Rucaparib (AG-014699,PF-01367338) | CAS#459868-92-9 APExBIO 貨號A4156
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特點
PARP抑制劑系列商品->>Rucaparib (AG-014699,PF-01367338)
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Rucaparib (AG-014699,PF-01367338)| CAS#459868-92-9 APExBIO 貨號A4156
Potent PARP inhibitor
Rucaparib，也稱為 AG-014699 或 PF-01367338，是一種聚（ADP 核糖）聚合酶（PARP）抑制劑。 PARP 是一種 DNA 損傷激活核酶( DNA damage-activated nuclear enzyme)，在鹼基切除修復途徑中具有關鍵的信號傳導作用。因此，rucaparib 也被發現對 DNA 修復缺陷的細胞最有效，這些細胞缺陷是由於暴露於基因毒性劑而引起的，例如輻射會產生 DNA 損傷，當 DNA 修復受損時，其毒性會增強。 rucaparib 存在下放射敏感性的增加與 γ-H2AX 和 p53BP1 焦點確定的持續性 DNA 斷裂有關。 Rucaparib 使前列腺癌細胞放射增敏，最有效的是那些 PTEN 缺陷並表達 ETS 基因融合蛋白(ETS gene fusion proteins)的細胞，該蛋白抑制 NHEJ DNA 修復 (NHEJ DNA repair)。
References
Ruth Plummer, Paul Lorigan, Neil Steven, Lucy Scott, Mark R. Middleton, Richard H. Wilson, Evan Mulligan, Nicola Curtin, Diane Wang, Raz Dewji, Antonello Abbattista, Jorge Gallo, Hilary Calvert. A phase II study of the potent PARP inhibitor, Rucaparib (PF-01367338, AG014699), with temozolomide in patients with metastatic melanoma demonstrating evidence of chemopotentiation.
Payel Chatterjee, Gaurav Choudhary, Warren D. Heston, Eric A. Klein, Alex Almasan. The PARP inhibitor rucaparib radiosensitizes prostate cancer cells, most effectively those that are PTEN-deficient and are expressing ETS gene fusion proteins, which inhibit NHEJ DNA repair. Cancer Research. 2012. 72: B27.
Chemical structure
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 421.36 |
| Cas No. | 459868-92-9 |
| Formula | C19H18FN3O·H3PO4 |
| Synonyms | Rucaparib phosphate,AG-14699,AG 014699 |
| Solubility | ≥21.08 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| Chemical Name | 8-fluoro-2-(4-((methylamino)methyl)phenyl)-4,5-dihydro-1H-azepino[5,4,3-cd]indol-6(3H)-one phosphate |
| SDF | Download SDF |
| Canonical SMILES | OP(O)(O)=O.FC1=CC2=C3C(CCNC2=O)=C(C4=CC=C(CNC)C=C4)NC3=C1 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
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APExBIO提供優質的胜肽和生物分析試劑，廣泛產品線如Protease、Chromatin/Epigenetics表觀遺傳學、MAPK Signal、DNA Damege/DNA repair、細胞凋亡、腫瘤生物學、Stem cell等研究領域， 還提供定制的服務，包括多肽合成，抗體的生產和檢測的發展。產品線DNA/RNA prep kit、Drug Screening panel、Bioactive peptides、Growth factors、Biotinylation Reagents、tag peptides、amino Acids、Growth factors等。APExBIO產品質量都伴隨著證書的分析，高效液相色譜，質譜，和HMNR數據。
| 品項 | CAS# | #貨號 | 應用 |
| Z-VAD-FMK | CAS# 187389-52-2 | 貨號 A1902 |
Proteases ICE-like proteases |
| TAPI-1 | CAS#171235-71-5 | 貨號 B4686 |
Proteases TACE/ADAM17 inhibitor Product Citation+3 |
| Talabostat mesylate | CAS# 150080-09-4 | 貨號B3941 |
Proteases DPP4 二肽基肽酶特異性抑制劑 |
| Z-IETD-FMK | CAS# 210344-98-2 | 貨號B3232 | inhibitor of caspase 8 |
| Cisplatin | CAS# 15663-27-1 | 貨號A8321 | 高效、廣譜的化療藥物 |
| 17-DMAG (Alvespimycin) HCl | CAS#467214-21-7 | 貨號A2213 | Hsp90 inhibitor |
| CA-074 Me | CAS# 147859-80-1 | 貨號A8239 | Cathepsin B inhibitor |
| VX-765 | CAS# 273404-37-8 | 貨號A8238 | Caspase-1 inhibitor |
| A4108 | Resminostat (RAS2410) | 864814-88-0 | 98.00% | Potent HDAC inhibitor |
| A4110 | MLN8237 (Alisertib) | 1028486-01-2 | 98.77% | Aurora A Kinase inhibitor, Potent and selective |
| A4111 | VX-680 (MK-0457,Tozasertib) | 639089-54-6 | 99.93% | Aurora kinase inhibitor |
| A4112 | Barasertib (AZD1152-HQPA) | 722544-51-6 | 98.25% | Aurora Kinase B inhibitor, Potent and selective |
| A4113 | ZM 447439 | 331771-20-1 | 98.80% | Aurora Kinase inhibitor,potent and selective |
| A4114 | MLN8054 | 869363-13-3 | 97.64% | Aurora A inhibitor |
| A4115 | JNJ-7706621 | 443797-96-4 | 98.11% | Potent CDK/Aurora kinase inhibitor |
| A4116 | Danusertib (PHA-739358) | 827318-97-8 | 99.39% | Pan-aurora kinase inhibitor |
| A4117 | AT9283 | 896466-04-9 | 99.29% | Aurora kinase/JAK inhibitor |
| A4118 | Hesperadin | 422513-13-1 | 98.29% | Aurora B kinase inhibitor |
| A4119 | AMG-900 | 945595-80-2 | 98.99% | Aurora kinase inhibitor |
| A4120 | MK-5108 (VX-689) | 1010085-13-8 | 96.91% | Aurora-A kinase inhibitor,highly selective |
| A4121 | SNS-314 Mesylate | 1146618-41-8 | 99.94% | Aurora A/B/C kinases inhibitor, potent and selective |
| A4122 | PHA-680632 | 398493-79-3 | 98.53% | Aurora kinase inhibitor,novel and potent |
| A4123 | KW 2449 | 1000669-72-6 | 99.94% | Multikinase inhibitor |
| A4124 | TAK-901 | 934541-31-8 | 98.00% | Novel Aurora A/B inhibitor |
| A4125 | CYC116 | 693228-63-6 | 98.71% | Potent Aurora A/B inhibitor |
| A4126 | Aurora A Inhibitor I | 1158838-45-9 | 98.83% | Aurora A inhibitor |
| A4127 | GSK1070916 | 942918-07-2 | 98.00% | Aurora B/C inhibitor |
| A4128 | PF-03814735 | 942487-16-3 | 98.00% | Aurora A/B inhibitor |
| A4129 | ENMD-2076 L-(+)-Tartaric acid | 1291074-87-7 | 99.36% | Aurora kinases inhibitor |
| A4130 | ENMD-2076 | 934353-76-1 | 98.78% | Selective Aurora A/Flt3 inhibitor |
| A4132 | CCT137690 | 1095382-05-0 | 98.00% | Aurora A/B/C inhibitor |
| A4135 | Tofacitinib (CP-690550) Citrate | 540737-29-9 | 99.64% | Potent JAK inhibitor |
| A4136 | TG101348 (SAR302503) | 936091-26-8 | 99.39% | JAK-2 inhibitor,potent and selective |
| A4137 | AZD1480 | 935666-88-9 | 99.31% | JAK2 inhibitor,ATP-competitive and novel |
| A4138 | Tofacitinib (CP-690550,Tasocitinib) | 477600-75-2 | 99.94% | Janus kinase inhibitor |
| A4139 | AG-490 | 133550-30-8 | 99.76% | JAK2/EGFR inhibitor |
| A4140 | WP1066 | 857064-38-1 | 99.84% | JAK2/STAT3 inhibitor,cell-permeable |
| A4141 | Baricitinib (LY3009104, INCB028050) | 1187594-09-7 | 98.06% | JAK1/JAK2 inhibitor,selective orally bioavailable |
| A4143 | CYT387 | 1056634-68-4 | 98.70% | JAK-1/-2 inhibitor,ATP competitive |
| A4144 | AZ 960 | 905586-69-8 | 98.00% | JAKs inhibitor |
| A4145 | TG101209 | 936091-14-4 | 99.46% | JAK2/3 inhibitor |
| A4146 | CEP-33779 | 1257704-57-6 | 98.00% | JAK2 inhibitor,highly selective |
| A4147 | LY2784544 | 1229236-86-5 | 98.00% | JAK2 inhibitor,highly potent and selective |
| A4148 | NVP-BSK805 2HCl | 1092499-93-8 (free base) | 99.23% | JAK2 inhibitor |
| A4149 | S-Ruxolitinib (INCB018424) | 941685-37-6 | 99.34% | JAK1/2 inhibitor,potent and selective |
| A4150 | WHI-P154 | 211555-04-3 | 99.19% | JAK3 inhibitor |
| A4151 | ZM 39923 HCl | 1021868-92-7 | 99.91% | JAK3 inhibitor,potent and selective |
| A4152 | BMS-911543 | 1271022-90-2 | 98.41% | JAK2 inhibitor,selective small molecule |
| A4153 | BMN 673 | 1207456-01-6 | 99.26% | Potent PARP inhibitor |
| A4154 | Olaparib (AZD2281, Ku-0059436) | 763113-22-0 | 99.80% | Potent PARP1/PARP2 inhibitor |
| A4156 | Rucaparib (AG-014699,PF-01367338) | 459868-92-9 | 98.46% | Potent PARP inhibitor |
| A4157 | Iniparib (BSI-201) | 160003-66-7 | 99.08% | PARP1 inhibitor,intravenously adminsitered |
| A4158 | AG-14361 | 328543-09-5 | 99.17% | Potent PARP1 inhibitor |
| A4159 | PJ34 hydrochloride | 344458-15-7 | 99.54% | PARP inhibitor,potent and cell-permeable |
| A4160 | A-966492 | 934162-61-5 | 99.03% | PARP-1/-2 inhibitor, highly potent |
| A4161 | 3-aminobenzamide | 3544-24-9 | 99.66% | Potent PARP inhibitor |
| A4163 | UPF 1069 | 1048371-03-4 | 98.00% | Selective PARP2 inhibitor |
| A4164 | AZD2461 | 1174043-16-3 | 98.00% | Novel PARP inhibitor |
| A4166 | EPZ5676 | 1380288-87-8 | 99.28% | DOT1L inhibitor,potent and SAM competitive |
| A4167 | SGC 0946 | 1561178-17-3 | 99.65% | DOT1L inhibitor,highly potent and selective |
| A4168 | Entacapone | 130929-57-6 | 99.28% | COMT inhibitor |
| A4170 | EPZ004777 | 1338466-77-5 | 99.43% | DOT1L inhibitor |
| A4171 | EPZ005687 | 1396772-26-1 | 98.66% | EZH2 inhibitor,potent and selective |
| A4176 | Thioguanine | 154-42-7 | 98.18% | Purine antimetabolite |
| A4180 | SRT1720 HCl | 1001645-58-4 | 99.52% | SIRT1 activator |
| A4181 | EX 527 (SEN0014196) | 49843-98-3 | 99.71% | SIRT1 inhibitor |
| A4182 | Resveratrol | 501-36-0 | 99.94% | SIRT1 activator |
| A4183 | Sirtinol | 410536-97-9 | 98.00% | SIRT inhibitor |
| A4184 | PFI-1 (PF-6405761) | 1403764-72-6 | 97.20% | BET inhibitor |
| A4186 | Bromosporine | 1619994-69-2 | 98.00% | Bromodomain inhibitor,non-selective |
| A4187 | FG-4592 (ASP1517) | 808118-40-3 | 99.92% | HIF prolyl-hydroxylase inhibitor |
| A4188 | 2-Methoxyestradiol (2-MeOE2) | 362-07-2 | 99.00% | Apoptotic, antiproliferative and antiangiogenic agent |
| A4189 | IOX2(Glycine) | 931398-72-0 | 98.10% | HIF-1α prolyl hydroxylase-2 (PHD2) inhibitor |
| A4190 | GSK J4 HCl | 1373423-53-0(free base) | 98.00% | Inhibitor of H3K27 demethylase JMJD3,potent and cell-permeable |
| A4191 | GSK J1 | 1373422-53-7 | 99.50% | H3K27 demethylase JMJD3 inhibitor |
| A4192 | SGI-1776 free base | 1025065-69-3 | 99.19% | Pim kinase inhibitor,ATP-competitive |
| A4193 | SMI-4a | 438190-29-5 | 99.76% | Potent Pim inhibitor |
| A4194 | Obatoclax mesylate (GX15-070) | 803712-79-0 | 98.49% | Potent Bcl-2 inhibitor |
| A4199 | Sabutoclax | 1228108-65-3 | 98.00% | pan-Bcl-2 inhibitor |
| A4200 | Apogossypolone (ApoG2) | 886578-07-0 | 98.00% | Bcl-2 inhibitor,nonpeptidic small molecule |
| A4202 | RITA (NSC 652287) | 213261-59-7 | 99.53% | Mdm2-p53 interaction and p53 ubiquitination blocking |
| A4203 | Tenovin-1 | 380315-80-0 | 99.90% | SIRT2 inhibitor, activates p53 |
| A4204 | JNJ-26854165 (Serdemetan) | 881202-45-5 | 98.35% | P53 activator, blocking Mdm2-p53 interaction |
| A4206 | Pifithrin-α (PFTα) | 63208-82-2 | 98.16% | p53 inhibitor |
| A4208 | NSC 319726 | 71555-25-4 | 98.00% | Reactivator of mutant p53 |
| A4209 | NSC 207895 (XI-006) | 58131-57-0 | 98.00% | MDMX inhibitor,anti-cancer agent |
| A4210 | Bay 11-7821 (BAY 11-7082) | 19542-67-7 | 99.91% | IKK/NF-κB/TNFα inhibitor |
| A4211 | Lenalidomide (CC-5013) | 191732-72-6 | 98.66% | Antineoplastic agent,inhibits angiogenesis |
| A4212 | Pomalidomide (CC-4047) | 19171-19-8 | 98.46% | Immunomodulator,antumor/anti-angiogenic |
| A4213 | Necrostatin-1 | 4311-88-0 | 99.88% | RIP1 inhibitor |
| A4216 | Thalidomide | 50-35-1 | 99.21% | Immunomodulatory agent,sedative drug,angiogenesis inhibitor |
| A4217 | QNZ (EVP4593) | 545380-34-5 | 99.41% | Potent NF-κB inhibitor |
| A4219 | Birinapant (TL32711) | 1260251-31-7 | 98.13% | Potent XIAP/cIAP1 antagonist |
| A4221 | YM155 | 781661-94-7 | 99.60% | Survivin suppressant,apoptosis inhibitor |
| A4224 | GDC-0152 | 873652-48-3 | 99.00% | IAP antagonist,potent amd samll-molecule |
| A4227 | Tipifarnib (Zarnestra) | 192185-72-1 | 99.18% | Farnesyltransferase inhibitor,potent and specific |
| A4228 | Nutlin-3 | 890090-75-2 | 98.35% | MDM2 antagonist,inhibits MDM2-p53 interaction |
| A4230 | NSC 66811 | 6964-62-1 | 98.00% | MDM2 inhibitor |
| A4232 | Cyclophosphamide monohydrate | 6055-19-2 | 98.00% | alkylating, cytotoxic agent,antitumor activity |
| A4233 | Methylprednisolone | 83-43-2 | 99.31% | Apoptosis inducer,GR agonist |
| A4234 | TW-37 | 877877-35-5 | 98.13% | Bcl-2 inhibitor, inhibits Bcl-2,Bcl-XL and Mcl-1 |
| A4237 | Amuvatinib (MP-470, HPK 56) | 850879-09-3 | 99.91% | Tyrosine kinase inhibitor |
| A4240 | Abiraterone | 154229-19-3 | 99.30% | Potent CYP17 inhibitor |
| A4300 | GW9662 | 22978-25-2 | 99.25% | PPARγ antagonist |
| A4301 | T0070907 | 313516-66-4 | 99.88% | Human PPARγ antagonist,potent and selective |
| A4302 | Rosiglitazone maleate | 155141-29-0 | 99.15% | PPARγ agonist,high-affinity and selective,potent insulin sensitizer |
| A4303 | GSK3787 | 188591-46-0 | 99.73% | PPARβ/δ antagonist,novel and irreversible |
| A4304 | Rosiglitazone | 122320-73-4 | 99.80% | Potent PPARγ agonist |
| A4305 | WY-14643 (Pirinixic Acid) | 50892-23-4 | 99.87% | PPARα agonist,selective and highly potent |
| A4306 | Ciprofibrate | 52214-84-3 | 98.88% | PPARα agonist |
| A4307 | GW0742 | 317318-84-6 | 99.64% | PPARδ/β agonist,potent and selective |
| A4308 | Alizarin | 72-48-0 | 98.03% | Chelator for calcium,used to stain calcium deposites,Alizarin complexone is used for bone staining to study bone remodeling |
| A4309 | GW501516 | 317318-70-0 | 98.27% | PPARδ agonist,selective and potent |
| A4310 | Rosiglitazone HCl | 302543-62-0 | 99.31% | PPARγ agonist |
| A4311 | PF-4981517 | 1390637-82-7 | 98.00% | CYP3A4 inhibitor,potent and selective |
| A4313 | Cobicistat (GS-9350) | 1004316-88-4 | 99.94% | Selective CYP3A inhibitor |
| A4316 | Ketoconazole | 65277-42-1 | 99.48% | Inhibitor of cyclosporine oxidase and testosterone 6 beta-hydroxylase |
| A4317 | Apremilast (CC-10004) | 608141-41-9 | 98.98% | PDE4 inhibitor |
| A4318 | Avasimibe | 166518-60-1 | 99.66% | ACAT inhibitor,orally bioavailable |
| A4319 | Roflumilast | 162401-32-3 | 99.08% | PDE-4 inhibitor |
| A4320 | Voriconazole | 137234-62-9 | 99.96% | CYP51 inhibitor |
| A4321 | Sildenafil Citrate | 171599-83-0 | 99.63% | Treat erectile dysfunction and PAH |
| A4322 | Clarithromycin | 81103-11-9 | 99.39% | CYP3A inhibitor, potent |
| A4323 | Vardenafil HCl Trihydrate | 330808-88-3 | 99.63% | PDE5 inhibitor, potent and selective |