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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PF-01367338 Suppliers

Canada 1 China 213 India 4 The Netherlands 1 United States 20 Global 239
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
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2922
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Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6003
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61
JinYan Chemicals(ShangHai) Co.,Ltd.
Tel
13817811078
Fax
86-021-50426522,50426273
Email
sales@jingyan-chemical.com
Country
China
ProdList
9976
Advantage
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WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
Tel
17702719238 18971495150;
Email
sales@sun-shinechem.com
Country
China
ProdList
1077
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64
Chemsky (shanghai) International Co.,Ltd
Tel
021-50135380
Email
shchemsky@sina.com
Country
China
ProdList
15402
Advantage
60
Shanghai Feibo Chemical Technology Co., Ltd
Tel
021-58955608,2250286 15921236618
Email
blinkzeng@gmail.com
Country
China
ProdList
522
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62
Synches Co., Ltd.
Tel
021-53292253
Fax
021-53292253
Email
biz@synches.com
Country
China
ProdList
199
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Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4747
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Shanghai PharmaChem CO.,Ltd.
Tel
13621878384
Fax
13621878384
Email
wm_pharchem@163.com
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China
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NCE Biomedical Co.,Ltd.
Tel
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
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+86-27-87599188
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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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