니라파립
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니라파립 속성
- 녹는점
- 187-189°C
- 끓는 점
- 463.6±45.0 °C(Predicted)
- 밀도
- 1.34
- 저장 조건
- 2-8°C(protect from light)
- 용해도
- DMSO(약간 용해됨), 메탄올(약간 용해됨)
- 산도 계수 (pKa)
- 15.36±0.30(Predicted)
- 물리적 상태
- 고체
- 물리적 상태
- 단단한 모양
- 색상
- 연한 노란색에서 밝은 노란색까지
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
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| 유해·위험 문구: |
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| 예방조치문구: |
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니라파립 C화학적 특성, 용도, 생산
개요
(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide is also known as MK-4827(Niraparib) tosylate is a selective inhibitor of PARP1/PARP2 (The poly(ADP-ribose) polymerase) with great activity in cancer cells with mutant BRCA-1 and BRCA-2. It has been recently approved by FDA for the maintenance treatment of adult patients with recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in complete or partial response to platinum-based chemotherapy. In vitro studies have shown that niraparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes resulting in DNA damage, apoptosis and cell death.용도
Niraparib is a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.Pharmacology
The synthesis and initial pharmacology of niraparib have been published. Niraparib has affinity for PARP 1 and 2 inhibition (IC50 = 3.8 and 2.1 nM, respectively) and inhibits the proliferation of cancer cells with mutant BRCA1 and BRCA2 with IC50 values in the 10–100 nM range in vitro. Niraparib demonstrated efficacy as a single agent in a xenograft model of BRCA1-deficient cancer. Niraparib has also been reported to act as a preclinical radiosensitiser and has entered into clinical oncology trials.참고 문헌
https://newdrugapprovals.org/2016/12/22/niraparib-mk-4827/https://www.fda.gov/drugs/informationondrugs/approveddrugs/ucm548487.htm
https://www.drugbank.ca/drugs/DB11793
Sandhu, Shahneen K, et al. "The poly (ADP-ribose) polymerase inhibitor niraparib (MK4827) in BRCA, mutation carriers and patients with sporadic cancer: a phase 1 dose-escalation trial." Lancet Oncology14.9 (2013):882.
Jones, P, et al. "Niraparib: A Poly (ADP-ribose) Polymerase (PARP) Inhibitor for the Treatment of Tumors with Defective Homologous Recombination. " Journal of Medicinal Chemistry 58.8(2015):3302-14.
니라파립 준비 용품 및 원자재
원자재
MK-4827 (R-enantioMer)
methyl 2-(4-(1-(tert-butoxycarbonyl)piperidin-3-yl)phenyl)-2H-indazole-7-carboxylate
Niraparib intermediate 1
methyl 2-{4-[(3S)-1-(tert-butoxycarbonyl)piperidin-3-yl]-phenyl}-2H-indazole-7-carboxylate
2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide hydrochloride
MK-4827 (tosylate)
Methyl 3-formyl-2-nitrobenzoate
준비 용품
니라파립 공급 업체
글로벌( 282)공급 업체
| 공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
|---|---|---|---|---|---|
| SyncoZymes (Shanghai) Co., Ltd., | +86-021-68187180-811 +86-13681683526 |
lchen@syncozymes.com | China | 188 | 58 |
| Hebei Yanxi Chemical Co., Ltd. | +8617531190177 |
peter@yan-xi.com | China | 5993 | 58 |
| Hangzhou ICH Biofarm Co., Ltd | +undefined8613073685410 |
sales@ichemie.com | China | 985 | 58 |
| Henan Fengda Chemical Co., Ltd | +86-371-86557731 +86-13613820652 |
info@fdachem.com | China | 7038 | 58 |
| Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 |
sales@capotchem.com | China | 29797 | 60 |
| Beijing Cooperate Pharmaceutical Co.,Ltd | 010-60279497 |
sales01@cooperate-pharm.com | CHINA | 1811 | 55 |
| Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21695 | 55 |
| Hangzhou FandaChem Co.,Ltd. | 008657128800458; +8615858145714 |
fandachem@gmail.com | China | 9353 | 55 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 |
ivan@atkchemical.com | China | 32480 | 60 |
| career henan chemical co | +86-0371-86658258 |
sales@coreychem.com | China | 29914 | 58 |
니라파립 관련 검색:
MK-4827 (tosylate)
(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxaMide
3-(4-Bromophenyl)piperidine-1-carboxylic acid tert-butyl ester
Nintedanib
4-(4-Methylpiperazinomethyl)-3-(trifluoromethyl)aniline
MK-1775
Ponatinib Hydrochloride
Galeterone
Abemaciclib mesylate (LY2835219)
GDC-0084
SH-4-54
Osimertinib mesylate
Tazemetostat (EPZ-6438)
Mertansine
(S)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-triMethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate
Enasidenib
Ivosidenib
ABBV-075