TT 232|147159-51-1|(CAP-232; TLN-232)-陌孚医药/Medlife

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TT 232 (Synonyms: CAP-232; TLN-232)

目录号: PC11007 纯度: ≥98%

CAS No. :147159-51-1

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中文名称

TT 232

中文别名

H-D-PHE-CYS-TYR-D-TRP-LYS-CYS-THR-NH2(DISULFIDE BRIDGE: 2-6);化合物 T23479

英文名称

TT 232

英文别名

1-methoxy-6,6,9-trimethyl-3-pentyl-6a,7,10,10a-tetrahydrobenzo[c]chromene;L-Threoninamide,D-phenylalanyl-L-cysteinyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-cysteinyl-, cyclic...;TT 232;TT-232;(4R,7S,13S,16S)-7-(4-aminobutyl)-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-13-(4-hydroxybenzyl)-10-(1H-indol-3-ylmethyl)-6,9,12,15-tetraoxo-16-(D-phenylalanylamino)-1,2-dithia-5;L-Threoninamide, D-phenylalanyl-L-cysteinyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-cysteinyl-, cyclic (2-6)-disulfide;Phe-cys-tyr-trp-lys-cys-thr-NH2 (2-6)-disulfide;Phenylalanyl-cysteinyl-tyrosyl-tryptophyl-lysyl-cysteinyl-threoninamide (2-6)-disulfide;L-ThreoninaMide, D-phenylalanyl-L-cysteinyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-cysteinyl-, cyclic (2→6)-disulfide

Cas No.

147159-51-1

分子式

C₄₅H₅₈N₁₀O₉S₂

分子量

947.13

包装储存

Sealed storage, away from moisture and light, under nitrogen

Powder	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

生物活性

TT-232 (CAP-232), a somatostatin derivative, is a peptide SSTR1/SSTR4 agonist. TT-232 inhibits cancer cell proliferation and induces apoptosis. TT-232 is also a broad-spectrum anti-inflammatory and analgesic agent.

性状

Solid

IC50 & Target[1][2]

SSTR1

SSTR4

体外研究(In Vitro)

TT-232 (10 μg/mL, 48 h) induces apoptosis in human colon (HT-29 and SW620), pancreatic (818), leukemia (K-562), melanoma (WM 938/B, M-1 and EP) and lymphoma (HT-58) tumor cell lines.
TT-232 (20-30 μg/mL, 24 h) shows antiproliferative effect on various human tumor cell lines.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	MCF7, PC-3, P818, K-562, 4-1ST, ect.
Concentration:	20-30 μg/mL
Incubation Time:	24 h
Result:	Inhibited cell proliferation by 87%, 90%, 98%, 95%, respectively.

体内研究(In Vivo)

TT-232 (15-750 μg/kg/day, twice a day) inhibits tumor growth in mice transplanted with Colon 26 cell.
TT-232 (0.6 or 15 μg/kg s.c or i.p.) shows antitumor effect on P-388 rodent lymphocytic leukemia tumor mice.
TT-232 (7.5-20 μg/kg, i.v.) inhibits Carrageenin-induced paw oedema in rats.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mice transplanted with Colon 26 cell .
Dosage:	15, 150, 750 μg/kg/day
Administration:	Intraperitoneal injection (i.p.)
Result:	Reached 70% tumor inhibition at 750 μg/kg.

运输条件

Room temperature or refrigerated transportation.

储存方式

Sealed storage, away from moisture and light, under nitrogen

Powder	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

ClinicalTrial

参考文献

[1]. Szende B, et al. TT-232: a somatostatin structural derivative as a potent antitumor drug candidate. Anticancer Drugs. 2003 Sep;14(8):585-8. [Information]

[2]. Kéri G, et al. A tumor-selective somatostatin analog (TT-232) with strong 体外研究 and in vivo antitumor activity. Proc Natl Acad Sci U S A. 1996 Oct 29;93(22):12513-8. [Information]

[3]. Tejeda M, et al. Growth inhibitory effect of the somatostatin structural derivative (TT-232) on leukemia models. Anticancer Res. 2005 Jan-Feb;25(1A):325-30. [Information]

[4]. Pintér E, et al. Pharmacological characterisation of the somatostatin analogue TT-232: effects on neurogenic and non-neurogenic inflammation and neuropathic hyperalgesia. Naunyn Schmiedebergs Arch Pharmacol. 2002 Aug;366(2):142-50. [Information]

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