Cat. No.: HY-109565

Tolinapant

Name: Tolinapant
Brand: MedChemExpress
SKU: HY-109565
Price: 95.00 USD
Availability: InStock
Rating: 5 (5 reviews)

(Synonyms: ASTX660)

5 Cited Publications

고객리뷰

Based on 5 publication(s) in Google Scholar

Tolinapant (ASTX660) is an orally active cIAP1/2 and XIAP antagonist, with an IC₅₀ of < 40 nM against XIAP and an IC₅₀ of <12 nM against cIAP1. Tolinapant triggers TNFα-dependent Apoptosis in cancer cells. Tolinapant inhibits tumor growth in mouse xenograft models. Tolinapant can be used in research related to breast cancer, melanoma, lymphoma, multiple myeloma, acute lymphoblastic leukemia and advanced solid tumors.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity : 99.81%
CAS No.: 1799328-86-1
화학식: C₃₀H₄₂FN₅O₃
분자량:539.68

보관:

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

Tolinapant Chemical Structure

CAS No.: 1799328-86-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (5)
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

cIAP1

<12 nM (IC₅₀)

cIAP2

XIAP

＜40 nM (IC₅₀)

All TNF Receptor Isoforms :

All IAP Isoforms :

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

ApoptosisAnti-cancerCytokines & ChemokinesAdaptive Immunity

Apoptosis

Tolinapant dihydrochloride potently inhibits the binding of SMAC peptides to purified XIAP-BIR3 (IC₅₀ <40 nM) and cIAP1-BIR3 (IC₅₀ <12 nM) proteins by occupying the endogenous SMAC-binding pocket^[1].
Tolinapant (0.001-10 μM; 5 min-16 h) dihydrochloride antagonizes endogenous XIAP in A375 melanoma cells, and displaces SMAC from XIAP at concentrations above 0.01 μM after 16 h, or within 5 min at a concentration of 1 μM^[1].

Apoptosis

Anti-cancer

Tolinapant (72 h) dihydrochloride inhibits the viability of most melanoma cell lines, with enhanced activity in the presence of TNFα, and exerts no significant effect on the viability of normal skin fibroblasts^[1].

Anti-cancer

Cytokines & Chemokines

Tolinapant dihydrochloride exhibits single-agent or TNFα-potentiated anti-survival activity in 43% of the tested triple-negative breast cancer (TNBC) cell lines, including MDA-MB-231, HCC38, HCC1806, Hs578T, BT549, HCC1395, DU4475, MDA-MB-453, and the mouse EMT6 cell line^[3].
Tolinapant (1-3 μM; 24 h) dihydrochloride significantly enhances the lytic activity of NY-ESO-1 TCR-T cells against A375 melanoma cells, and this effect is dependent on TNF-α^[4].
Tolinapant (0.01-1 μM; 48 h) dihydrochloride significantly enhances CD19 CAR-NK cell-mediated lysis of NALM6-Luc2 cells in a TNF-α-dependent manner^[4].

Anti-cancer

Adaptive Immunity

Tolinapant (3 μM; for at least 33 days) dihydrochloride enhances the long-term proliferation and persistence of CD19 CAR-T cells, maintains their cytotoxic activity, and preserves the expression of the memory T cell marker CCR7 during repeated antigen stimulation^[4].

Anti-cancer

Apoptosis

Tolinapant dihydrochloride inhibits the proliferation of various cancer cell lines in a manner dependent on the presence of inflammatory stimulation^[5].

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

Western Blot Analysis^[1]

Cell Line:

A375 human melanoma cells
Concentration:

0.001-10 μmol/L (16 h incubation); 1 μmol/L (short-term incubation)
Incubation Time:

16 h (0.001-10 μmol/L); 5-240 min (1 μmol/L)
Result:

Reduced SMAC levels immunoprecipitated with XIAP at concentrations above 0.01 μmol/L after 16 hours of treatment.
Antagonized the interaction of SMAC with XIAP within 5 minutes of exposure to 1 μmol/L.

Cell Proliferation Assay^[4]

Cell Line:

human CD19 CAR-T cells, NALM6-Luc2 (B-ALL)
Concentration:

3 μM
Incubation Time:

at least 33 days
Result:

Increased CD19 CAR-T cell growth rate relative to DMSO control, with CAR-T cells persisting for at least 33 days (compared to decline by Day 18 in controls).
Maintained specific lysis of NALM6-Luc2 cells at consistently high 80-90% throughout the study period.
Preserved expression of the memory T cell marker CCR7.

In Vivo

Anti-cancerApoptosisOthersAdaptive Immunity

Anti-cancer

Apoptosis

Tolinapant (5-20 mg/kg; p.o.; daily; 25 days; 20 mg/kg; p.o.; 7 days on/7 days off; 2 cycles) dihydrochloride significantly inhibits MDA-MB-231 breast cancer xenograft growth in SCID mice, with prolonged pharmacodynamic effects including cIAP1 degradation, XIAP antagonism, and apoptosis induction^[1].

Anti-cancer

Tolinapant (10-20 mg/kg; p.o.; daily; 14 days) dihydrochloride significantly inhibits A375 melanoma xenograft growth in nude mice^[1].

Others

Tolinapant (30-100 mg/kg; p.o.; daily; 7-14 days) dihydrochloride achieves complete on-target engagement via full cIAP1 protein degradation in cynomolgus NHP PBMCs^[2].

Anti-cancer

Adaptive Immunity

Tolinapant (16 mg/kg; p.o.; once daily; 21 days) dihydrochloride enhances the in vivo anti-tumor efficacy of low-dose MMG49 CAR-T cells in a disseminated multiple myeloma xenograft model by accelerating CAR-T cell proliferation and persistence, enabling tumor control equivalent to a 10-fold higher dose of CAR-T cells alone^[4].

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

Animal Model:

BALB/cJHanHsd-Prkdcscid (male)^[1]
Dosage:

5 mg/kg; 10 mg/kg; 20 mg/kg; 20 mg/kg (intermittent schedule)
Administration:

p.o.; daily; 25 days; p.o.; 7 days on/7 days off; 2 cycles
Result:

Significantly inhibited tumor growth (P < 0.05 from days 15, 18, and 11 for 5, 10, and 20 mg/kg daily dosing, respectively).
Achieved significant tumor growth inhibition (P < 0.05 vs. vehicle from day 8) with intermittent 20 mg/kg schedule, equivalent to continuous 20 mg/kg daily schedule.
Distributed to tumors with detectable compound levels up to 168 hours post-dose (AUC_last = 129 μmol/L/h/mL).
Induced rapid cIAP1 degradation, reduced XIAP:SMAC association (persisting up to 3 days), and increased cleaved PARP and cleaved caspase-3 within 1 hour post-dose.
Showed no excessive body weight loss or adverse effects.

Animal Model:

BALB/cOlaHsd-Foxn1nu (male)^[1]
Dosage:

10 mg/kg; 20 mg/kg
Administration:

p.o.; daily; 14 days
Result:

Caused significant tumor growth inhibition (P < 0.05 from day 8).
Showed no excessive body weight loss or adverse effects.

Animal Model:

NOD/SCID/IL2Rγcnull (NOG) (6- to 8-week-old female; disseminated multiple myeloma xenograft model)^[4]
Dosage:

16 mg/kg
Administration:

p.o.; once daily; 21 days
Result:

Attenuated tumor expansion by day 11 and reduced tumor load thereafter when combined with 1×10⁵ MMG49 CAR-T cells, resulting in lower tumor load than treatment with 1×10⁶ MMG49 CAR-T cells alone by day 21.
Accelerated in vivo MMG49 CAR-T cell expansion, with significantly higher CAR-T cell numbers in the combination group than in the CAR-T monotherapy group between days 10 and 17.
Showed no anti-tumor effect when used alone.

Related Protocols :

Clinical Trial

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

Chemical Information

CAS No. 1799328-86-1
Appearance Solid
분자량 539.68
화학식 C₃₀H₄₂FN₅O₃
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
Synonyms

ASTX660
선적

Room temperature in continental US; may vary elsewhere.

보관

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

Publications (5)

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Journal Impact Factor

Cell Rep Med

Pharmacological Activation of Non-canonical NF-κB Signaling Activates Latent HIV-1 Reservoirs In Vivo. [Abstract]

2020 Jun 23;1(3):100037. PMID: 33205060
J Natl Cancer Inst

2026 Aug 8:djag266. PMID: 42569934
Cancer Gene Ther

b-AP15 enhances TRAIL-induced cell death in HNSCC via the induction of ROS/JNK/DR5 signalling. [Abstract]

2026 May 2. PMID: 42069980
Blood Res

Translational investigation of tolinapant (ASTX660) in acute myeloid leukemia by integrating clinical, bioinformatic and pharmacological approaches. [Abstract]

2025 Dec 30;60(1):67. PMID: 41469824
bioRxiv

SMAC mimetics induce human macrophages to phagocytose live cancer cells. [Abstract]

2024 Nov 28:2024.11.25.625306. PMID: 39651304

용액&용해도

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)

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

1.8529 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

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.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (301 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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)
Handling Instructions (2659 KB)

References

[1]. Ward GA, et al. ASTX660, a Novel Non-peptidomimetic Antagonist of cIAP1/2 and XIAP, Potently Induces TNFα-Dependent Apoptosis in Cancer Cell Lines and Inhibits Tumor Growth. Molecular cancer therapeutics. 2018 Jul;17(7):1381-1391. [Content Brief]

[2]. Martins V, et al. The preclinical pharmacokinetics of Tolinapant-A dual cIAP1/XIAP antagonist with in vivo efficacy. Pharmacology research & perspectives. 2024 Dec;12(6):e70030. [Content Brief]

[3]. Smyth T, et al. The dual IAP antagonist, ASTX660, increases the anti-tumor activity of paclitaxel in preclinical models of triple-negative breast cancer in vivo[J]. Cancer Research, 2016, 76(14_Supplement): 1287-1287.

[4]. Tazuru K, et al. The IAP antagonist tolinapant enhances the anti-tumor activity of cell therapies. European journal of pharmacology. 2025 May 15;995:177400. [Content Brief]

[5]. Mita MM, et al. A Phase I Study of ASTX660, an Antagonist of Inhibitors of Apoptosis Proteins, in Adults with Advanced Cancers or Lymphoma. Clinical cancer research : an official journal of the American Association for Cancer Research. 2020 Jun 15;26(12):2819-2826. [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

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.

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

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Tolinapant

5 Cited Publications

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Tolinapant

Publications Citing Use of MedChemExpress (MCE) Tolinapant

All TNF Receptor Isoforms

All IAP Isoforms