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;N-[(1S)-1-[6-(4-フルオロ-1H-ピラゾール-1-イル)-3-ピリジル]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-カルボアミド
英語名:
Pralsetinib
英語别名:
PRALSETINIB;BLU-667;Rralsetinib;CPD2049;BLU-667-API;13C4]-Pralsetinib;PRALSETINIB (BLU667);BLU-667 (Pralsetinib);Pralsetinib Monohydrate;BLU-667;BLU 667;BLU667;2097132-94-8
CBNumber:
CB04632289
化学式:
C27H32FN9O2
分子量:
533.6
MOL File:
2097132-94-8.mol

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
安全性情報
  • リスクと安全性に関する声明
  • 危険有害性情報のコード(GHS)
絵表示(GHS) GHS hazard pictograms
注意喚起語 警告
危険有害性情報
コード 危険有害性情報 危険有害性クラス 区分 注意喚起語 シンボル P コード
H302 飲み込むと有害 急性毒性、経口 4 警告 GHS hazard pictograms P264, P270, P301+P312, P330, P501
H315 皮膚刺激 皮膚腐食性/刺激性 2 警告 GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 強い眼刺激 眼に対する重篤な損傷性/眼刺激 性 2A 警告 GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H335 呼吸器への刺激のおそれ 特定標的臓器毒性、単回暴露; 気道刺激性 3 警告 GHS hazard pictograms
注意書き
P261 粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。
P280 保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。
P301+P312 飲み込んだ場合:気分が悪い時は医師に連絡する こと。
P302+P352 皮膚に付着した場合:多量の水と石鹸で洗うこと。
P305+P351+P338 眼に入った場合:水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

プラルセチニブ 価格

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入

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 &amp; 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 上流と下流の製品情報

原材料

準備製品


プラルセチニブ 生産企業

Global( 127)Suppliers
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Nantong HI-FUTURE Biology Co., Ltd.
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+1-631-485-4226
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Shenzhen Shengda Pharma Limited
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Zhejiang J&C Biological Technology Co.,Limited
+1-2135480471 +1-2135480471
sales@sarms4muscle.com China 10522 58

2097132-94-8(プラルセチニブ)キーワード:


  • 2097132-94-8
  • CPD2049
  • (1r,4S)-N-((S)-1-(6-(4-fluoro-1H-pyrazol-1-yl)pyridin-3-yl)ethyl)-1-methoxy-4-(4-methyl-6-((5-methyl-1H-pyrazol-3-yl)amino)pyrimidin-2-yl)cyclohexanecarboxamide
  • BLU-667 (Pralsetinib)
  • BLU-667;BLU 667;BLU667;2097132-94-8
  • (1r,4S)-N-((S)-1-(6-(4-fluoro-1H-pyrazol-1-yl)pyridin-3-yl)ethyl)-1-methoxy-4-(4-methyl-6-((5-methyl-1H-pyrazol-3-yl)amino)pyrimidin-2-yl)cyclohexane-1-carboxamide
  • PRALSETINIB (BLU667)
  • (1s,4R)-N-((S)-1-(6-(4-fluoro-1H-pyrazol-1-yl)pyridin-3-yl)ethyl)-1-methoxy-4-(4-methyl-6-((5-methyl-1H-pyrazol-3-yl)amino)pyrimidin-2-yl)cyclohexanecarboxamide
  • Cyclohexanecarboxamide, N-[(1S)-1-[6-(4-fluoro-1H-pyrazol-1-yl)-3-pyridinyl]ethyl]-1-methoxy-4-[4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyrimidinyl]-, cis-
  • BLU-667
  • PRALSETINIB
  • Rralsetinib
  • 13C4]-Pralsetinib
  • (cis)-N-((S)-1-(6-(4-fluoro-1H-pyrazol-1-yl)pyridin-3-yl)ethyl)-1-methoxy-4-(4-methyl-6-(5- methyl-1H-pyrazol-3-ylamino)pyrimidin-2-yl)cyclohexanecarboxamide
  • (1s,4R)-N-((S)-1-(6-(4-fluoro-1H-pyrazol-1-yl)pyridin-3-yl)ethyl)-1-methoxy-4-(4-methyl -6-((5-methyl-1H-pyrazol-3-yl)amino)pyrimidin-2-yl)cyclohexane-1-carboxamide
  • BLU-667-API
  • Pralsetinib Monohydrate
  • 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
  • N-[(1S)-1-[6-(4-フルオロ-1H-ピラゾール-1-イル)-3-ピリジル]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-カルボアミド
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