Dolastatin 10 (Synonyms: DLS 10; NSC 376128)

Cat. No.: HY-15580 Purity: 98.11%: FAQs
Data Sheet SDS COA Handling Instructions

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

For research use only. We do not sell to patients.

Dolastatin 10 Chemical Structure

CAS No. : 110417-88-4

Size	Price	Stock	Quantity
1 mg	USD 260	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 650	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 980	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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

IC₅₀ & Target

Auristatin

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]
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]
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]
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]
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]
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]
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	0.01 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]
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]
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	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	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]
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	0.229 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]
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-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]

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.

Clinical Trial

Molecular Weight

785.09

Formula

C₄₂H₆₈N₆O₆S

CAS No.

110417-88-4

Appearance

Solid

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

Structure Classification

Others

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

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.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Concentration _(final)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.11%

Select Batch:

Data Sheet (275 KB) SDS (394 KB)

COA (254 KB) RP-HPLC (254 KB) MS (70 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

Dolastatin 10 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Dolastatin 10110417-88-4DLS 10 NSC 376128Dolastatin10Dolastatin-10DLS10DLS-10NSC376128NSC 376128NSC-376128Microtubule/TubulinADC CytotoxinADC PayloadInhibitorinhibitorinhibit

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