| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Taltobulin intermediate-2 itself has no direct biological target. However, its downstream product Taltobulin targets tubulin (microtubules), disrupting polymerization and inducing mitotic arrest.
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|---|---|
| ln Vitro |
Taltobulin intermediate-2 as a synthetic building block has no direct in vitro activity. However, the final API Taltobulin exhibits potent antimicrotubule activity with IC50 values in the low nanomolar range against various cancer cell lines and circumvents P-glycoprotein-mediated resistance.
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| ln Vivo |
Taltobulin intermediate-2 has no direct in vivo activity. Taltobulin, the compound for whose synthesis this intermediate is used, demonstrates potent antitumor efficacy in xenograft models and is effective against multidrug-resistant tumors.
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| Enzyme Assay |
Taltobulin intermediate-2 is a chemical intermediate and is not typically subjected to enzyme binding assays. For quality control purposes, HPLC and LC-MS are used to verify its identity and purity. Researchers should consult the Certificate of Analysis for specific characterization data.
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| Cell Assay |
For Taltobulin intermediate-2, standard cell-based assays are not applicable as it is a synthetic intermediate. However, the final compound Taltobulin is evaluated in cell viability assays using cancer cell lines (e.g., NCI-H460, MDA-MB-231) with incubation for 48-72 hours and analysis by MTT or CellTiter-Glo.
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| Animal Protocol |
Animal studies are not conducted directly on Taltobulin intermediate-2. For Taltobulin, typical xenograft models involve subcutaneous tumor implantation in immunocompromised mice, followed by intravenous administration of Taltobulin ADC formulations (0.5-5 mg/kg) and monitoring of tumor volume and body weight.
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| ADME/Pharmacokinetics |
As an intermediate, no pharmacokinetic data is available for Taltobulin intermediate-2. For Taltobulin, PK studies typically show a short half-life (t1/2 = 30-60 minutes) in rodents due to rapid clearance, high plasma protein binding (>95%), and limited oral bioavailability.
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| Toxicity/Toxicokinetics |
No direct toxicity data is available for Taltobulin intermediate-2. For Taltobulin, as a tubulin-binding agent, it exhibits typical cytotoxic class effects including dose-limiting neutropenia, peripheral neuropathy, and gastrointestinal toxicity.
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| References |
[1]. Loganzo F, et al. HTI-286, a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Cancer Res. 2003 Apr 15;63(8):1838-45.
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| Additional Infomation |
Taltobulin intermediate-2 is strictly a research-use chemical and is not a pharmaceutical for human consumption. The final drug Taltobulin is a synthetic analogue of the tripeptide hemiasterlin and functions as a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance. It has been investigated in preclinical studies for cancer therapy but has not received regulatory approval for human use.
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| Molecular Formula |
C11H12O3
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|---|---|
| Molecular Weight |
192.211183547974
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| Exact Mass |
192.078
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| CAS # |
91133-59-4
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| PubChem CID |
12218047
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
14
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| Complexity |
237
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C(=O)O)C(C)(C)C1C=CC=CC=1
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| InChi Key |
ULDLCYGZHGFPIM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H12O3/c1-11(2,9(12)10(13)14)8-6-4-3-5-7-8/h3-7H,1-2H3,(H,13,14)
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| Chemical Name |
3-methyl-2-oxo-3-phenylbutanoic 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 | 5.2026 mL | 26.0132 mL | 52.0264 mL | |
| 5 mM | 1.0405 mL | 5.2026 mL | 10.4053 mL | |
| 10 mM | 0.5203 mL | 2.6013 mL | 5.2026 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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