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TT2-32 acetate (TLN-232; CAP-232) is a novel somatostatin analog acting as a peptide agonist for sst1/sst4 somatostatin receptors with antitumor activity. TT-232 inhibited tyrosine kinase activity of tumor cell lines and this inhibition correlated well with the inhibition of cell proliferation of a large number of cancer cell lines in vitro and reduces the size of different tumors in animal models in vivo.
| ln Vitro |
Inducing apoptosis in human colon (HT-29 and SW620), pancreatic (818), leukemia (K-562), melanoma (WM 938/B, M-1 and EP) cells, and lymphoma (HT-58) tumor cell line is possible with TT-232 (10 μg/mL, 48 hours) [1]. A range of human tumor cell lines exhibit anti-proliferative effects when exposed to TT-232 (20–30 μg/mL, 24 h) [2]. detection of cell viability [2]
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|---|---|
| ln Vivo |
In mice receiving colon 26 cell transplants, TT-232 (15-750 μg/kg/day, twice daily) suppresses tumor growth [2]. In mice harboring P-388 rodent lymphocytic leukemia tumors, TT-232 (0.6 or 15 μg/kg sc or ip) has anti-tumor activity [3]. Rats' paw edema caused by carrageenan is prevented by intravenous injection of TT-232 (7.5–20 μg/kg) [4].
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| Cell Assay |
Cell Viability Assay [2]
Cell Types: MCF7, PC-3, P818, K-562, 4-1ST, etc. Tested Concentrations: 20-30 μg/mL Incubation Duration: 24 h Experimental Results: The cell proliferation inhibition rates were 87%, 90%, 98%, and 95% respectively. |
| Animal Protocol |
Animal/Disease Models: Mice transplanted with colon 26 cells [2].
Doses: 15, 150, 750 μg/kg/day Route of Administration: intraperitoneal (ip) injection Experimental Results: Tumor inhibition reached 70% at 750 μg/kg. |
| References |
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| Additional Infomation |
Tln 232 is under investigation in clinical trial NCT00422786 (Phase II Study of CAP-232 in Patients With Refractory Metastatic Renal Cell Carcinoma).
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| Molecular Formula |
C45H58N10O9S2
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|---|---|
| Molecular Weight |
947.14
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| Exact Mass |
328.24
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| Elemental Analysis |
C, 56.05; H, 6.20; N, 13.91; O, 17.47; S, 6.37
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| CAS # |
147159-51-1
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| Related CAS # |
TT2-32 acetate; 147159-51-1;147159-51-1 (TFA);d8-TT2-32 acetate;
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| PubChem CID |
6918265
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| Appearance |
White to off-white solid powder
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| Density |
1.42g/cm3
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| Boiling Point |
1409.4ºC at 760mmHg
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| Flash Point |
806.2ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.69
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| LogP |
6.038
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
66
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| Complexity |
1640
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| Defined Atom Stereocenter Count |
8
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| SMILES |
C1(=CNC2C=CC=CC1=2)C[C@@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H](N)CC2C=CC=CC=2)C(=O)N[C@@H](CC2C=CC(O)=CC=2)C(=O)N1)C(=O)N[C@]([H])(C(=O)N)[C@H](O)C
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| InChi Key |
SNAJPQVDGYDQSW-DYCFWDQMSA-N
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| InChi Code |
InChI=1S/C45H58N10O9S2/c1-25(56)38(39(48)58)55-45(64)37-24-66-65-23-36(53-40(59)31(47)19-26-9-3-2-4-10-26)44(63)51-34(20-27-14-16-29(57)17-15-27)42(61)52-35(21-28-22-49-32-12-6-5-11-30(28)32)43(62)50-33(41(60)54-37)13-7-8-18-46/h2-6,9-12,14-17,22,25,31,33-38,49,56-57H,7-8,13,18-21,23-24,46-47H2,1H3,(H2,48,58)(H,50,62)(H,51,63)(H,52,61)(H,53,59)(H,54,60)(H,55,64)/t25-,31-,33+,34+,35-,36+,37+,38+/m1/s1
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| Chemical Name |
(4R,7S,10R,13S,16R)-7-(4-aminobutyl)-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-16-[[(2R)-2-amino-3-phenylpropanoyl]amino]-13-[(4-hydroxyphenyl)methyl]-10-(1H-indol-3-ylmethyl)-6,9,12,15-tetraoxo-1,2-dithia-5,8,11,14-tetrazacycloheptadecane-4-carboxamide
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| Synonyms |
TT232 acetate TT2 32 TT2-32
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0558 mL | 5.2791 mL | 10.5581 mL | |
| 5 mM | 0.2112 mL | 1.0558 mL | 2.1116 mL | |
| 10 mM | 0.1056 mL | 0.5279 mL | 1.0558 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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