| Field | Specification |
|---|---|
| Alternative names | APG-1387 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C60H72N10O10S2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Dasminapant, also known as APG-1387, is a bivalent SMAC mimetic and IAP antagonist that blocks the activity of IAP family proteins, including XIAP, cIAP-1, cIAP-2 and ML-IAP. It induces degradation of cIAP-1 and XIAP proteins, as well as caspase-3 activation and PARP cleavage, leading to apoptosis, and it can be used for the research of hepatocellular carcinoma, ovarian cancer and nasopharyngeal carcinoma[1][2][3][4][5]. It is supplied as a white to off-white solid (C60H72N10O10S2, MW 1157.40) at 99.70% purity.
Physical & Chemical Properties
| CAS Number | 1570231-89-8 |
|---|---|
| Molecular Formula | C60H72N10O10S2 |
| Molecular Weight | 1157.40 g/mol |
| Purity | 99.70% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=S(C1=CC=CC(S(=O)(N(C[C@@H]2NC([C@@H](NC)C)=O)CC[C@](CC[C@H]3C(NC(C4=CC=CC=C4)C5=CC=CC=C5)=O)([H])N3C2=O)=O)=C1)(N(C[C@@H]6NC([C@@H](NC)C)=O)CC[C@](CC[C@H]7C(NC(C8=CC=CC=C8)C9=CC=CC=C9)=O)([H])N7C6=O)=O |
| Signaling Pathway | Apoptosis |
| Solubility | In Vitro: DMSO: 50 mg/mL (43.20 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O: < 0.1 mg/mL (insoluble) |
| Storage | -20°C, stored under nitrogen. In solvent: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[4]. Li Q, et al. Abstract 6216: Therapeutic potential of IAP inhibitor APG-1387 in combination with PARP- or MEK-targeted therapy, or chemotherapy in pancreatic cancer. American Association for Cancer Research. Aug 2020. 80(16).
[5]. Pan w, et al. Abstract 1754: Smac mimetics APG-1387 synergizes with immune checkpoint inhibitors in preclinical models. American Association for Cancer Research. Jul 2018. 78(13).
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 50 mg/mL (43.20 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
| H2O | < 0.1 mg/mL | insoluble |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); stored under nitrogen; avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (2.16 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | 2.5 mg/mL (2.16 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 2.5 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (2.16 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
In HepG2 and HCCLM3 cells, Dasminapant (0.02-20 μM; 24 h) triggers rapid cIAP degradation[1]. TNF-α- and TRAIL-mediated anti-cancer activities are enhanced by Dasminapant (2 μM; 24 h) in HepG2 and HCCLM3 cells. HepG2 and HCCLM3 cells are sensitized by Dasminapant to NK cell-mediated killing in vitro[1].
Western Blot Analysis[1]
| Cell Line | HepG2 and HCCLM3 cells |
|---|---|
| Concentration | 0.02, 0.2, 2, 20 μM |
| Incubation Time | 1, 6, 24 hours |
| Result | Decreased the expression of cIAP1 and cIAP2 in both cell lines in a dose- and time-dependent manner. Inhibited the expression of X chromosome-linked IAP (XIAP) at a high dose. |
In Vivo
In mice, Dasminapant (20 mg/kg; i.p. every 3 days for 4 weeks) makes HCCLM3 tumors more sensitive to NK cell-mediated killing[1]. As monotherapy, Dasminapant (20 mg/kg; i.p. every 3 days for 4 weeks) has some degree of anti-tumor effect and is well tolerated in mice[1].
| Animal Model | Non-obese diabetic and severe combined immunodeficiency (NOD-SCID) mice bearing HCCLM3 tumors are injected with NK cells[1] |
|---|---|
| Dosage | 20 mg/kg |
| Administration | I.p. every 3 days for 4 weeks |
| Result | Decreased the expression of cIAP1 and cIAP2, and less potent to XIAP expression. Potentiated the effects of pre-activated NK cells on HCCLM3 xenograft tumor growth and tumor weight. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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