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Rucaparib phosphate PARP 억제제

Name: Rucaparib phosphate
Brand: Selleck Chemicals
SKU: S1098
Rating: 5 (136 reviews)

제품 번호: S1098

Rucaparib phosphate는 세포 무함유 분석에서 PARP1에 대해 1.4 nM의 K_i를 갖는 PARP 억제제이며, 다른 8개의 PARP 도메인에 대한 결합 친화성도 나타냅니다. 임상 3상.

Rucaparib phosphate PARP 억제제 Chemical Structure

화학 구조

분자량: 421.36

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품질 관리 (Quality Control)

배치: 순도: 99.89%

99.89

관련 타겟	HDAC ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase eIF
기타 PARP 억제제	XAV-939 AZD5305 (Saruparib) Veliparib (ABT-888) PJ34 HCl AG-14361 Iniparib (BSI-201) G007-LK A-966492 UPF 1069 Pamiparib

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주	분석 유형	농도	배양 시간	제형	활성 설명	PMID
BT-474	Function Assay	0.1/1/500/1000 nM			inhibits PARP activity at starting concerntration of 500 nM	25128455
BT474	Growth Inhibition Assay	500 nM	10–15 d		reduces cell growth in the four lines and significantly	25128455
SKBR3	Growth Inhibition Assay	500 nM	10–15 d		reduces cell growth in the four lines and significantly	25128455
AU565	Growth Inhibition Assay	500 nM	10–15 d		reduces cell growth in the four lines and significantly	25128455
EFM192A	Growth Inhibition Assay	500 nM	10–15 d		reduces cell growth in the four lines and significantly	25128455
MDA-MB-231	Function Assay	10/20/40 μM	24 h		increases p-AKT levels in a dose-dependent manner	24420152
MDA-MB-231	Cell Viability Assay	0.1-40 μM	24 h		IC50 = 17.77 μM	24420152
MDA-MB-231	Apoptosis Assay	10/20/40 μM	24 h		induces apoptosis dose dependently	24420152
MDA-MB-231	Growth Inhibition Assay	10/20/40 μM	24 h		blocks cell cycle progression in G2/M phase	24420152
H460	Growth Inhibition Assay	400 nM	24 h		increases cellular radiosensitivity	24411611
A549	Growth Inhibition Assay	400 nM	24 h		increases cellular radiosensitivity	24411611
DT40	Growth Inhibition Assay				IC50=21 nM	24356813
DU145	Growth Inhibition Assay				IC50=18 nM	24356813
COLO704	Growth Inhibition Assay				IC50=2.52 ± 0.67 μM	23729402
OVMANAb	Growth Inhibition Assay				IC50=2.58 ± 0.38 μM	23729402
OV177	Growth Inhibition Assay				IC50=2.78 ± 0.71 μM	23729402
OAW28	Growth Inhibition Assay				IC50=3.61 ± 0.28 μM	23729402
OVSAHO	Growth Inhibition Assay				IC50=3.64 ± 0.33 μM	23729402
OVKATE	Growth Inhibition Assay				IC50=3.64 ± 1.79 μM	23729402
OVCAR3	Growth Inhibition Assay				IC50=3.74 ± 0.40 μM	23729402
PEO14	Growth Inhibition Assay				IC50=3.84 ± 0.76 μM	23729402
A2780	Growth Inhibition Assay				IC50=3.94 ± 0.25 μM	23729402
OVTOKO	Growth Inhibition Assay				IC50=4.14 ± 1.53 μM	23729402
KURAMOCHIb	Growth Inhibition Assay				IC50=4.34 ± 0.29 μM	23729402
TOV21G	Growth Inhibition Assay				IC50=5.07 ± 1.30 μM	23729402
OVISE	Growth Inhibition Assay				IC50=5.68 ± 0.23 μM	23729402
KK	Growth Inhibition Assay				IC50=6.15 ± 1.42 μM	23729402
RMUGS	Growth Inhibition Assay				IC50=7.03 ± 1.83 μM	23729402
PEO6	Growth Inhibition Assay				IC50=7.06 ± 0.74 μM	23729402
OVCA429	Growth Inhibition Assay				IC50=8.29 ± 1.64 μM	23729402
OV167	Growth Inhibition Assay				IC50=8.33 ± 1.18 μM	23729402
RMG1	Growth Inhibition Assay				IC50=9.32 ± 2.36 μM	23729402
OVCAR5	Growth Inhibition Assay				IC50=9.50 ± 2.59 μM	23729402
EFO21	Growth Inhibition Assay				IC50=9.92 ± 1.87 μM	23729402
ES2	Growth Inhibition Assay				IC50=10.12 ± 1.23 μM	23729402
Tyk-nu	Growth Inhibition Assay				IC50=10.20 ± 1.12 μM	23729402
CAOV3	Growth Inhibition Assay				IC50=10.37 ± 0.87 μM	23729402
OV207	Growth Inhibition Assay				IC50=12.27 ± 0.32 μM	23729402
HEY	Growth Inhibition Assay				IC50=13.01 ± 0.75 μM	23729402
DOV13	Growth Inhibition Assay				IC50>15 μM	23729402
EFO27	Growth Inhibition Assay				IC50>15 μM	23729402
HEY C2	Growth Inhibition Assay				IC50>15 μM	23729402
KOC-7cc	Growth Inhibition Assay				IC50>15 μM	23729402
MCASb	Growth Inhibition Assay				IC50>15 μM	23729402
OAW42	Growth Inhibition Assay				IC50>15 μM	23729402
OV2008	Growth Inhibition Assay				IC50>15 μM	23729402
OV90	Growth Inhibition Assay				IC50>15 μM	23729402
OVCA420b	Growth Inhibition Assay				IC50>15 μM	23729402
OVCA432	Growth Inhibition Assay				IC50>15 μM	23729402
PEA2	Growth Inhibition Assay				IC50>15 μM	23729402
SKOV3	Growth Inhibition Assay				IC50>15 μM	23729402
TOV112D	Growth Inhibition Assay	0-3 μM			IC50>15 μM	23729402
C4-2	Growth Inhibition Assay	0-3 μM	14 d	DMSO	decreases colony number dose dependently	23565244
PC3	Growth Inhibition Assay	0-3 μM	14 d	DMSO	decreases colony number dose dependently	23565244
DU145	Growth Inhibition Assay	0-3 μM	14 d	DMSO	decreases colony number dose dependently	23565244
VCaP	Growth Inhibition Assay	0-3 μM	14 d	DMSO	decreases colony number dose dependently	23565244
LNCaP	Growth Inhibition Assay	0-3 μM	14 d	DMSO	decreases colony number dose dependently	23565244
MDA-MB-468	Cell Viability Assay				IC50=9.7 μM	22678161
MDA-MB-231	Cell Viability Assay				IC50=13 μM	22678161
Cal-51	Cell Viability Assay				IC50=8.6 μM	22678161
LoVo	Function assay		30 mins		Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay, EC50 = 0.00469 μM.	26652717
MX1	Cytotoxicity assay				Cytotoxicity against BRCA1-deficient human MX1 cells, EC50 = 0.0053 μM.	26652717
Rosetta2 (DE3)	Function assay				Inhibition of human N-terminal 6xhis-tagged ARTD6 (873 to 1161) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate by fluorescence assay, IC50 = 0.014 μM.	24900770
Rosetta2 (DE3)	Function assay				Inhibition of human 6xhis-tagged ARTD5 (1030 to 1317) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate by fluorescence assay, IC50 = 0.025 μM.	24900770
LoVo	Cytotoxicity assay	0.4 uM	5 days		Potentiation of temozolomide-induced cytotoxicity in human LoVo cells assessed as temozolomide GI50 at 0.4 uM after 5 days by Celltiter-Glo assay, GI50 = 0.144 μM.	26652717
Capan1	Cytotoxicity assay				Cytotoxicity against BRCA2-deficient human Capan1 cells, EC50 = 0.609 μM.	26652717
MDA-MB-436	Anticancer assay		96 hrs		Anticancer activity against human BRCA1-deficient MDA-MB-436 cells after 96 hrs by MTT assay, CC50 = 3 μM.	26342868
OVCAR3	Antiproliferative assay		24 hrs		Antiproliferative activity against human OVCAR3 cells after 24 hrs by MTT assay, IC50 = 3.31 μM.	29456106
MRC5	Cytotoxicity assay				Cytotoxicity against human MRC5 cells, EC50 = 8.53 μM.	26652717
MCF7	Anticancer assay		96 hrs		Anticancer activity against human MCF7 cells after 96 hrs by MTT assay, CC50 = 19.47 μM.	26342868
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
Rh41	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
SK-N-MC	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
TC32	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량	421.36	화학식	C₁₉H₁₈FN₃O.H₃PO₄	보관 (수령일로부터)	3년-20°C분말
CAS 번호	459868-92-9	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	AG-014699 phosphate, PF-01367338 phosphate			Smiles	CNCC1=CC=C(C=C1)C2=C3CCNC(=O)C4=C3C(=CC(=C4)F)N2.OP(=O)(O)O

용해도 (Solubility)

In vitro
배치:

DMSO : 85 mg/mL (201.72 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 7 mg/mL

Ethanol : Insoluble

DMSO : 84 mg/mL (199.35 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 93 mg/mL (220.71 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 2 mg/mL

Ethanol : Insoluble

DMSO : 84 mg/mL (199.35 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 2 mg/mL

Ethanol : Insoluble

DMSO : 84 mg/mL (199.35 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 6 mg/mL

Ethanol : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

특징	The first PARP inhibitor used in clinical trials combined with temozolomide.
Targets/IC₅₀/Ki	PARP (Cell-free assay) 1.4 nM(Ki)
시험관 내(In vitro)	Rucaparib is a potent inhibitor of purified full-length human PARP-1 and shows higher inhibition of cellular PARP in LoVo and SW620 cells. Besides, Rucaparib binds detectably to eight other PARP domains, including PARP2, 3, 4, 10, 15, 16, TNKS1 and TNKS2. The radio-sensitization by Rucaparib is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib could target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions. Rucaparib inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells.
키나아제 분석	K_i 결정
키나아제 분석	[³²P]NAD⁺ 결합을 이용한 인간 전장 재조합 PARP-1의 억제 효능을 측정한다. 산 불용성 물질로 결합된 [³²P]ADP-ribose는 PhosphorImager를 사용하여 정량화한다. K_i 값은 비선형 회귀 분석을 통해 계산한다.
생체 내(In vivo)	Rucaparib is not toxic but significantly enhances temozolomide-induced TGD in the DNA repair protein-competent D384Med xenografts. Pharmacokinetics studies also show that Rucaparib is detected in the brain tissue, which indicates that Rucaparib has potential in intra-cranial malignancy therapy. Rucaparib significantly potentiates the cytotoxicity of topotecan and temozolomide in NB-1691, SH-SY-5Y, and SKNBE (2c) cells. Rucaparib enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/17363489/ [2] http://www.nature.com/scibx/journal/v5/n13/full/scibx.2012.323.html [3] https://pubmed.ncbi.nlm.nih.gov/21706052/ [4] https://pubmed.ncbi.nlm.nih.gov/20978505/ [5] https://pubmed.ncbi.nlm.nih.gov/19174487/

적용 분야 (Applications)

방법	바이오마커	PMID
Western blot	PAR BRCA1	27960087
Growth inhibition assay	Cell viability	31119062
Immunofluorescence	α-tubulin PAR γH2AX 53BP1	30589644

임상시험 정보 (Clinical Trial Information)

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2026-07-29)

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT03899155	RECRUITING	Cancer	Bristol-Myers Squibb	2019-08-09	PHASE2
NCT03768063	ACTIVE_NOT_RECRUITING	Cancer	Hoffmann-La Roche	2019-02-28	PHASE3
NCT02925234	RECRUITING	Cancer; Tumors; Neoplasm; Neoplasia	The Netherlands Cancer Institute	2016-08	PHASE2
NCT04455750	ACTIVE_NOT_RECRUITING	Castration-Resistant Prostate Carcinoma; Metastatic Prostate Adenocarcinoma; Stage IV Prostate Cancer AJCC v8; Stage IVA Prostate Cancer AJCC v8; Stage IVB Prostate Cancer AJCC v8	Alliance for Clinical Trials in Oncology	2021-10-14	PHASE3
NCT04253262	ACTIVE_NOT_RECRUITING	Metastatic Castration-resistant Prostate Cancer	Brown University	2020-04-03	PHASE1; PHASE2
NCT04624178	ACTIVE_NOT_RECRUITING	Leiomyosarcoma	Memorial Sloan Kettering Cancer Center	2020-11-05	PHASE2

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Rucaparib phosphate PARP 억제제

분자량: 421.36

품질 관리 (Quality Control)

세포 배양, 처리 및 작업 농도 (Cell Culture, Treatment & Working Concentration)

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

용해도 (Solubility)

몰농도 계산기

생체 내 제형 계산기 (투명한 용액)

작용 메커니즘 (Mechanism of Action)

적용 분야 (Applications)

임상시험 정보 (Clinical Trial Information)

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)