| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Taltobulin intermediate-1 does not have a defined biological target, as it is a synthetic intermediate rather than a pharmacologically active compound. Its function is chemical—it serves as a building block for the synthesis of Taltobulin. Taltobulin, the final drug, is a potent tubulin (microtubule/tubulin) inhibitor that disrupts tubulin polymerization, induces mitotic arrest, and induces apoptosis. The intermediate itself is not evaluated for biological activity against specific targets.
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| ln Vitro |
As a chemical intermediate, Taltobulin intermediate-1 exhibits no intrinsic pharmacological activity in vitro. Its utility is demonstrated in the synthesis of Taltobulin, a common toxin component in ADC preparations. The compound is used in medicinal chemistry and oncology-focused drug development for the synthesis of next-generation targeted cancer therapeutics. In cell-based assays, the compound itself is not tested for biological activity. Instead, the final ADC products are evaluated for their pharmacological properties.
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| ln Vivo |
Taltobulin intermediate-1 does not exhibit in vivo biological activity, as it is not a therapeutic agent. The compound is used as a synthetic intermediate for the preparation of Taltobulin and ADC payloads. Any in vivo effects would be associated with the final ADC products synthesized from this intermediate, not with the intermediate itself. The compound is not administered to animals in pharmacological studies and has no known physiological effects.
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| Enzyme Assay |
In vitro assays for Taltobulin intermediate-1 focus on its use as a synthetic intermediate. Standard characterization includes nuclear magnetic resonance (¹H NMR, ¹³C NMR), mass spectrometry, and HPLC purity analysis (>98%). For synthetic applications, the compound is used in multi-step synthesis to prepare Taltobulin. The Boc-protected amino acid can be deprotected and coupled with other fragments to form the final tubulin inhibitor. No receptor binding assays are performed with the intermediate itself.
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| Cell Assay |
Cell-based experiments are not performed with Taltobulin intermediate-1, as it is a chemical intermediate rather than a test compound for biological activity. When the compound is used to synthesize Taltobulin or ADC payloads, those final products are tested in cell culture using standard protocols. Typically, final compounds are dissolved in DMSO and diluted in culture medium to achieve desired concentrations (0.1-100 µM). The intermediate itself is not evaluated in cellular systems.
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| Animal Protocol |
In vivo animal studies are not conducted with Taltobulin intermediate-1, as it is a research reagent for chemical synthesis. When the compound is used to synthesize ADC payloads or drug candidates, those final products undergo standard preclinical evaluation, including pharmacokinetic studies in rodents, efficacy studies in tumor xenograft models, and toxicology studies. These studies evaluate the safety and efficacy of the final drug molecules, not the synthetic intermediate.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Taltobulin intermediate-1 are not characterized, as it is not a drug substance. Based on its physicochemical properties (molecular weight 307.39, Boc-protected amino acid), the compound would be expected to have moderate lipophilicity and moderate oral bioavailability if administered. The Boc group would likely be cleaved in vivo to release the free amine. However, the compound is not intended for human exposure and has not been evaluated in formal pharmacokinetic studies.
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| Toxicity/Toxicokinetics |
Taltobulin intermediate-1 is a research reagent and should be handled with standard laboratory precautions, including the use of gloves, safety glasses, and working in a fume hood. The compound should be stored in a cool, dry place away from moisture and strong oxidizing agents. No acute toxicity data are available. The compound is not intended for drug, household, or other uses.
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| References | |
| Additional Infomation |
Taltobulin intermediate-1 is a key intermediate in the synthesis of Taltobulin, a potent tubulin inhibitor used as a toxin component in ADC preparations. Taltobulin disrupts tubulin polymerization, induces mitotic arrest, and induces apoptosis. The intermediate is used in medicinal chemistry and oncology-focused drug development. It has not undergone clinical trials and is not approved as a pharmaceutical. Its mechanism of action is chemical—serving as a precursor for the synthesis of tubulin-targeting ADC payloads.
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| Molecular Formula |
C17H25NO4
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|---|---|
| Molecular Weight |
307.38
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| Exact Mass |
307.178
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| CAS # |
228266-38-4
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| Related CAS # |
(Rac)-Taltobulin intermediate-1;676487-35-7
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| PubChem CID |
10425339
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.107±0.06 g/cm3(Predicted)
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| Boiling Point |
419.6±34.0 °C(Predicted)
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| Flash Point |
207.6±25.7 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.518
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| LogP |
4.15
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
22
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| Complexity |
405
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O(C(C)(C)C)C(N(C)[C@H](C(=O)O)C(C)(C)C1C=CC=CC=1)=O
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| InChi Key |
ZWQAFCGLXUTMKH-CYBMUJFWSA-N
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| InChi Code |
InChI=1S/C17H25NO4/c1-16(2,3)22-15(21)18(6)13(14(19)20)17(4,5)12-10-8-7-9-11-12/h7-11,13H,1-6H3,(H,19,20)/t13-/m1/s1
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| Chemical Name |
(2S)-3-methyl-2-[methyl-[(2-methylpropan-2-yl)oxycarbonyl]amino]-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 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 | 3.2533 mL | 16.2665 mL | 32.5330 mL | |
| 5 mM | 0.6507 mL | 3.2533 mL | 6.5066 mL | |
| 10 mM | 0.3253 mL | 1.6267 mL | 3.2533 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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