| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| Other Sizes |
| Targets |
No direct biological target; the compound is a synthetic intermediate for Tesirine (SG3249). Tesirine targets DNA as a minor groove cross-linker. The PBD dimer binds to the minor groove of DNA and forms cross-links, preventing DNA replication and transcription, leading to cell death. Tesirine intermediate-1 itself has no known biological activity.
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| ln Vitro |
Tesirine intermediate-1 itself has no reported in vitro biological activity as it is a synthetic precursor. The final product Tesirine (SG3249) is a highly cytotoxic PBD dimer that cross-links DNA. Tesirine is used as a warhead component in ADCs. The intermediate is used for synthesis of Tesirine and related compounds.
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| ln Vivo |
Tesirine intermediate-1 itself has no reported in vivo activity. The final product Tesirine (SG3249) is used as a cytotoxic payload in ADCs for targeted cancer therapy. The ADC delivers the PBD dimer to tumor cells, where it is released and exerts its DNA-crosslinking cytotoxicity. The intermediate is not used directly in vivo.
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| Enzyme Assay |
Not applicable for Tesirine intermediate-1 as it is a synthetic intermediate. For Tesirine (SG3249), in vitro assays include DNA cross-linking assays (gel-based or HPLC-based), cell viability assays (e.g., MTT, CellTiter-Glo) in cancer cell lines, and apoptosis assays. The PBD dimer's cytotoxicity is typically assessed in a panel of cancer cell lines with IC50 values in the pM to nM range.
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| Cell Assay |
Not applicable for Tesirine intermediate-1. For Tesirine (SG3249), cells are cultured and treated with the compound at concentrations ranging from pM to nM for 48–96 hours. Cytotoxicity is assessed by cell viability assays. DNA damage is evaluated by gamma-H2AX staining. Cell cycle analysis and apoptosis assays are performed to characterize the mechanism of cell death.
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| Animal Protocol |
Not applicable for Tesirine intermediate-1. For Tesirine-containing ADCs, in vivo studies are conducted in xenograft mouse models. The ADC is administered intravenously at doses typically ranging from 1–10 mg/kg. Tumor growth inhibition, survival, and toxicity are evaluated. The ADC delivers the PBD payload specifically to tumor cells.
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| ADME/Pharmacokinetics |
Not applicable for Tesirine intermediate-1. For Tesirine (SG3249), PK properties are typically evaluated in the context of ADC pharmacology. The PBD dimer itself is highly potent and requires targeted delivery to minimize systemic toxicity. ADC PK is characterized by measuring total antibody, conjugated antibody, and released payload in plasma.
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| Toxicity/Toxicokinetics |
Toxicology data for Tesirine intermediate-1 have not been published as it is a synthetic intermediate. Tesirine (SG3249) is highly cytotoxic and is used as a payload in ADCs. The toxicity of PBD dimers is well-established, and their use is limited to targeted delivery via ADCs to minimize off-target effects.
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| References |
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| Additional Infomation |
Tesirine intermediate-1 (CAS: 1430738-05-8, molecular formula C28H48N2O7Si2, molecular weight 580.86) is a synthetic intermediate for Tesirine (SG3249). Tesirine is a PBD dimer DNA cross-linker used as ADC payload. The compound is not in clinical trials and has no regulatory approval.
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| Molecular Formula |
C28H48N2O7SI2
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|---|---|
| Molecular Weight |
580.86093044281
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| Exact Mass |
580.3
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| CAS # |
1430738-05-8
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| PubChem CID |
86717745
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
39
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| Complexity |
860
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| Defined Atom Stereocenter Count |
1
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| SMILES |
[Si](C(C)C)(C(C)C)(C(C)C)OC1C=C(C(=CC=1OC)C(N1CC(C[C@H]1CO[Si](C)(C)C(C)(C)C)=O)=O)[N+](=O)[O-]
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| InChi Key |
IUVUOBISHKAUDN-NRFANRHFSA-N
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| InChi Code |
InChI=1S/C28H48N2O7Si2/c1-18(2)39(19(3)4,20(5)6)37-26-15-24(30(33)34)23(14-25(26)35-10)27(32)29-16-22(31)13-21(29)17-36-38(11,12)28(7,8)9/h14-15,18-21H,13,16-17H2,1-12H3/t21-/m0/s1
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| Chemical Name |
5S)-5-[[tert-butyl(dimethyl)silyl]oxymethyl]-1-[5-methoxy-2-nitro-4-tri(propan-2-yl)silyloxybenzoyl]pyrrolidin-3-one
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| Synonyms |
Tesirine intermediate-1
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 | 1.7216 mL | 8.6079 mL | 17.2159 mL | |
| 5 mM | 0.3443 mL | 1.7216 mL | 3.4432 mL | |
| 10 mM | 0.1722 mL | 0.8608 mL | 1.7216 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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