CAS 95734-82-0|Nedaplatin

Introduction：Basic information about CAS 95734-82-0|Nedaplatin, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Nedaplatin BiologicalActivity
3. Chemical & Physical Properties
4. Toxicological Information
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
MUTATION DATA
5. Safety Information
6. Synonyms

Common Name	Nedaplatin
CAS Number	95734-82-0	Molecular Weight	303.181
Density	/	Boiling Point	265.6ºC at 760 mmHg
Molecular Formula	C₂H₈N₂O₃Pt	Melting Point	/
MSDS	/	Flash Point	128.7ºC

Names

Name	nedaplatin
Synonym	More Synonyms

Nedaplatin BiologicalActivity

Description	Nedaplatin is a derivative of cisplatin and DNA damage agent.Target: OthersNedaplatin(NDP) is a derivative of cisplatin which produced less nausea & vomiting and nephrotoxicity. the effect of NDP on the 7-ethyl-1-hydroxy-CPT (the active form of CPT-11)-induced inhibitory effect on DNA topoisomerase I was examined. The topoisomerase I-inhibitory effect of 7-ethyl-1-hydroxy-CPT was enhanced 10-fold in the presence of NDP at microgram/milliliter concentrations [1]. NDP was developed as a second generation platinum complex. Because it has greater antitumour activity and lower nephrotoxicity than cisplatin (CDDP). At the high-dose of NDP in FN therapy, a reduction of tumour size and long-term tumour-free survival were frequently observed. The survival effect of the combinations of NDP with 5-FU was superior to those of the combination of CDDP with 5-FU. In conclusion, the sequence-dependent antitumour efficacy and toxicity of the combination of NDP or CDDP with 5-FU was demonstrated in this study, and FN therapy appeared to be the most efficient regimen as a clinical therapy [2].
Related Catalog	Signaling Pathways >>Cell Cycle/DNA Damage >>DNA/RNA SynthesisResearch Areas >>Cancer
References	[1]. Kanzawa, F., et al., In vitro synergistic interactions between the cisplatin analogue nedaplatin and the DNA topoisomerase I inhibitor irinotecan and the mechanism of this interaction. Clin Cancer Res, 2001. 7(1): p. 202-9. [2]. Uchida, N., et al., Sequence-dependent antitumour efficacy of combination chemotherapy of nedaplatin, a novel platinum complex, with 5-fluorouracil in an in vivo murine tumour model. Eur J Cancer, 1998. 34(11): p. 1796-801.

Description

Nedaplatin is a derivative of cisplatin and DNA damage agent.Target: OthersNedaplatin(NDP) is a derivative of cisplatin which produced less nausea & vomiting and nephrotoxicity. the effect of NDP on the 7-ethyl-1-hydroxy-CPT (the active form of CPT-11)-induced inhibitory effect on DNA topoisomerase I was examined. The topoisomerase I-inhibitory effect of 7-ethyl-1-hydroxy-CPT was enhanced 10-fold in the presence of NDP at microgram/milliliter concentrations [1]. NDP was developed as a second generation platinum complex. Because it has greater antitumour activity and lower nephrotoxicity than cisplatin (CDDP). At the high-dose of NDP in FN therapy, a reduction of tumour size and long-term tumour-free survival were frequently observed. The survival effect of the combinations of NDP with 5-FU was superior to those of the combination of CDDP with 5-FU. In conclusion, the sequence-dependent antitumour efficacy and toxicity of the combination of NDP or CDDP with 5-FU was demonstrated in this study, and FN therapy appeared to be the most efficient regimen as a clinical therapy [2].

Related Catalog

Signaling Pathways >>Cell Cycle/DNA Damage >>DNA/RNA SynthesisResearch Areas >>Cancer

References

[1]. Kanzawa, F., et al., In vitro synergistic interactions between the cisplatin analogue nedaplatin and the DNA topoisomerase I inhibitor irinotecan and the mechanism of this interaction. Clin Cancer Res, 2001. 7(1): p. 202-9.

[2]. Uchida, N., et al., Sequence-dependent antitumour efficacy of combination chemotherapy of nedaplatin, a novel platinum complex, with 5-fluorouracil in an in vivo murine tumour model. Eur J Cancer, 1998. 34(11): p. 1796-801.

Chemical & Physical Properties

Boiling Point	265.6ºC at 760 mmHg
Molecular Formula	C₂H₈N₂O₃Pt
Molecular Weight	303.181
Flash Point	128.7ºC
Exact Mass	303.018280
PSA	42.01000
LogP	0.12010
InChIKey	KLNFSAOEKUDMFA-UHFFFAOYSA-M
SMILES	O=C([O-])CO.[NH2-].[NH2-].[Pt+2]
Storage condition	2-8°C

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TP2482800

CHEMICAL NAME :: Platinum, diammine(hydroxyacetato(2-)-O(sup 1),O(sup 2))-, (SP-4-3)-

CAS REGISTRY NUMBER :: 95734-82-0

LAST UPDATED :: 199612

DATA ITEMS CITED :: 14

MOLECULAR FORMULA :: C2-H8-N2-O3-Pt

MOLECULAR WEIGHT :: 303.21

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 20 mg/kg

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - other changes in urine composition Nutritional and Gross Metabolic - changes in sodium

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 44100 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 4 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 48600 ug/kg/26W-I

TOXIC EFFECTS :: Cardiac - other changes Kidney, Ureter, Bladder - other changes Endocrine - other changes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 10800 ug/kg/26W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in bladder weight Blood - changes in platelet count Related to Chronic Data - changes in testicular weight

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 45 mg/kg/30D-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Ear) - change in acuity Sense Organs and Special Senses (Ear) - changes in cochlear structure or function

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 13 mg/kg

SEX/DURATION :: female 17-21 day(s) after conception lactating female 20 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects Reproductive - Effects on Newborn - physical Related to Chronic Data - changes in ovarian weight

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 4500 ug/kg

SEX/DURATION :: female 17-21 day(s) after conception lactating female 20 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - physical

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 46 mg/kg

SEX/DURATION :: male 64 day(s) pre-mating female 2 week(s) pre-mating - 7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Paternal Effects - other effects on male Reproductive - Maternal Effects - menstrual cycle changes or disorders Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 46 mg/kg

SEX/DURATION :: male 64 day(s) pre-mating female 2 week(s) pre-mating - 7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 750 mg/kg

SEX/DURATION :: female 7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

MUTATION DATA

TEST SYSTEM :: Rodent - mouse

DOSE/DURATION :: 6300 ug/kg

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 22,821,1991

Safety Information

Hazard Codes	Xn

Synonyms

(glycolato-O,O')diammine platinum(II)

2,2-diaMino-1,3-dioxa-2-platinacyclopentan-4-one

Platinum, [2-(hydroxy-κO)acetato(2-)-κO]-, ammoniate (1:2)

[(Hydroxy-κO)acetato(2-)-κO]platinum diammoniate

Nedaplatin

o(sup2))-diammine(hydroxyacetato(2-)-o(sup1(sp-4-3)-platinu

cis-diammine(glycolato)platinum(ii)

PlatinuM,diaMMine[(hydroxy-kO)acetato(2-)-kO]-,(SP-4-3)

Nedaplait

254-s

cis-diamine-glycolate-O,O'-platinum(II)

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