| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
The target is PI3Kα (p110α), with lower potency against PI3Kβ, PI3Kγ, and PI3Kδ. Vulolisib binds the ATP-binding pocket of PI3Kα and inhibits its lipid kinase activity, blocking AKT/mTOR signaling and reducing proliferation and survival in PI3Kα-dependent tumor cells.
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|---|---|
| ln Vitro |
Vulolisib exhibits antiproliferative action against the PI3Kα mutant cell lines HCC1954 (H1047R), MKN1 (E545K), and HGC-27 (E542K), with IC50 values of 21 nM, 60 nM, and 40 nM, in that order [1].
Vulolisib inhibits PI3Kα with an IC50 of 0.2 nM, PI3Kβ with 168 nM, PI3Kγ with 90 nM, and PI3Kδ with 49 nM, demonstrating strong PI3Kα selectivity. It shows antiproliferative activity against cancer cells expressing mutated or amplified PI3Kα. |
| ln Vivo |
Vulolisib (10, 30, and 60 mg/kg; IG; administered daily for 7 days) revealed superior tolerance and exposure than inavolisib [1]. Vulolisib (10 mg/kg; oral; once daily for 19 days) reduced tumor growth with a TGI of 132% [1]. Vulolisib (5 mg/kg; IG, single dose) showed excellent pharmacokinetic characteristics [1]. Pharmacokinetic characteristics of Vulolisib in male Balb/c mice [1]. IG (5 mg/kg) tmax (h) 0.5 Cmax (ng/mL) 1057 AUC0-t (ng/mL·h) 2185 AUC0-∞ (ng/mL·h) 2274 t1/2 (h) 1.6 MRT ( h) 2.2
No standard in vivo efficacy data are publicly established for vulolisib in accessible summaries. It is an orally active research compound with antiproliferative activity; compound-specific animal efficacy and pharmacokinetic datasets are limited, and it remains a preclinical tool. |
| Enzyme Assay |
PI3Kα kinase activity is measured using recombinant PI3Kα and a fluorescent or biotinylated PIP2 substrate in the presence of ATP; ADP generation is detected by fluorescence polarization or TR-FRET, and IC50 values are derived. Selectivity is confirmed against PI3Kβ, PI3Kγ, PI3Kδ, and mTOR.
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| Cell Assay |
PI3Kα-dependent cancer cells (e.g., PIK3CA-mutant lines) are treated with vulolisib; viability is measured by CellTiter-Glo, and phospho-AKT (Ser473) and downstream targets are assessed by immunoblotting. Apoptosis is measured by annexin V flow cytometry.
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| Animal Protocol |
Animal/Disease Models: SD (SD (Sprague-Dawley)) rat [1]
Doses: 10, 30 and 60 mg/kg Route of Administration: IG; one time/day for 7 days Experimental Results: Demonstrated better tolerability and exposure than inavolisib quantity. Animal/Disease Models: Female BALB/c nude mice (6-8 weeks; injected with HCC1954) [1] Doses: 10mg/kg Route of Administration: PO; one time/day for 19 days. Experimental Results: Inhibited tumor growth, TGI was 132%. Animal/Disease Models: Male balb/c (Bagg ALBino) mouse [1] Doses: 5 mg/kg Route of Administration: IG, single dose (pharmacokinetic/PK/PK analysis) Experimental Results: demonstrated good pharmacokinetic/PK/PK properties. No standardized animal protocol is published for vulolisib. If evaluated, immunodeficient mice bearing PI3Kα-dependent xenografts would receive the compound orally; tumor volume would be measured serially, and tumors would be analyzed for phospho-AKT and apoptosis markers, but published in vivo datasets are insufficient. |
| References |
| Molecular Formula |
C18H19F2N5O3S
|
|---|---|
| Molecular Weight |
423.436969041824
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| Exact Mass |
423.117
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| CAS # |
2390105-79-8
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| PubChem CID |
146267141
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| Appearance |
White to off-white solid powder
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| LogP |
2
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| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
645
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| Defined Atom Stereocenter Count |
2
|
| SMILES |
N(C1=CC=C2C3=NC(N4C(SC[C@H]4C(F)F)=O)=CN3CCOC2=C1)[C@@H](C)C(=O)N
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| InChi Key |
KEEKMOIRJUWKNK-CABZTGNLSA-N
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| InChi Code |
InChI=1S/C18H19F2N5O3S/c1-9(16(21)26)22-10-2-3-11-13(6-10)28-5-4-24-7-14(23-17(11)24)25-12(15(19)20)8-29-18(25)27/h2-3,6-7,9,12,15,22H,4-5,8H2,1H3,(H2,21,26)/t9-,12-/m0/s1
|
| Chemical Name |
(2S)-2-[[2-[(4R)-4-(difluoromethyl)-2-oxo-1,3-thiazolidin-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]amino]propanamide
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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 |
| 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) |
DMSO: ~100 mg/mL (~236.2 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.90 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.90 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3616 mL | 11.8080 mL | 23.6161 mL | |
| 5 mM | 0.4723 mL | 2.3616 mL | 4.7232 mL | |
| 10 mM | 0.2362 mL | 1.1808 mL | 2.3616 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.
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