ChemicalBook > CAS DataBase List > PF-01367338

PF-01367338

Product Name: PF-01367338
CAS No.: 459868-92-9
Chemical Name: PF-01367338
Synonyms: CS-47;Rubraca;AG14699;AG-014699;PF-01367338;Rucaparib(AG-01);Rucaparib D4 HCl;AG014699 phosphate;AG 014699 phosphate;AG-014699 phosphate
CBNumber: CB82515928
Molecular Formula: C19H21FN3O5P
Formula Weight: 421.37
MOL File: 459868-92-9.mol

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PF-01367338 Property

Melting point:: >173°C (dec.)
storage temp.: Sealed in dry,Room Temperature
solubility: Soluble in DMSO (up to 25 mg/ml).
form: Yellow solid.
color: Yellow
Stability:: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H226Flammable liquid and vapour

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P210Keep away from heat/sparks/open flames/hot surfaces. — No smoking.

P233Keep container tightly closed.

P240Ground/bond container and receiving equipment.

P241Use explosion-proof electrical/ventilating/lighting/…/equipment.

P242Use only non-sparking tools.

P243Take precautionary measures against static discharge.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P303+P361+P353IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P370+P378In case of fire: Use … for extinction.

P403+P235Store in a well-ventilated place. Keep cool.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 11570
Product name: Rucaparib (phosphate)
Purity: ≥98%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 11570
Product name: Rucaparib (phosphate)
Purity: ≥98%
Packaging: 5mg
Price: $139
Updated: 2024/03/01

Cayman Chemical

Product number: 11570
Product name: Rucaparib (phosphate)
Purity: ≥98%
Packaging: 10mg
Price: $243
Updated: 2024/03/01

TRC

Product number: A425500
Product name: AG14699
Packaging: 5mg
Price: $90
Updated: 2021/12/16

TRC

Product number: A425500
Product name: AG14699
Packaging: 10mg
Price: $140
Updated: 2021/12/16

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PF-01367338 Chemical Properties,Usage,Production

Description

Rucaparib phosphate (459868-92-9) is a potent (Ki<5 nM) PARP1 inhibitor.1?Cytotoxic to human cancer cells or xenograft tumors with mutated or epigenetically silenced BRCA1/2.2?Demonstrates antiproliferative effects in 26 out of 39 ovarian cancer cell lines.3?Synergizes with other anticancer agents such as topotecan, carboplatin, doxorubicin, paclitaxel,3 and temozolomide.4?Ameliorates the cardiotoxicity of doxorubicin.5?Recently approved for human use by the FDA.

Uses

PARP inhibitor oncolytic

in vivo

Rucaparib (AG014699) phosphate and AG14584 significantly increase Temozolomide toxicity. Rucaparib (1 mg/kg) phosphate significantly increases Temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) phosphate results in a 50% increase in the temozolomide-induced tumor growth delay^[1].
Rucaparib (10 mg/kg for i.p. or 50, 150 mg/kg for p.o.; daily for 5 days per week for 6 weeks) phosphate significantly inhibits the growth of the tumor, and there is one complete tumor regression and two persistent partial regressions^[2].
Rucaparib (150 mg/kg; p.o.; once per week for 6 weeks or three times per week for 6 weeks) phosphate has greatest antitumor effect with three complete regressions^[2].
Rucaparib phosphate enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts^[6].

Animal Model:	Female athymic nude mice, implanted SW620 colorectal tumor cells (1 × 10⁷ cells per animal) s.c.^[1]
Dosage:	0.1 mg/kg in combination with Temozolomide (p.o., 200 mg/kg), 0.05, 0.15, and 0.5 mg/kg in combination with Temozolomide (p.o., 68 mg/kg) or 10 mg/kg
Administration:	IP, single dose for 0.1 mg/kg and 10 mg/kg, five daily doses for 0-0.5 mg/kg
Result:	Significantly increased Temozolomide toxicity, showed outstanding chemosensitization potency and caused enhancement of Temozolomide-induced tumor growth delay

Animal Model:	CD-1 nude mice bearing established Capan-1 xenografts^[2]
Dosage:	10 mg/kg or 50, 100 and 150?mg/kg
Administration:	IP for 10 mg/kg; PO for 50, 100 and 150?mg/kg, single dose (Pharmacokinetics)
Result:	Parent drug was detectable in the plasma only at 30?min after 10?mg/kg i.p and up to 4?h for 50–150?mg/kg p.o.. Was still detectable in most mice receiving oral rucaparib at 3 days. Does not easily cross the plasma membrane.

Animal Model:	CD-1 nude mice bearing established Capan-1 xenografts^[2]
Dosage:	10?mg/kg i.p. daily for 5 days per week for 6 weeks, 50 or 150?mg/kg p.o. daily × five weekly × six, 150?mg/kg p.o. once per week for 6 weeks or three times per week for 6 weeks, or 150?mg/kg p.o. daily for five days every 3 weeks
Administration:	IP or PO
Result:	10?mg/kg i.p. significantly inhibited the growth of the tumor, daily oral administration at 150?mg/kg had an equivalent effect on tumor growth to 10?mg/kg i.p.. The schedule with the greatest antitumor effect was oral administration of 150?mg/kg on a once weekly schedule with three complete regressions.

Animal Model:	CD-1 nude mice, NB1691 and SHSY5Y xenografts^[6]
Dosage:	1 mg/kg
Administration:	IP, daily for 5 d in combination with Temozolomide (orally daily ×5 at a dose of 68 mg/kg)
Result:	Enhanced the antitumor activity of Temozolomide and indicated complete and sustained tumor regression.

IC 50

PARP-1: 1.4 nM (Ki); PARP-2; PARP-3

References

[1] HUW D THOMAS. Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial.[J]. Molecular Cancer Therapeutics, 2007, 6 3: 945-956. DOI:10.1158/1535-7163.mct-06-0552
[2] YVETTE DREW. Therapeutic potential of poly(ADP-ribose) polymerase inhibitor AG014699 in human cancers with mutated or methylated BRCA1 or BRCA2.[J]. JNCI Journal of the National Cancer Institute, 2011, 103 4: 334-346. DOI:10.1093/jnci/djq509
[3] MAIKE IHNEN. Therapeutic potential of the poly(ADP-ribose) polymerase inhibitor rucaparib for the treatment of sporadic human ovarian cancer.[J]. Molecular Cancer Therapeutics, 2013, 12 6: 1002-1015. DOI:10.1158/1535-7163.mct-12-0813
[4] RUTH PLUMMER. A phase II study of the potent PARP inhibitor, Rucaparib (PF-01367338, AG014699), with temozolomide in patients with metastatic melanoma demonstrating evidence of chemopotentiation.[J]. Cancer Chemotherapy and Pharmacology, 2013, 71 5: 1191-1199. DOI:10.1007/s00280-013-2113-1
[5] MAJID ALI. The clinically active PARP inhibitor AG014699 ameliorates cardiotoxicity but does not enhance the efficacy of doxorubicin, despite improving tumor perfusion and radiation response in mice.[J]. Molecular Cancer Therapeutics, 2011, 10 12: 2320-2329. DOI:10.1158/1535-7163.mct-11-0356

PF-01367338 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from PF-01367338 manufacturers

Hebei Chuanghai Biotechnology Co., Ltd

Product: Rucaparib 459868-92-9
Price: US $0.00-0.00/KG
Min. Order: 1KG
Purity: 99%
Supply Ability: 500000kg
Release date: 2023-04-06

Henan Aochuang Chemical Co.,Ltd.

Product: Rucaparib phosphate;PF01367338 phosphate 459868-92-9
Price: US $0.00-0.00/kg
Min. Order: 1kg
Purity: 98%
Supply Ability: 1Ton
Release date: 2022-09-30

Baoji Guokang Healthchem co.,ltd

Product: ;Rucaparib 459868-92-9
Price: US $206.30/g
Min. Order: 1g
Purity: 99%
Supply Ability: 1000G
Release date: 2021-06-08

459868-92-9, PF-01367338Related Search:

Olaparib Rucaparib Camsylate 2-bromo-8-fluoro-4,5-dihydro-1H-azepino[5,4,3-cd]indol-6(3H)-one 4-AMINO-1,8-NAPHTHALIMIDE 3-Aminobenzamide NU1025 1H-BenziMidazole, 4-fluoro-2-Methyl-1-(1-Methylethyl)-6-(4,4,5,5-tetraMethyl-1,3,2-dioxaborolan-2-yl)- 6-Bromo-4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole 5-((4-Ethylpiperazin-1-yl)methyl)pyridin-2-amine 4-(8-fluoro-6-oxo-3,4,5,6-tetrahydro-1H-azepino[5,4,3-cd]indol-2-yl)benzaldehyde Everolimus MK-2206 2HCl Talazoparib (BMN 673) Veliparib Rapamycin ABT-888 Ruxolitinib Rucaparib

PF01367338 phosphate

Rucaparib (AG-014699,PF-01367338) phosphate

Rucaparib (AG-014699) phosphate

AG014699;RUCAPARIB PHOSPHATE

Rucaparib (phosphate)(AG-014699,PF-01367338)

Rucaparib phosphate salt

Rucaparib phosphate (AG-14699, PF-01367338)

CS-47

AG 014699 - PF 01367338 | Rucaparib

AG-014447 (as free base)

AG-14699 (as phosphate salt)

AG-14699 (AS PHOSPHATE SALT); AG-014447 (AS FREE BASE); RUCAPARIB; PF-01367338; AG014699;

AG 014699 phosphate

AG014699 phosphate

AG-014699 phosphate

RUCAPARIB PHOSPHATE;AG014699 PHOSPHATE;PF01367338 PHOSPHATE;AG 014699 PHOSPHATE;PF 01367338 PHOSPHATE;AG-014699 PHOSPHATE;PF-01367338 PHOSPHATE

AG14699 (AS PHOSPHATE SALT); AG 14699; AG-14699; AG014447 (AS FREE BASE); AG-014447; AG 014447; PF01367338; PF-01367338; PF 01367338; RUCAPARIB; RUBRACA;

Rubraca

AG-014699

AG-014699;PF-01367338

PF-01367338

AG14699

8-Fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-6H-pyrrolo[4,3,2-ef][2]benzazepin-6-one phosphate

Rucaparib (AG-014699 , PF-01367338)

Rucaparib phosphate

AG-014699 (Rucaparib)

6H-Pyrrolo[4,3,2-ef][2]benzazepin-6-one, 8-fluoro-1,3,4,5-tetrahydro-2-[4-[(MethylaMino)Methyl]phenyl]-, phosphate (1:1)

PF-01367338/AG14699

Rucaparib(AG-014699)

8-fluoro-5-(4-((methylamino)methyl)phenyl)-3,4-dihydro-2H-azepino[5,4,3-cd]indol-1(6H)-one phosphoric acid

8-Fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-6H-pyrrolo[4,3,2-ef][2]benzazepin-6-one phosphate Rucaparib(AG-014699)

AG 014699 8-Fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-6H-pyrrolo[4,3,2-ef][2]benzazepin-6-one phosphate

Rucaparib ( PF-01367338)

Rucaparib phosphate AG-014699

8-Fluoro-2-(4-((methylamino)methyl)phenyl)-4,5-dihydro-1H-azepino[5,4,3-cd]indol-6(3H)-one phosphate

Rucaparib(AG-01)

8-fluoro-5-(4-((methylamino)methyl)phenyl)-2,3,4,6-tetrahydro-1H-azepino[5,4,3-cd]indol-1-onephosphate

8-Fluoro-2-(4-((methylamino)methyl)phenyl)-4,5-dihydro-1H-azepino[5,4,3-cd]indol-6(3H)-one pho

PF-01367338 USP/EP/BP

Rucaparib D4 HCl

TIANFUCHEM--PF-01367338

Rucaparib Phosphate, 10 mM in DMSO

459868-92-9

C19H21FN3O5P

C19H18FN3OH3PO4

C19H18FN3OH3O4P

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Inhibitor

Amines

Aromatics

Heterocycles

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