LOBAPLATIN

Product NameLOBAPLATIN
CAS135558-11-1
MFC9H18N2O3Pt
MW397.33
EINECS604-604-1
MOL File135558-11-1.mol

Chemical Properties

Melting point	220° (dec)
storage temp.	Store at -20°C
solubility	Water: ≥ 50 mg/mL (125.84 mM; DMSO can inactivate Lobaplatin's activity)
form	Solid
color	White to off-white
Water Solubility	Water: ≥ 50 mg/mL (125.84 mM; DMSO can inactivate Lobaplatin's activity)
InChI	1S/C6H12N2.C3H5O3.Pt/c7-3-5-1-2-6(5)4-8;1-2(4)3(5)6;/h5-8H,1-4H2;2H,1H3,(H,5,6);/q-2;-1;+4/p-1/t;2-;/m.0./s1
InChIKey	HADHSETVEMCBPU-TYOUJGAFSA-M
SMILES	O=C1[O-][Pt+2]2(N[CH2]C3CCC3CN2)[O-]C1C

Safety Information

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids
Toxicity	LD50 i.p. in mice: 46 mg/kg (Voegeli)

Usage And Synthesis

Uses

Lobaplatin (D-19466) is a diastereometric mixture of platinum(II) complexe. Lobaplatin arrests cell cycle at G1 and G2/M phase. Lobaplatin induces apoptosis by increasing expressions of caspase and Bax, decreasing expression of Bcl-2. Lobaplatin can be used for research of cancer[1][2][3].

Biological Activity

Lobaplatin (D-19466) is a third-generation platinum anticancer agent in vitro and in vivo, consisting of ~50:50 mixture of the two trans-1,2-cyclobutanedimethanamine diastereomers in complex with L-lactic acid. Llobaplatin shows antitumor efficacy against various human cancer cancer xenografts and significantly prolongs the survival of mice bearing P388 leukemia (mean life span increase post single i.p. in mg/kg = 46%/4.64 & 77/14.7). Compared to first and second generation platinum compounds, lobaplatin appears to be more stable, less toxic, have a better therapeutic index and may overcome tumor resistance.

in vivo

Lobaplatin (5 and 10 mg/kg; i.p.; once a week, for 3 weeks) suppresses tumor growth of esophageal squamous cell carcinoma (ESCC) xenograft^[1].

Animal Model:	Male BALB/c nude mice (4-6 weeks) with ESCC xenograft^[1]
Dosage:	Intraperitoneal injection; once a week, for 3 weeks
Administration:	5 and 10 mg/kg
Result:	Suppressed tumor volumes in a dose-dependent manner. Increased expressions of Bax and decreased expressions of Bcl-2.

References

[1] Du L, et, al. Antitumor activity of Lobaplatin against esophageal squamous cell carcinoma through caspase-dependent apoptosis and increasing the Bax/Bcl-2 ratio. Biomed Pharmacother. 2017 Nov;95:447-452. DOI:10.1016/j.biopha.2017.08.119
[2] Wu Q, et, al. Lobaplatin arrests cell cycle progression in human hepatocellular carcinoma cells. J Hematol Oncol. 2010 Oct 31;3:43. DOI:10.1186/1756-8722-3-43
[3] McKeage MJ. Lobaplatin: a new antitumour platinum drug. Expert Opin Investig Drugs. 2001 Jan;10(1):119-28. DOI:10.1517/13543784.10.1.119

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