| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
(Rac)-Taltobulin intermediate-1 does not have a defined biological target as it is a synthetic intermediate. 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 promotes apoptosis in rapidly dividing cancer cells.
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|---|---|
| ln Vitro |
As a chemical intermediate, (Rac)-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.
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| ln Vivo |
(Rac)-Taltobulin intermediate-1 does not exhibit in vivo biological activity, as it is not a therapeutic agent. It 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.
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| Enzyme Assay |
In vitro assays for (Rac)-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. 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.
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| Cell Assay |
Cell-based experiments are not performed with (Rac)-Taltobulin intermediate-1, as it is a chemical intermediate. When the compound is used to synthesize Taltobulin or ADC payloads, those final products are tested in cell culture.
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| Animal Protocol |
In vivo animal studies are not conducted with (Rac)-Taltobulin intermediate-1. When 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.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of (Rac)-Taltobulin intermediate-1 are not characterized, as it is not a drug substance. The compound is not intended for human exposure.
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| Toxicity/Toxicokinetics |
(Rac)-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 at -20°C.
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| References | |
| Additional Infomation |
(Rac)-Taltobulin intermediate-1 is a racemic synthetic intermediate used in the preparation of Taltobulin, a microtubule-targeting agent and ADC payload. It has not undergone clinical trials and is not approved as a pharmaceutical.
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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 # |
676487-35-7
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| Related CAS # |
Taltobulin intermediate-1;228266-38-4
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| PubChem CID |
11695225
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
419.6±34.0 °C at 760 mmHg
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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 |
0
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| SMILES |
CC(C)(C)OC(=O)N(C)C(C(=O)O)C(C)(C)C1=CC=CC=C1
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| InChi Key |
ZWQAFCGLXUTMKH-UHFFFAOYSA-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)
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| Chemical Name |
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 |
| 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) |
DMSO: ≥ 100 mg/mL (~325.3 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.13 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (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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