| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
The intermediate itself has no direct biological target. TAM558, the payload molecule, is designed to be conjugated to an anti-FAP antibody. The ADC OMTX705 targets fibroblast activation protein (FAP), a cell surface protein overexpressed in cancer-associated fibroblasts and many solid tumors.
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|---|---|
| ln Vitro |
The intermediate itself has no direct in vitro activity. TAM558, when conjugated as part of OMTX705, delivers a cytotoxic payload to FAP-expressing cells. The cytolysin TAM470 acts by forming pores in cell membranes, leading to cell death. OMTX705 exhibits potent antitumor activity in FAP-positive tumor models.
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| ln Vivo |
The intermediate itself has no direct in vivo activity. OMTX705, the ADC containing TAM558 as the payload, exhibits antitumor activity in xenograft models. It binds to FAP on tumor-associated fibroblasts and delivers the cytotoxic payload, leading to targeted cell death and tumor growth inhibition.
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| Enzyme Assay |
As a chemical intermediate, TAM558 intermediate-5 is not used in biological assays. Quality control involves standard chemical analysis: HPLC for purity assessment (typically ≥95%), LC-MS for molecular weight confirmation (772.05 g/mol), and NMR for structural verification. The molecular formula is C41H65N5O7S.
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| Cell Assay |
Cell-based assays are not applicable to this intermediate. For OMTX705 ADC, typical protocols involve incubating FAP-positive cells with serial dilutions of the ADC (0.1 nM to 1 uM) for 48-96 hours, then assessing cell viability with MTT or CellTiter-Glo. Alternatively, TAM558 alone can be tested in FAP-negative cells to evaluate off-target toxicity.
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| Animal Protocol |
Animal studies are not conducted directly on this intermediate. For OMTX705, typical xenograft protocols involve subcutaneous implantation of FAP-positive tumor cells into immunocompromised mice. When tumors reach ~100-200 mm3, OMTX705 is administered intravenously at 0.5-10 mg/kg once or twice weekly, with tumor volume monitored.
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| ADME/Pharmacokinetics |
No pharmacokinetic data is available for this intermediate. For ADC OMTX705, PK studies would evaluate the antibody-conjugated payload in circulation. TAM558 itself, as a hydrophilic payload, likely has a short half-life when not conjugated. Unconjugated payload levels in plasma are typically very low.
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| Toxicity/Toxicokinetics |
No direct toxicity data is available for this intermediate. For OMTX705, as an ADC targeting FAP-expressing fibroblasts, its toxicity profile may include effects on normal tissues expressing FAP (wound healing, tissue remodeling). Standard safety precautions should be taken when handling this research chemical.
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| Additional Infomation |
TAM558 intermediate-5 is a research-use chemical and not a pharmaceutical for human consumption. TAM558 is the payload for the FAP-targeted ADC OMTX705. OMTX705 is a humanized anti-FAP antibody conjugated to TAM470, a cytolysin that forms pores in cell membranes. This ADC is in preclinical development for solid tumors but has not received regulatory approval.
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| Molecular Formula |
C41H65N5O7S
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|---|---|
| Molecular Weight |
772.05
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| Exact Mass |
771.46
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| CAS # |
1415659-15-2
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| PubChem CID |
89520284
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
22
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| Heavy Atom Count |
54
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| Complexity |
1170
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| Defined Atom Stereocenter Count |
7
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| SMILES |
CCCN([C@H](C[C@H](C1=NC(=CS1)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C[C@H](C)C(=O)O)OCCC)C(C)C)C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H]3CCCCN3C
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| InChi Key |
ACRSOTAEOXNROB-WPIAVMABSA-N
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| InChi Code |
InChI=1S/C41H65N5O7S/c1-9-19-46(40(50)36(27(6)11-3)44-38(49)33-14-12-13-20-45(33)8)34(26(4)5)24-35(53-21-10-2)39-43-32(25-54-39)37(48)42-30(22-28(7)41(51)52)23-29-15-17-31(47)18-16-29/h15-18,25-28,30,33-36,47H,9-14,19-24H2,1-8H3,(H,42,48)(H,44,49)(H,51,52)/t27-,28-,30+,33+,34+,35+,36-/m0/s1
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| Chemical Name |
(2S,4R)-5-(4-hydroxyphenyl)-2-methyl-4-[[2-[(1R,3R)-4-methyl-3-[[(2S,3S)-3-methyl-2-[[(2R)-1-methylpiperidine-2-carbonyl]amino]pentanoyl]-propylamino]-1-propoxypentyl]-1,3-thiazole-4-carbonyl]amino]pentanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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 | 1.2953 mL | 6.4763 mL | 12.9525 mL | |
| 5 mM | 0.2591 mL | 1.2953 mL | 2.5905 mL | |
| 10 mM | 0.1295 mL | 0.6476 mL | 1.2953 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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