459868-92-9
8-Fluoro-2-[4-(methylaminomethyl)phenyl]-3,4,5,6-tetrahydro-1H-azepino[5,4,3-cd]indol-6-one phosphate
CAS: 459868-92-9
Molecular Formula: C19H21FN3O5P
459868-92-9 - Names and Identifiers
| Name | 8-Fluoro-2-[4-(methylaminomethyl)phenyl]-3,4,5,6-tetrahydro-1H-azepino[5,4,3-cd]indol-6-one phosphate |
| Synonyms | CS-47 AG-14699 AG014699 AG-014699 PF-01367338 RUCAPARIB PHOSPHATE PF01367338 phosphate Rucaparib phosphate salt AG-014447 (as free base) Rucaparib (AG-014699) phosphate Rucaparib phosphate (AG-14699, PF-01367338) Rucaparib (AG-014699,PF-01367338) phosphate Rucaparib (phosphate)(AG-014699,PF-01367338) 8-Fluoro-2-[4-(methylaminomethyl)phenyl]-3,4,5,6-tetrahydro-1H-azepino[5,4,3-cd]indol-6-one phosphate 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one phosphate |
| CAS | 459868-92-9 |
| InChI | InChI=1/C19H18FN3O.H3O4P/c1-21-10-11-2-4-12(5-3-11)18-14-6-7-22-19(24)15-8-13(20)9-16(23-18)17(14)15;1-5(2,3)4/h2-5,8-9,21,23H,6-7,10H2,1H3,(H,22,24);(H3,1,2,3,4) |
459868-92-9 - Physico-chemical Properties
| Molecular Formula | C19H21FN3O5P |
| Molar Mass | 421.37 |
| Melting Point | >173°C (dec.) |
| Boling Point | 625.2°C at 760 mmHg |
| Flash Point | 331.9°C |
| Solubility | Soluble in DMSO (up to 25 mg/ml). |
| Vapor Presure | 1.5E-15mmHg at 25°C |
| Appearance | Yellow solid. |
| Color | Yellow |
| Storage Condition | Sealed in dry,Room Temperature |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| Use | Rucaparib (AG-014699,PF-01367338) is a PARP inhibitor. The Ki acting on PARP1 is 1.4 nM, and it also has binding affinity for the remaining 8 PARP sites. Phase 3. |
| In vitro study | AG-014699 effectively inhibited purified full-length human PARP-1 and showed a strong PARP inhibitory effect on LoVo and SW620 cells. AG-014699 is the phosphate form of AG14447 and is the first PARP inhibitor used in clinical trials in combination with temozolomide. The radiosensitization of AG-014699 is due to inhibition of downstream NF-κB activation, and inhibition of SSB repair. AG-014699 acts on DNA damage-activated NF-κB and overcomes the toxicity of conventional NF-κB inhibitors without compromising other important inflammatory responses. 1 μm AG-014699 inhibited PARP-1 of the activity in D283Med cells by 97.1%. AG-014699 significantly enhanced the cytotoxicity of Topotecan and Temozolomide in NB-1691, SH-SY-5Y, and SKNBE(2c) cells. |
| In vivo study | AG-014699 is non-toxic and significantly enhances TGD induced by temozoloride in DNA repair functional protein of D384Med transplanted tumor. Pharmacokinetic studies showed that AG-014699 was also detected in brain tissue, indicating that AG-014699 has potential for the treatment of intracranial malignant tumors. In vivo models (NB1691 and SHSY5Y xenograft tumors) studies have shown that AG-014699 enhances the anti-cancer activity of temozolomide, resulting in complete and long-lasting tumor regression. |
459868-92-9 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.373 ml | 11.866 ml | 23.733 ml |
| 5 mM | 0.475 ml | 2.373 ml | 4.747 ml |
| 10 mM | 0.237 ml | 1.187 ml | 2.373 ml |
| 5 mM | 0.047 ml | 0.237 ml | 0.475 ml |
Last Update：2024-01-02 23:10:35
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View History
459868-92-9
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C.I. Solvent Green 1, acetate salt
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Vitamin B
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Tricresyl phosphate