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Purity: ≥98%
Serabelisib (formerly known as INK-1117, MLN-1117, and/or TAK-117) is a potent, selective, and oral bioavailable inhibitor of PI3Kα (phosphoinositide 3-kinase) isoform with IC50 of 21 nmol/L against PI3Kα. It demonstrated a high level of selectivity against many other kinases and > 100-fold selectivity compared to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR. B and T lymphocyte clonal expansion, differentiation, and effector function are all dependent on class IA PI3K. The p110δ catalytic isoform of PI3K is highly expressed in lymphocytes and plays a prominent role in B and T cell responses. Although p110, a different class IA PI3K catalytic isoform, is a promising drug target in cancer, little is known about its role in lymphocytes. The marginal zone B cell compartment and T cell-dependent germinal center formation were not disrupted in mice when specific p110α inhibition using the investigational compound MLN1117 (previously known as INK1117) was used.
| Targets |
p110α (IC50 = 15 nM); p110β (IC50 = p110 nM); p110δ (IC50 = 13900 nM); p110γ (IC50 = 1900 nM); mTOR (IC50 = 1670 nM)
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| ln Vitro |
Serabelisib (MLN1117) inhibits Akt phosphorylation and growth in PIK3CA mutant breast cancer cells with IC50s around 2 μM, yet has no effect on cells lacking PTEN. BCR-stimulated B cells were given a 1 mM dose. By using intracellular flow cytometry, serabelisib (MLN1117) exhibits a significant reduction (up to 50%) in the strength of the phosphorylated Akt (p-Akt) signal. Serabelisib has a dose-dependent effect[1].
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| ln Vivo |
Treatment with Serabelisib (MLN1117) at 30 and 60 mg/kg causes little reduction of TNP-specific IgG3. Notably, reduction of TNP-specific IgG3 at higher doses of Serabelisib (MLN1117) (120 mg/kg) is observed, consistent with the partial reduction in cell division in B cells treated with Serabelisib before anti-IgM stimulation. However, 120 mg/kg is above the effective dose of Serabelisib (MLN1117) for tumor growth inhibition (30-60 mg/kg)[1].
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| Enzyme Assay |
TAK-117 administration in PIK3CA-mutant tumor cell lines results in potent PI3K pathway inhibition, blockade of cellular proliferation, and apoptosis. INK1117 potently inhibits PI3K and demonstrates a greater than 100-fold selectivity relative to other class I PI3K family members and mTOR as well as a high degree of selectivity against a large panel of protein kinases. INK1117 blocks proliferation of tumor cell lines bearing PIK3CA mutations, and inhibits cellular phosphorylation and activity of AKT. However, INK1117 shows much less activity in PTEN-deficient tumor cells, which typically display constitutive PI3K pathway activation independent of PI3Kα.
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| Cell Assay |
A total of 5000 SK-OV-3 and U87MG cell lines are seeded in triplicate wells of a 96-well flat bottom culture plate and allowed to adhere for 18 hours in low serum media (0.2% FBS). Inhibitors in 0.2% FBS media are added to each well at the specified concentrations after the media is aspirated. Utilizing the MTS assay (Cell Titer 96 Aqueous One solution cell proliferation assay kit), cell viability is assessed after 48 hours while absorbance (490 nm) is measured in a microplate spectrophotometer[1].
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| Animal Protocol |
Mice: For all experiments, wild-type Balb/cJ mice aged 8 weeks are used. Using a sterile, one-time-use 1.5′ feeding needle, patients are administered serabelisib and GDC-0941 via oral gavage. Intraperitoneal injection is used to administer IC87114. In the non-immunization experiment, two mice from each of the three groups (Vehicle, GDC-0941, and Serabelisib (MLN1117)) receive the prescribed medications for nine days before being sacrificed on day ten. Two separate studies contrasting Serabelisib (MLN1117) with GDC-0941 or IC87114 were conducted for the immunization experiment using four mice per group. The vehicle group always receives both vehicles that were used to create the two unique drugs. From day one to day thirteen, mice are given the medications. All mice receive the NP-OVA vaccine, precipitated in alum, on day 0. On day 13, the drug treatment is stopped, and mice are killed for the purpose of collecting their spleens and serum.
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| References |
| Molecular Formula |
C19H17N5O3
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| Molecular Weight |
363.37
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| Exact Mass |
363.1331
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| Elemental Analysis |
C, 62.80; H, 4.72; N, 19.27; O, 13.21
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| CAS # |
1268454-23-4
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| Related CAS # |
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| Appearance |
Brown solid powder
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| SMILES |
C1COCCN1C(=O)C2=CN=C3N2C=C(C=C3)C4=CC5=C(C=C4)OC(=N5)N
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| InChi Key |
BLGWHBSBBJNKJO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H17N5O3/c20-19-22-14-9-12(1-3-16(14)27-19)13-2-4-17-21-10-15(24(17)11-13)18(25)23-5-7-26-8-6-23/h1-4,9-11H,5-8H2,(H2,20,22)
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| Chemical Name |
[6-(2-amino-1,3-benzoxazol-5-yl)imidazo[1,2-a]pyridin-3-yl]-morpholin-4-ylmethanone
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7520 mL | 13.7601 mL | 27.5202 mL | |
| 5 mM | 0.5504 mL | 2.7520 mL | 5.5040 mL | |
| 10 mM | 0.2752 mL | 1.3760 mL | 2.7520 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Status | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05300048 | Recruiting | Drug: Serabelisib Drug: Nab paclitaxel |
PIK3CA Mutation Advanced Solid Tumor |
Faeth Therapeutics | April 22, 2022 | Phase 1 |
| NCT02625259 | Completed | Drug: TAK-117 Drug: Lansoprazole |
Neoplasm, Advanced | Millennium Pharmaceuticals, Inc. |
January 8, 2016 | Phase 1 |
| NCT01449370 | Completed | Drug: TAK-117 | Metastatic Solid Tumors | Millennium Pharmaceuticals, Inc. |
October 2011 | Phase 1 |
| NCT02724020 | Completed | Drug: MLN1117 Drug: MLN0128 |
Clear-cell Metastatic Renal |
Millennium Pharmaceuticals, Inc. |
June 30, 2016 | Phase 2 |
| NCT03193853 | Completed | Drug: Tak-228 & Tak-117 | Triple Negative Breast Cancer |
Joyce O'Shaughnessy | July 18, 2017 | Phase 2 |
Expression of TAZ and Osterix, markers of commitment to osteoblastogenesis in human ADSC. Toxicol Appl Pharmacol. 2013 Oct 15;272(2):399-407 |
Time course of serum bone turnover biomarkers and femur histopathology changes with AZD2858 dosed orally for 3, 7, 14, 21 or 28 days |
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