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PF-01367338

Basic information Safety Supplier Related

PF-01367338 Basic information

Product Name:
PF-01367338
Synonyms:
  • 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
CAS:
459868-92-9
MF:
C19H21FN3O5P
MW:
421.37
Product Categories:
  • Inhibitors
  • Inhibitor
  • Amines
  • Aromatics
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
Mol File:
459868-92-9.mol
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PF-01367338 Chemical Properties

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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PF-01367338 Usage And Synthesis

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

References

1) Thomas?et al.?(2007),?Preclinical selection of a n novel poly(ADP-ribose) polymerase inhibitor for clinical trial; Mol. Cancer Ther.,?6?945 2) Drew?et al.?(2011),?Therapeutic potential of poly(ADP-ribose) polymerase inhibitor AG014699 in human cancers with mutated or methylated BRCA1 or BRCA2; J. Natl. Cancer Inst.,?103?334 3) Ihnen?et al.?(2013),?Therapeutic potential of the poly(ADP-ribose) polymerase inhibitor rucaparib for the treatment of sporadic human ovarian cancer; Mol. Cancer Ther.,?12?1002 4) Plummer?et al.?(2013),?A phase II study of the potent PARP inhibitor, Rucaparib (PF-01367338, AG014699), with temozolomide in patients with metastatic melanoma demonstrating evidence of chemopotentiation; Cancer Chemother. Pharmacol.,?71?1191 5) Ali?et al.?(2011),?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; Mol. Cancer Ther.,?10?2320

PF-01367338Supplier

Shanghai Boyle Chemical Co., Ltd.
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Chembest Research Laboratories Limited
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021-20908456
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JinYan Chemicals(ShangHai) Co.,Ltd.
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13817811078
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WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
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027-65522453
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Chemsky (shanghai) International Co.,Ltd
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021-50135380
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shchemsky@sina.com