Nedaplatin

Modify Date: 2024-01-03 19:17:05

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

 Use of Nedaplatin


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].

 Names

Name nedaplatin
Synonym More Synonyms

 Nedaplatin Biological Activity

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
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
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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