Referencia número: HY-15580

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Dolastatin 10

(Synonyms: DLS 10; NSC 376128)

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Dolastatin 10 (DLS 10) is a potent antimitotic peptide that inhibits tubulin polymerization.

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Pureza: 98.34%
No. CAS: 110417-88-4
Fòrmula: C₄₂H₆₈N₆O₆S
Peso molecular:785.09

Almacenamiento:

Sealed storage, away from moisture.

Powder -80°C, 2 years , -20°C, 1 year

* The compound is unstable in solutions, freshly prepared is recommended.

Dolastatin 10 Chemical Structure

No. CAS: 110417-88-4

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Ensayo clínico
Chemical Information
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Dolastatin 10 (DLS 10) is a potent antimitotic peptide that inhibits tubulin polymerization.

IC₅₀ & Target

Auristatin

Ver todos los productos específicos de isoformas ADC Payloads :

Cellular Effect

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]

In Vitro

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.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 110417-88-4
Appearance Solid
Peso molecular 785.09
Fòrmula 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
- Others
Initial Source
- Marine natural products
- Other marine organisms
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

* The compound is unstable in solutions, freshly prepared is recommended.

Solvente y solubilidad

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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

Keywords

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Referencia número:
Cantidad:
MCE Japan Authorized Agent:

Nombre del producto:
No. CAS:
Species:
Pureza:
Cantidad:

Dolastatin 10

Monomethyl auristatin E

MMAD

Eribulin

MMAF

Paclitaxel

Auristatin F

Monomethyl auristatin E (Standard)

Paclitaxel (Standard)

Eribulin mesylate

Lurtotecan

Monomethyl auristatin E (GMP)

Epothilone B

Ver todos los productos específicos de isoformas ADC Payloads

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Dolastatin 10

Monomethyl auristatin E

MMAD

Eribulin

MMAF

Paclitaxel

Auristatin F

Monomethyl auristatin E (Standard)

Paclitaxel (Standard)

Eribulin mesylate

Lurtotecan

Monomethyl auristatin E (GMP)

Epothilone B

Ver todos los productos específicos de isoformas ADC Payloads

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Dolastatin 10 Related Classifications

HY-15580 Related Classifications