Hemiasterlin (Synonyms: (-)-Hemiasterlin; Milnamide B)

Name: Hemiasterlin
Brand: MedChemExpress
SKU: HY-117371
Rating: 4.5 (1 reviews)

Cat. No.: HY-117371 Purity: 99.77%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Hemiasterlin ((-)-Hemiasterlin) is an antimitotic marine natural product with potent anticancer effcts. Hemiasterlin can be used as a cytotoxic payload (ADC Cytotoxin) in antibody-drug conjugates (ADCs).

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

Hemiasterlin Chemical Structure

CAS No. : 157207-90-4

Size	Price	Stock	Quantity
5 mg	USD 765	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1230	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 2460	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 3950	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 6320	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Pyrrolobenzodiazepines

Cellular Effect

Cell Line	Type	Value	Description	References
KB	IC₅₀	76 nM Compound: 1	Concentration required to kill human epidermoid KBV1 cell lines containing very high levels of P-glycoprotein after 3 days of continuous exposure Concentration required to kill human epidermoid KBV1 cell lines containing very high levels of P-glycoprotein after 3 days of continuous exposure	[PMID: 15454219]
KB 3-1	IC₅₀	0.3 nM Compound: 1	Concentration required to kill human epidermoid KB-3-1 cell lines containing very low levels of P-glycoprotein after 3 days of continuous exposure Concentration required to kill human epidermoid KB-3-1 cell lines containing very low levels of P-glycoprotein after 3 days of continuous exposure	[PMID: 15454219]
KB 3-1	IC₅₀	1 nM Compound: 1	Concentration required to kill human epidermoid KB85 cell lines containing moderate levels of P-glycoprotein after 3 days of continuous exposure Concentration required to kill human epidermoid KB85 cell lines containing moderate levels of P-glycoprotein after 3 days of continuous exposure	[PMID: 15454219]
MCF7	IC₅₀	0.3 nM Compound: 1	Antimitotic activity against human MCF7 cells expressing p53 mutant by MTT assay Antimitotic activity against human MCF7 cells expressing p53 mutant by MTT assay	[PMID: 12608848]
MCF7	IC₅₀	0.3 nM Compound: 1	Cytotoxicity activity against human MCF7 cells expressing p53 mutant by MTT assay Cytotoxicity activity against human MCF7 cells expressing p53 mutant by MTT assay	[PMID: 12608848]
MCF7	ED₅₀	0.5 nM Compound: hemiasterlin	Antiproliferative activity against human MCF7 cells after 20 hrs by microculture tetrazolium assay Antiproliferative activity against human MCF7 cells after 20 hrs by microculture tetrazolium assay	[PMID: 26821210]

In Vitro

Hemiasterlin is an antimitotic agent by disrupting microtubule dynamics causing mitotic arrest and cell death with low- to sub-nanomolar potencies against several cancer cell lines^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

526.71

Formula

C₃₀H₄₆N₄O₄

CAS No.

157207-90-4

Appearance

Solid

Color

White to off-white

SMILES

OC(/C(C)=C/[C@H](C(C)C)N(C)C([C@H](C(C)(C)C)NC([C@@H](NC)C(C)(C1=CN(C)C2=CC=CC=C12)C)=O)=O)=O

Structure Classification

Initial Source

Animals

marine sponges

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (189.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8986 mL	9.4929 mL	18.9858 mL
5 mM	0.3797 mL	1.8986 mL	3.7972 mL
10 mM	0.1899 mL	0.9493 mL	1.8986 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.75 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.75 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.75 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.77%

Select Batch:

Data Sheet (271 KB) SDS (252 KB)

COA (248 KB) HNMR (396 KB) LCMS (131 KB)

Handling Instructions (2659 KB)

References

[1]. Jiraborrirak Charoenpattarapreeda, et al. Expeditious Total Synthesis of Hemiasterlin through a Convergent Multicomponent Strategy and Its Use in Targeted Cancer Therapeutics. Angew Chem Int Ed Engl. 2020 Dec 14;59(51):23045-23050. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.8986 mL	9.4929 mL	18.9858 mL	47.4644 mL
	5 mM	0.3797 mL	1.8986 mL	3.7972 mL	9.4929 mL
	10 mM	0.1899 mL	0.9493 mL	1.8986 mL	4.7464 mL
	15 mM	0.1266 mL	0.6329 mL	1.2657 mL	3.1643 mL
	20 mM	0.0949 mL	0.4746 mL	0.9493 mL	2.3732 mL
	25 mM	0.0759 mL	0.3797 mL	0.7594 mL	1.8986 mL
	30 mM	0.0633 mL	0.3164 mL	0.6329 mL	1.5821 mL
	40 mM	0.0475 mL	0.2373 mL	0.4746 mL	1.1866 mL
	50 mM	0.0380 mL	0.1899 mL	0.3797 mL	0.9493 mL
	60 mM	0.0316 mL	0.1582 mL	0.3164 mL	0.7911 mL
	80 mM	0.0237 mL	0.1187 mL	0.2373 mL	0.5933 mL
	100 mM	0.0190 mL	0.0949 mL	0.1899 mL	0.4746 mL

Hemiasterlin 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:

Hemiasterlin157207-90-4(-)-Hemiasterlin Milnamide BADC CytotoxinADC Payloadantimitoticanticancer effctsADCInhibitorinhibitorinhibit

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Hemiasterlin (Synonyms: (-)-Hemiasterlin; Milnamide B)

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Hemiasterlin Related Antibodies

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Hemiasterlin Related Antibodies

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Complete Stock Solution Preparation Table

Hemiasterlin Related Classifications

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