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60-89-9

60-89-9 structure
60-89-9 structure
  • Name: Mepazine
  • Chemical Name: 10-[(1-methylpiperidin-3-yl)methyl]phenothiazine
  • CAS Number: 60-89-9
  • Molecular Formula: C19H22N2S
  • Molecular Weight: 310.45600
  • Catalog: Signaling Pathways Apoptosis Apoptosis
  • Create Date: 2018-08-25 12:35:19
  • Modify Date: 2024-01-14 20:03:47
  • Mepazine (Pecazine) is a potent and selective MALT1 inhibitor. Mepazine inhibits GSTMALT1 full length and GSTMALT1 325-760 with IC50s of 0.83 and 0.42 μM, respectively. Mepazine affects viability of ABC-DLBCL cells by enhancing apoptosis[1].

Name 10-[(1-methylpiperidin-3-yl)methyl]phenothiazine
Synonyms Lacumin
10-[(1-methyl-3-piperidinyl)methyl]-10H-phenothiazine
Pecazine
MEPAZINE
10-(1-methyl-piperidin-3-ylmethyl)-10H-phenothiazine
mepasin
Pacatal
Nothiazine
Meprazine
Mepazin
Pecatal
Pakatal
10-(1-methyl-[3]piperidylmethyl)-phenothiazine
Description Mepazine (Pecazine) is a potent and selective MALT1 inhibitor. Mepazine inhibits GSTMALT1 full length and GSTMALT1 325-760 with IC50s of 0.83 and 0.42 μM, respectively. Mepazine affects viability of ABC-DLBCL cells by enhancing apoptosis[1].
Related Catalog
In Vitro Mepazine (5-20 μM; 4 days) causes a decrease of cell viability in the activated B cell subtype of diffuse large B cell lymphoma (ABCDLBCL) cells, without significantly affecting GCB-DLBCL cells[1]. Cell Viability Assay[1] Cell Line: ABC-DLBCL cell lines (HBL1, OCI-Ly3, U2932, TMD8, OCI-Ly10) and GCB-DLBCL cell lines (BJAB, Su-DHL-6, Su-DHL-4) Concentration: 5, 10, and 20 μM Incubation Time: 4 days Result: Caused a decrease of cell viability in the ABC-DLBCL cells HBL1, OCI-Ly3, U2932, and TMD8, without significantly affecting GCB-DLBCL cells.
In Vivo Mepazine (16 mg/kg; intraperitoneal administration) interferes with growth and induces apoptosis of ABC-DLBCL cell line OCI-Ly10 in NOD/scid IL-2Rgnull (NSG) mice with a murine DLBCL xenogeneic tumor model. Daily administration of Mepazine strongly impairs the expansion of the ABC-DLBCL cell line OCI-Ly10[1]. Animal Model: 6- to 8-week-old female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice with a murine DLBCL xenogeneic tumor model[1] Dosage: 400 μg per animal (25 g), corresponding to approximately 16 mg/kg. Administration: Intraperitoneal administration; started 1 or 12 days after transplantation and given continuously every 24 hr; daily application Result: Daily administration strongly impaired the expansion of the ABC-DLBCL cell line OCI-Ly10.
References

[1]. Nagel D, et al. Pharmacologic inhibition of MALT1 protease by phenothiazines as a therapeutic approach for the treatment of aggressive ABC-DLBCL. Cancer Cell. 2012 Dec 11;22(6):825-37.

Density 1.159 g/cm3
Boiling Point 444.4ºC at 760 mmHg
Molecular Formula C19H22N2S
Molecular Weight 310.45600
Flash Point 222.6ºC
Exact Mass 310.15000
PSA 31.78000
LogP 4.63400
Index of Refraction 1.627

CHEMICAL IDENTIFICATION

RTECS NUMBER :
SP2625000
CHEMICAL NAME :
Phenothiazine, 10-((1-methyl-3-piperidyl)methyl)-
CAS REGISTRY NUMBER :
60-89-9
LAST UPDATED :
199707
DATA ITEMS CITED :
6
MOLECULAR FORMULA :
C19-H22-N2-S
MOLECULAR WEIGHT :
310.49
WISWESSER LINE NOTATION :
T C666 BN ISJ B1- CT6NTJ A1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
200 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939- Volume(issue)/page/year: 24,136,1961
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
140 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 8,489,1958
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
750 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CANJAE Canadian Anaesthetists' Society Journal. (Toronto, Ont., Canada) V.1-33, 1954-86. Volume(issue)/page/year: 3,224,1956
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
70 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 4,232,1954
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
20 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CANJAE Canadian Anaesthetists' Society Journal. (Toronto, Ont., Canada) V.1-33, 1954-86. Volume(issue)/page/year: 3,224,1956 *** REVIEWS *** TOXICOLOGY REVIEW JMSCA9 Journal of Mental Science. (London, UK) V.4-108, 1857-1962. For publisher information, see BJPYAJ. Volume(issue)/page/year: 106,755,1960
Hazard Codes Xi
HS Code 2934300000
HS Code 2934300000
Summary 2934300000. other compounds containing in the structure a phenothiazine ring-system (whether or not hydrogenated), not further fused. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%