Dolastatin 10
Based on 1 Customer Validation
Dolastatin 10 (DLS 10) is a potent antimitotic peptide that inhibits tubulin polymerization.
For research use only. We do not sell to patients.
- Purity: 98.34%
- CAS No.: 110417-88-4
- Formula: C42H68N6O6S
- Molecular Weight:785.09
-
Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* The compound is unstable in solutions, freshly prepared is recommended.
Biological Activity
|
Auristatin |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A10 | EC50 |
0.25 nM
Compound: 1
|
Antitumor activity against rat A10 cells assessed as loss of cellular microtubule after 18 hrs by indirect immunofluorescence
Antitumor activity against rat A10 cells assessed as loss of cellular microtubule after 18 hrs by indirect immunofluorescence
|
[PMID: 11473421] |
| A498 | GI50 |
0.033 nM
Compound: 1
|
Anticancer activity against human A498 cells assessed as growth inhibition
Anticancer activity against human A498 cells assessed as growth inhibition
|
[PMID: 35072477] |
| BXPC-3 | GI50 |
0.051 nM
Compound: 1
|
Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay
Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay
|
[PMID: 28895394] |
| BXPC-3 | GI50 |
0.051 nM
Compound: 2
|
Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay
Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay
|
[PMID: 28926240] |
| CA46 | IC50 |
30 nM
Compound: Dolastatin 10
|
Cytotoxicity against human CA46 cell line
Cytotoxicity against human CA46 cell line
|
[PMID: 16837194] |
| DU-145 | GI50 |
0.007 nM
Compound: 1
|
Growth inhibition of human DU145 cells after 48 hrs by SRB assay
Growth inhibition of human DU145 cells after 48 hrs by SRB assay
|
[PMID: 28895394] |
| DU-145 | GI50 |
0.007 nM
Compound: 2
|
Growth inhibition of human DU145 cells after 48 hrs by SRB assay
Growth inhibition of human DU145 cells after 48 hrs by SRB assay
|
[PMID: 28926240] |
| HCT-116 | IC50 |
0.48 nM
Compound: 1
|
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability measured after 48 hrs by ATPlite 1step luminescence assay
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability measured after 48 hrs by ATPlite 1step luminescence assay
|
[PMID: 27380142] |
| HCT-116 | IC50 |
24 nM
Compound: 1
|
Cytotoxicity against oncogenic KRAS knockout human HCT116 cells expressing wild type KRAS assessed as reduction in cell viability measured after 48 hrs by ATPlite 1step luminescence assay
Cytotoxicity against oncogenic KRAS knockout human HCT116 cells expressing wild type KRAS assessed as reduction in cell viability measured after 48 hrs by ATPlite 1step luminescence assay
|
[PMID: 27380142] |
| HCT-116 | IC50 |
65 nM
Compound: 1
|
Cytotoxicity against human HIF1alpha and HIF2alpha deficit HCT116 cells assessed as reduction in cell viability measured after 48 hrs by ATPlite 1step luminescence assay
Cytotoxicity against human HIF1alpha and HIF2alpha deficit HCT116 cells assessed as reduction in cell viability measured after 48 hrs by ATPlite 1step luminescence assay
|
[PMID: 27380142] |
| HT-29 | IC50 |
0.06 nM
Compound: 1
|
Anticancer activity against human HT-29 assessed as reduction in cell viability incubated for 96 hrs by microculture tetrazolium assay
Anticancer activity against human HT-29 assessed as reduction in cell viability incubated for 96 hrs by microculture tetrazolium assay
|
[PMID: 35072477] |
| HT-29 | IC50 |
0.018 nM
Compound: 1
|
Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 96 hrs by SRB assay
Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 96 hrs by SRB assay
|
[PMID: 39068862] |
| HT-29 | IC50 |
0.06 nM
Compound: Dolastatin 10
|
Inhibitory activity against growth of HT-29 cell line
Inhibitory activity against growth of HT-29 cell line
|
[PMID: 9554885] |
| HT-29 | IC50 |
0.06 nM
Compound: Dolastatin 10
|
Compound was evaluated for antiproliferative activity against human colon adenocarcinoma (HT-29) cell lines.
Compound was evaluated for antiproliferative activity against human colon adenocarcinoma (HT-29) cell lines.
|
[PMID: 9873636] |
| KB | IC50 |
<0.1 ng/mL
Compound: 1
|
Cytotoxicity against human KB cells
Cytotoxicity against human KB cells
|
[PMID: 9748368] |
| KM-20L2 | GI50 |
0.01 nM
Compound: 1
|
Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay
Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay
|
[PMID: 28895394] |
| KM-20L2 | GI50 |
0.01 nM
Compound: 2
|
Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay
Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay
|
[PMID: 28926240] |
| KM-20L2 | GI50 |
0.006 nM
Compound: 1
|
Anticancer activity against human KM-20L2 cells assessed as growth inhibition
Anticancer activity against human KM-20L2 cells assessed as growth inhibition
|
[PMID: 35072477] |
| L1210 | IC50 |
0.9 nM
Compound: 1
|
Cytotoxicity against mouse L1210 cells assessed as cell growth inhibition measured after 24 hrs
Cytotoxicity against mouse L1210 cells assessed as cell growth inhibition measured after 24 hrs
|
[PMID: 35072477] |
| L1210 | IC50 |
0.03 nM
Compound: Dolastatin 10
|
Inhibitory activity against growth of L1210 cell line
Inhibitory activity against growth of L1210 cell line
|
[PMID: 9554885] |
| L1210 | IC50 |
0.03 nM
Compound: Dolastatin 10
|
Compound was evaluated for antiproliferative activity against murine leukemia (L1210) cell lines.
Compound was evaluated for antiproliferative activity against murine leukemia (L1210) cell lines.
|
[PMID: 9873636] |
| leukaemia cell line | ED50 |
4.6 x 10-5 μg/mL
Compound: 1
|
Cytotoxicity against human leukaemia cell line assessed as cell growth inhibition
Cytotoxicity against human leukaemia cell line assessed as cell growth inhibition
|
[PMID: 35072477] |
| MCF7 | IC50 |
0.083 nM
Compound: 4a
|
Growth inhibition of human MCF7 after 48 hrs by sulforhodamine B method
Growth inhibition of human MCF7 after 48 hrs by sulforhodamine B method
|
[PMID: 16124759] |
| MCF7 | GI50 |
0.005 nM
Compound: 1
|
Growth inhibition of human MCF7 cells after 48 hrs by SRB assay
Growth inhibition of human MCF7 cells after 48 hrs by SRB assay
|
[PMID: 28895394] |
| MCF7 | GI50 |
0.005 nM
Compound: 2
|
Growth inhibition of human MCF7 cells after 48 hrs by SRB assay
Growth inhibition of human MCF7 cells after 48 hrs by SRB assay
|
[PMID: 28926240] |
| MCF7 | IC50 |
0.03 nM
Compound: Dolastatin 10
|
Inhibitory activity against growth of MCF-7 cell line
Inhibitory activity against growth of MCF-7 cell line
|
[PMID: 9554885] |
| NCI-H446 | IC50 |
0.032 nM
Compound: 1
|
Anticancer activity against human NCI-H446 cells assessed as cell growth inhibition
Anticancer activity against human NCI-H446 cells assessed as cell growth inhibition
|
[PMID: 35072477] |
| NCI-H460 | GI50 |
0.229 nM
Compound: 1
|
Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay
Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay
|
[PMID: 28895394] |
| NCI-H460 | GI50 |
0.229 nM
Compound: 2
|
Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay
Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay
|
[PMID: 28926240] |
| NCI-H460 | GI50 |
0.004 nM
Compound: 1
|
Anticancer activity against human NCI-H460 cells assessed as growth inhibition
Anticancer activity against human NCI-H460 cells assessed as growth inhibition
|
[PMID: 35072477] |
| NCI-H510A | IC50 |
0.032 nM
Compound: 1
|
Anticancer activity against human NCI-H510A cells assessed as cell growth inhibition
Anticancer activity against human NCI-H510A cells assessed as cell growth inhibition
|
[PMID: 35072477] |
| NCI-H69 | IC50 |
0.032 nM
Compound: 1
|
Anticancer activity against human NCI-H69 cells assessed as cell growth inhibition
Anticancer activity against human NCI-H69 cells assessed as cell growth inhibition
|
[PMID: 35072477] |
| NCI-H82 | IC50 |
0.032 nM
Compound: 1
|
Anticancer activity against human NCI-H82 cells assessed as cell growth inhibition
Anticancer activity against human NCI-H82 cells assessed as cell growth inhibition
|
[PMID: 35072477] |
| OVCAR-3 | GI50 |
0.001 nM
Compound: 1
|
Anticancer activity against human OVCAR-3 cells assessed as growth inhibition
Anticancer activity against human OVCAR-3 cells assessed as growth inhibition
|
[PMID: 35072477] |
| P388 | ED50 |
0.001 μg/mL
Compound: 1
|
Effect against cell growth of the P388 lymphocytic leukemia (PS system)
Effect against cell growth of the P388 lymphocytic leukemia (PS system)
|
[PMID: 2258898] |
| P388 | ED50 |
0.1 ng/mL
Compound: Dolastatin10
|
Anticancer activity against lymphocytic leukemia P388 cells was determined
Anticancer activity against lymphocytic leukemia P388 cells was determined
|
[PMID: 9871690] |
| Panel NCI-60 (60 carcinoma cell lines) | GI50 |
0.01 nM
Compound: 1
|
Cytotoxicity against human Panel NCI-60 (60 carcinoma cell lines) assessed as cell growth inhibition
Cytotoxicity against human Panel NCI-60 (60 carcinoma cell lines) assessed as cell growth inhibition
|
[PMID: 35072477] |
| SF-268 | GI50 |
0.006 nM
Compound: 1
|
Growth inhibition of human SF268 cells after 48 hrs by SRB assay
Growth inhibition of human SF268 cells after 48 hrs by SRB assay
|
[PMID: 28895394] |
| SF-268 | GI50 |
0.006 nM
Compound: 2
|
Growth inhibition of human SF268 cells after 48 hrs by SRB assay
Growth inhibition of human SF268 cells after 48 hrs by SRB assay
|
[PMID: 28926240] |
| SF-295 | GI50 |
0.01 nM
Compound: 1
|
Anticancer activity against human SF-295 cells assessed as growth inhibition
Anticancer activity against human SF-295 cells assessed as growth inhibition
|
[PMID: 35072477] |
| SK-MEL-5 | GI50 |
0.009 nM
Compound: 1
|
Anticancer activity against human SK-MEL-5 cells assessed as growth inhibition
Anticancer activity against human SK-MEL-5 cells assessed as growth inhibition
|
[PMID: 35072477] |
Dolastatin 10 is a unique pentapeptide that isolated from the sea hare Dolabella auricularia. These in vitro data are quite comparable to those of Dolastatin 10 and Auristatin PE, each of which has GI50 values of 10?5-10?6 μg/mL (10?2-10?3 nM) against a similar minipanel of human cell lines[2]. The antibody-drug conjugate (ADC) comprises the anti-CD30 monoclonal antibody cAC10 conjugated to the cytotoxic agent monomethyl auristatin E (MMAE), a synthetic analog of the tubulin polymerization inhibitor Dolastatin 10[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 110417-88-4
-
Appearance Solid
-
Molecular Weight 785.09
-
Formula C42H68N6O6S
-
Color White to off-white
-
SMILES
O=C([C@H](C)[C@H]([C@]1([H])CCCN1C(C[C@@H](OC)[C@H]([C@@H](C)CC)N(C([C@@H](NC([C@@H](N(C)C)C(C)C)=O)C(C)C)=O)C)=O)OC)N[C@@H](CC2=CC=CC=C2)C3=NC=CS3
-
Synonyms
DLS 10; NSC 376128
-
Structure Classification
-
Initial Source
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * The compound is unstable in solutions, freshly prepared is recommended.
Solvent & Solubility
DMSO : ≥ 100 mg/mL (127.37 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (276 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[3]. Brentuximab vedotin. Drugs R D. 2011;11(1):85-95. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.2737 mL | 6.3687 mL | 12.7374 mL | 31.8435 mL |
| 5 mM | 0.2547 mL | 1.2737 mL | 2.5475 mL | 6.3687 mL | |
| 10 mM | 0.1274 mL | 0.6369 mL | 1.2737 mL | 3.1843 mL | |
| 15 mM | 0.0849 mL | 0.4246 mL | 0.8492 mL | 2.1229 mL | |
| 20 mM | 0.0637 mL | 0.3184 mL | 0.6369 mL | 1.5922 mL | |
| 25 mM | 0.0509 mL | 0.2547 mL | 0.5095 mL | 1.2737 mL | |
| 30 mM | 0.0425 mL | 0.2123 mL | 0.4246 mL | 1.0614 mL | |
| 40 mM | 0.0318 mL | 0.1592 mL | 0.3184 mL | 0.7961 mL | |
| 50 mM | 0.0255 mL | 0.1274 mL | 0.2547 mL | 0.6369 mL | |
| 60 mM | 0.0212 mL | 0.1061 mL | 0.2123 mL | 0.5307 mL | |
| 80 mM | 0.0159 mL | 0.0796 mL | 0.1592 mL | 0.3980 mL | |
| 100 mM | 0.0127 mL | 0.0637 mL | 0.1274 mL | 0.3184 mL |