Picoplatin
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MedKoo CAT#: 202230

CAS#: 181630-15-9

Description: Picoplatin is a new generation organic platinum analog with an extended spectrum of antineoplastic activity. Designed to overcome platinum drug resistance, picoplatin alkylates DNA, forming both inter- and intra-strand cross-linkages, resulting in inhibition of DNA replication and transcription, and the induction of apoptosis.


Chemical Structure

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Picoplatin
CAS# 181630-15-9

Theoretical Analysis

MedKoo Cat#: 202230
Name: Picoplatin
CAS#: 181630-15-9
Chemical Formula: C6H10Cl2N2Pt
Exact Mass:
Molecular Weight: 376.15
Elemental Analysis: C, 19.16; H, 2.68; Cl, 18.85; N, 7.45; Pt, 51.86

Price and Availability

Size Price Availability Quantity
5.0mg USD 675.0 2 Weeks
10.0mg USD 1100.0 2 Weeks
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Synonym: AMD473; AMD 473; AMD-473; NX 473; NX473; NX-473; ZD0473; ZD-0473; ZD 0473; Picoplatin.

IUPAC/Chemical Name: Cis-Amminedichloro (2-Methylpyridine) Platinum.

InChi Key: IIMIOEBMYPRQGU-UHFFFAOYSA-L

InChi Code: InChI=1S/C6H7N.2ClH.H3N.Pt/c1-6-4-2-3-5-7-6;;;;/h2-5H,1H3;2*1H;1H3;/q;;;;+2/p-2

SMILES Code: CC1=NC=CC=C1.Cl[Pt]Cl.N

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not soluble in water.

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 376.15 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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 1: Wheate NJ, Walker S, Craig GE, Oun R. The status of platinum anticancer drugs in the clinic and in clinical trials. Dalton Trans. 2010 Jun 30. [Epub ahead of print] PubMed PMID: 20593091.

2: Margiotta N, Denora N, Ostuni R, Laquintana V, Anderson A, Johnson SW, Trapani G, Natile G. Platinum(II) complexes with bioactive carrier ligands having high affinity for the translocator protein. J Med Chem. 2010 Jul 22;53(14):5144-54. PubMed PMID: 20568783.

3: More SS, Li S, Yee SW, Chen L, Xu Z, Jablons DM, Giacomini KM. Organic cation transporters modulate the uptake and cytotoxicity of picoplatin, a third-generation platinum analogue. Mol Cancer Ther. 2010 Apr;9(4):1058-69. Epub 2010 Apr 6. PubMed PMID: 20371711.

4: Olszewski U, Hamilton G. A better platinum-based anticancer drug yet to come? Anticancer Agents Med Chem. 2010 May 1;10(4):293-301. Review. PubMed PMID: 20187870.

5: Eckardt JR, Bentsion DL, Lipatov ON, Polyakov IS, Mackintosh FR, Karlin DA, Baker GS, Breitz HB. Phase II study of picoplatin as second-line therapy for patients with small-cell lung cancer. J Clin Oncol. 2009 Apr 20;27(12):2046-51. Epub 2009 Mar 16. PubMed PMID: 19289620.

6: Shah N, Dizon DS. New-generation platinum agents for solid tumors. Future Oncol. 2009 Feb;5(1):33-42. Review. PubMed PMID: 19243296.

7: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2008 Oct;30(8):643-72. PubMed PMID: 19088949.

8: Tomillero A, Moral MA. Gateways to clinical trials. July-August 2008. Methods Find Exp Clin Pharmacol. 2008 Jul-Aug;30(6):459-95. PubMed PMID: 18850047.

9: Teicher BA. Newer cytotoxic agents: attacking cancer broadly. Clin Cancer Res. 2008 Mar 15;14(6):1610-7. Review. PubMed PMID: 18347161.



Additional Information

 
Picoplatin is a new generation platinum chemotherapy agent that has an improved safety profile compared to existing platinum-based chemotherapeutics and was designed to overcome platinum resistance. Picoplatin has been evaluated in approximately 1100 patients and has demonstrated activity in multiple indications with no evidence of significant kidney, nerve toxicity or hearing loss. (Source: Poniard's website).
 
Picoplatin is a cytotoxic platinum compound in clinical development by Poniard Pharmaceuticals (previously NeoRx) for the treatment of patients with solid tumors. In Phase I and Phase II clinical trials, picoplatin demonstrated activity in a variety of solid tumors, including lung, ovarian, colorectal and hormone-refractory prostate cancer. However, in Phase III trials, picoplatin failed to hit its primary endpoint for advanced small cell lung cancer. Hopes are now pinned on its use for metastatic colorectal cancer. (source: wikipedia.com).