Tolinapant (Synonyms: ASTX660)

Name: Tolinapant
Brand: MedChemExpress
SKU: HY-109565
Rating: 5.0 (1 reviews)

Cat. No.: HY-109565 Purity: 99.81%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Tolinapant (ASTX660) is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).

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

Tolinapant Chemical Structure

CAS No. : 1799328-86-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 214	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 214	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 95	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 850	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1450	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE Tolinapant

•Cell Reports Medicine. 2020 Jun 23;1(3):100037. [Abstract]

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cIAP cIAP-1 cIAP-2 XIAP

Biological Activity
Purity & Documentation
References
Customer Review

Description

Tolinapant (ASTX660) is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).

IC₅₀ & Target

cIAP, XIAP^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-231	IC₅₀	1.8 nM Compound: 27; ASTX660	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by Alamar blue assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by Alamar blue assay	[PMID: 30091600]

In Vitro

Tolinapant is an orally bioavailable dual antagonist of cIAP and XIAP, currently being investigated in a single-agent Phase 1/2 clinical trial in patients with advanced solid tumors and lymphomas. Twenty-one triple-negative breast cancer (TNBC) cell lines are treated with Tolinapant in vitro and it is found that 43% are sensitive to Tolinapant^[1].

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

In Vivo

In HCC1806 xenografts in mice, Tolinapant (daily oral treatment) causes moderate tumor growth inhibition but not regression^[1].

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

Clinical Trial

Molecular Weight

539.68

Formula

C₃₀H₄₂FN₅O₃

CAS No.

1799328-86-1

Appearance

Solid

Color

White to off-white

SMILES

C[C@H]1N(C[C@@H]2N(CC(N3CC(C)(C)C4=NC(CO)=C(CC5=CC=C(F)C=C5)C=C43)=O)C[C@@H](C)NC2)CCOC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (185.29 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	1.8529 mL	9.2647 mL	18.5295 mL
5 mM	0.3706 mL	1.8529 mL	3.7059 mL
10 mM	0.1853 mL	0.9265 mL	1.8529 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 (4.63 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 (4.63 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 (4.63 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).

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: 99.81%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (254 KB) HNMR (266 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Tomoko Smyth, et al. Abstract 1287: The dual IAP antagonist, ASTX660, increases the anti-tumor activity of NSC 125973 in preclinical models of triple-negative breast cancer in vivo. Cancer Res 2016;76(14 Suppl).

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.8529 mL	9.2647 mL	18.5295 mL	46.3237 mL
	5 mM	0.3706 mL	1.8529 mL	3.7059 mL	9.2647 mL
	10 mM	0.1853 mL	0.9265 mL	1.8529 mL	4.6324 mL
	15 mM	0.1235 mL	0.6176 mL	1.2353 mL	3.0882 mL
	20 mM	0.0926 mL	0.4632 mL	0.9265 mL	2.3162 mL
	25 mM	0.0741 mL	0.3706 mL	0.7412 mL	1.8529 mL
	30 mM	0.0618 mL	0.3088 mL	0.6176 mL	1.5441 mL
	40 mM	0.0463 mL	0.2316 mL	0.4632 mL	1.1581 mL
	50 mM	0.0371 mL	0.1853 mL	0.3706 mL	0.9265 mL
	60 mM	0.0309 mL	0.1544 mL	0.3088 mL	0.7721 mL
	80 mM	0.0232 mL	0.1158 mL	0.2316 mL	0.5790 mL
	100 mM	0.0185 mL	0.0926 mL	0.1853 mL	0.4632 mL

Tolinapant 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:

Tolinapant1799328-86-1ASTX660ASTX 660ASTX-660IAPApoptosisInhibitorinhibitorinhibit

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Tolinapant (Synonyms: ASTX660)

Customer Review

Tolinapant Related Antibodies

1 Publications Citing Use of MCE Tolinapant

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All IAP Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Tolinapant Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Tolinapant Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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