What is the 8-FLUOR-2-{4-[(METHYLAMINO)METHYL]FENYL}-1,3,4,5-TETRAHYDRO-6HAZEPINO[5,4,3-CD]INDOOL-6-ON?

8-FLUOR-2-{4-[(METHYLAMINO)METHYL]FENYL}-1,3,4,5-TETRAHYDRO-6HAZEPINO[5,4,3-CD]INDOOL-6-ON is , while it's Molecular Formula is C19H18FN3O. Rucaparib is PARP1 inhibitor. It can be used in biological study of chemical screening to identify drugs that enhance or mitigate cellular responses to antibody-toxin fusion proteins using human B cell precursor leukemia cells and cervical adenocarcinoma cells.

What is the CAS number for 8-FLUOR-2-{4-[(METHYLAMINO)METHYL]FENYL}-1,3,4,5-TETRAHYDRO-6HAZEPINO[5,4,3-CD]INDOOL-6-ON?

The CAS number of 8-FLUOR-2-{4-[(METHYLAMINO)METHYL]FENYL}-1,3,4,5-TETRAHYDRO-6HAZEPINO[5,4,3-CD]INDOOL-6-ON is 283173-50-2.

What is 8-FLUOR-2-{4-[(METHYLAMINO)METHYL]FENYL}-1,3,4,5-TETRAHYDRO-6HAZEPINO[5,4,3-CD]INDOOL-6-ON (283173-50-2) used for?

Poly(ADP-ribose) polymerases (PARPs) are activated by DNA single- and double-strand breaks and promote repair of DNA damage through the relaxation of chromatin and recruitment of other repair proteins. Inhibition of PARP activity has been linked to synthetic lethality in cells with mutations in BRCA1 or BRCA2 and is used as a therapeutic strategy to selectively target cancers. Rucaparib is a potent, cell-permeable inhibitor of PARP1 (Ki = <5 nM) that is used in clinical therapy to sensitize cancer cells to chemotherapy. Rucaparib inactivates PARP activity in cells with homologous recombination DNA repair pathway mutations at LC50 values ranging from 1.3-5.5 μM. At 25 mg/kg, rucaparib arrests tumor growth in mice bearing epigenetically silenced BRCA1 UACC3199 xenograft tumors. It has been shown to increase efficacy of temozolomide in medulloblastoma cells and xenografts.

What is the 8-FLUOR-2-{4-[(METHYLAMINO)METHYL]FENYL}-1,3,4,5-TETRAHYDRO-6HAZEPINO[5,4,3-CD]INDOOL-6-ON?

8-FLUOR-2-{4-[(METHYLAMINO)METHYL]FENYL}-1,3,4,5-TETRAHYDRO-6HAZEPINO[5,4,3-CD]INDOOL-6-ON is , while it's Molecular Formula is C19H18FN3O. Rucaparib is PARP1 inhibitor. It can be used in biological study of chemical screening to identify drugs that enhance or mitigate cellular responses to antibody-toxin fusion proteins using human B cell precursor leukemia cells and cervical adenocarcinoma cells.

What is the CAS number for 8-FLUOR-2-{4-[(METHYLAMINO)METHYL]FENYL}-1,3,4,5-TETRAHYDRO-6HAZEPINO[5,4,3-CD]INDOOL-6-ON?

The CAS number of 8-FLUOR-2-{4-[(METHYLAMINO)METHYL]FENYL}-1,3,4,5-TETRAHYDRO-6HAZEPINO[5,4,3-CD]INDOOL-6-ON is 283173-50-2.

What is 8-FLUOR-2-{4-[(METHYLAMINO)METHYL]FENYL}-1,3,4,5-TETRAHYDRO-6HAZEPINO[5,4,3-CD]INDOOL-6-ON (283173-50-2) used for?

Poly(ADP-ribose) polymerases (PARPs) are activated by DNA single- and double-strand breaks and promote repair of DNA damage through the relaxation of chromatin and recruitment of other repair proteins. Inhibition of PARP activity has been linked to synthetic lethality in cells with mutations in BRCA1 or BRCA2 and is used as a therapeutic strategy to selectively target cancers. Rucaparib is a potent, cell-permeable inhibitor of PARP1 (Ki = <5 nM) that is used in clinical therapy to sensitize cancer cells to chemotherapy. Rucaparib inactivates PARP activity in cells with homologous recombination DNA repair pathway mutations at LC50 values ranging from 1.3-5.5 μM. At 25 mg/kg, rucaparib arrests tumor growth in mice bearing epigenetically silenced BRCA1 UACC3199 xenograft tumors. It has been shown to increase efficacy of temozolomide in medulloblastoma cells and xenografts.

Product Class

283173-50-2

Product Name：Rucaparib
Molecular Formula：C₁₉H₁₈FN₃O
Purity：99%
Molecular Weight：323.37

Inquiry

Product Details:

CasNo： 283173-50-2

Molecular Formula： C₁₉H₁₈FN₃O

Quality Manufacturer Supply Rucaparib,Export 283173-50-2 Efficient Transportation

Molecular Formula:C19H18FN3O
Molecular Weight:323.37
Boiling Point:625.248 °C at 760 mmHg
PKA:14.10±0.20(Predicted)
Flash Point:331.938 °C
PSA：56.92000
Density:1.281 g/cm³
LogP:3.69900

Rucaparib (Cas 283173-50-2) Usage

Description

Rucaparib is a first-in-class pharmaceutical drug that targets the DNA repair enzyme poly-ADP ribose polymerase-1 (PARP-1). It belongs to the class of PARP inhibitors, which work by blocking the activity of PARP enzymes involved in repairing damaged DNA in cancer cells. By inhibiting PARP, rucaparib prevents cancer cells from repairing DNA damage, leading to their death.

Uses

Rucaparib is approved for various indications related to the treatment of ovarian cancer:

Maintenance therapy: Rucaparib is indicated as maintenance treatment for patients with recurrent high-grade ovarian cancer, fallopian tube cancer, or primary peritoneal cancer who have responded to platinum-based chemotherapy. It is specifically used in patients with certain types of inherited (germline) or acquired (somatic) abnormal BRCA genes.

Treatment of BRCA-mutated ovarian cancer: Rucaparib is approved for the treatment of adult patients with BRCA-mutated ovarian cancer who have received two or more lines of chemotherapy.

Maintenance therapy after platinum-based chemotherapy: Rucaparib is also indicated as maintenance therapy for adult patients with recurrent or relapsed ovarian cancer who have achieved complete or partial response to platinum-based chemotherapy.

283173-50-2 Relevant articles

Stereospecific PARP Trapping by BMN 673 and Comparison with Olaparib and Rucaparib

J Murai，SYN Huang，A Renaud，Y Zhang，J Ji，S Takeda，J Morris，B Teicher，JH Doroshow，Y Pommier

, Molecular Cancer Therapeutics, 2014

Here, we evaluated the novel PARP inhibitor, BMN 673, and compared its effects on PARP1 and PARP2 with two other clinical PARP inhibitors, olaparib and rucaparib, using biochemical and cellular assays in genetically modified chicken DT40 and human cancer cell lines. Although BMN 673, olaparib, and rucaparib are comparable at inhibiting PARP catalytic activity..

Results of ARIEL2: A Phase 2 trial to prospectively identify ovarian cancer patients likely to respond to rucaparib using tumor genetic analysis

Iain A. McNeish，Amit M. Oza，RL Coleman，Clare L. Scott，Elizabeth M. Swisher

, Journal of Clinical Oncology 2015/05/20

Ovarian cancer remains the most lethal gynecologic malignancy. Although standard platinum-based chemotherapy results in high response rates, more than 70% of patients...

Therapeutic Potential of the Poly(ADP-ribose) Polymerase Inhibitor Rucaparib for the Treatment of Sporadic Human Ovarian Cancer

Maike Ihnen; Christine zu Eulenburg; Teodora Kolarova; Jing Wei Qi; Kanthinh Manivong; Meenal Chalukya; Judy Dering; Lee Anderson; Charles Ginther; Alexandra Meuter; Boris Winterhoff; Siân Jones; Victor E. Velculescu; Natarajan Venkatesan; Hong-Mei Rong; Sugandha Dandekar; Nitin Udar; Fritz Jänicke; Gerrit Los; Dennis J. Slamon; Gottfried E. Konecny

CANCER THERAPEUTICS INSIGHTS| JUNE 09 2013

Drug interactions with rucaparib were synergistic for topotecan, synergistic, or additive for carboplatin, doxorubicin or paclitaxel, and additive for gemcitabine. Synergy was most pronounced when rucaparib was combined with topotecan, which resulted in enhanced apoptosis, DNA fragmentation, and γH2AX formation.

283173-50-2 Process route

: C₁₉H₁₆FN₃O

: 283173-50-2
Rucaparib

Conditions

Conditions	Yield
C₁₉H₁₆FN₃O; With sodium tetrahydroborate; In ethanol; for 1h; With sodium hydroxide; In water; at 10 ℃; for 2h;	90.83%
With palladium 10% on activated carbon; hydrogen; for 12h; Reagent/catalyst;	84%
Multi-step reaction with 2 steps 1.1: sodium tetrahydroborate / methanol; tetrahydrofuran / 3 h / 0 - 20 °C / Large scale 1.2: 1 h / Large scale 1.3: 18 h / Large scale 2.1: sodium hydroxide / methanol; water; tetrahydrofuran / 18 h / 20 °C / Large scale With sodium tetrahydroborate; sodium hydroxide; In tetrahydrofuran; methanol; water;
Multi-step reaction with 2 steps 1.1: sodium tetrahydroborate; methanol / tetrahydrofuran / 2 h / 0 - 20 °C 1.2: 2 h 2.1: sodium hydroxide / water; methanol / 12 h / 0 - 5 °C With methanol; sodium tetrahydroborate; sodium hydroxide; In tetrahydrofuran; methanol; water;

: 880160-69-0
[4-(8-fluoro-6-oxo-3,4,5,6-tetrahydro-1H-azepino[5,4,3-cd]indol-2-yl)-benzyl]-methyl-carbamic acid methyl ester

: 283173-50-2
Rucaparib