Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
5mg |
|
||
Other Sizes |
|
Purity: ≥98%
Dolastatin 10 (also known as DLS 10), a peptide-based natural product isolated from the marine mollusk Dolabela auricularia, is a highly potent antimitotic peptide that inhibits tubulin polymerization with an IC50 value of 1.2μM. It is an analog of Monomethyl auristatin E (MMAE) and can induce DC (dendritic cells) homing and activate cellular antitumor immune responses in patients.
ln Vitro |
Dolastatin 10 is a distinct pentapeptide that was found in Dolabella aurillaryia, a type of sea hare. These in vitro results are similar to those obtained from similar human cell mini-panels with GI50 values of 10-5-10-6 μg/mL (10-2-10-3) for both dolastatin 10 and auristatin PE [2]. The anti-CD30 monoclonal antibody cAC10 is combined with the cytotoxic compound monomethyl auristatin E (MMAE), a synthetic analogue of the tubulin polymerization inhibitor dolastatin 10, to form the antibody-drug combination (ADC) [3].
|
---|---|
References |
[1]. Pitot HC, et al. Phase I trial of dolastatin-10 (NSC 376128) in patients with advanced solid tumors. Clin Cancer Res. 1999 Mar;5(3):525-31.
[2]. Pettit GR, et al. Antineoplastic agents. 592. Highly effective cancer cell growth inhibitory structural modifications ofdolastatin 10. J Nat Prod. 2011 May 27;74(5):962-8. [3]. Brentuximab vedotin. Drugs R D. 2011;11(1):85-95. |
Molecular Formula |
C42H68N6O6S
|
---|---|
Molecular Weight |
785.09092
|
CAS # |
110417-88-4
|
Related CAS # |
160800-57-7 (Auristatin E, a synthetic analog of dolastatin 10); 123884-00-4 (Dolastatin 15); 163768-50-1 (Auristatin F, a synthetic analog of dolastatin 10)
|
SMILES |
CC(C)[C@H](NC([C@@H](N(C)C)C(C)C)=O)C(N([C@@H]([C@@H](C)CC)[C@H](OC)CC(N1[C@H]([C@H](OC)[C@@H](C)C(N[C@H](C2=NC=CS2)CC3=CC=CC=C3)=O)CCC1)=O)C)=O
|
InChi Key |
OFDNQWIFNXBECV-VFSYNPLYSA-N
|
InChi Code |
InChI=1S/C42H68N6O6S/c1-13-28(6)37(47(10)42(52)35(26(2)3)45-40(51)36(27(4)5)46(8)9)33(53-11)25-34(49)48-22-17-20-32(48)38(54-12)29(7)39(50)44-31(41-43-21-23-55-41)24-30-18-15-14-16-19-30/h14-16,18-19,21,23,26-29,31-33,35-38H,13,17,20,22,24-25H2,1-12H3,(H,44,50)(H,45,51)/t28-,29+,31-,32-,33+,35-,36-,37-,38+/m0/s1
|
Chemical Name |
(S)-2-((S)-2-(dimethylamino)-3-methylbutanamido)-N-((3R,4S,5S)-3-methoxy-1-((S)-2-((1R,2R)-1-methoxy-2-methyl-3-oxo-3-(((S)-2-phenyl-1-(thiazol-2-yl)ethyl)amino)propyl)pyrrolidin-1-yl)-5-methyl-1-oxoheptan-4-yl)-N,3-dimethylbutanamide
|
Synonyms |
NSC-376128; DLS-10; NSC376128; DLS10; NSC 376128; DLS 10
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product is not stable in solution, please use freshly prepared working solution for optimal results. (2). Please store this product in a sealed and protected environment, 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)
|
Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~127.37 mM)
|
---|---|
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 | 1.2737 mL | 6.3687 mL | 12.7374 mL | |
5 mM | 0.2547 mL | 1.2737 mL | 2.5475 mL | |
10 mM | 0.1274 mL | 0.6369 mL | 1.2737 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.