| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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Purity: ≥98%
Inavolisib (RG6114; GDC0077), extracted from patent WO 2017001645 A1, formula I, is a novel, potent and orally bioavailable PI3K inhibitor with potential anticancer activity. It acts by blocking PI3K which is overactive in cancer. Inhibition of PI3K prevents the activation of the PI3K-mediated signaling pathway and results in the inhibition of growth and survival of PI3K-overexpressing tumor cells.
| Targets |
PI3Kα (IC50 = 0.038 nM)
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|---|---|
| ln Vitro |
GDC-0077 effectively inhibits mutant PI3K pathway signaling and cell viability through unique HER2-dependent mutant p110a degradation.[2]
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| ln Vivo |
GDC-0077 treatment at the MTD in vivo results in tumor regressions in multiple PIK3CA-mutant xenograft and patient-derived xenograft models.[2]
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| Enzyme Assay |
Dorsomorphin dihydrochloride (BML-275 dihydrochloride; Compound C dihydrochloride) is a potent, selective and ATP-competitiveAMPKinhibitor, with aKiof 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptorsALK2,ALK3, andALK6.
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| Cell Assay |
ATP-based cell viability assay in Colon cancer cell lines. Colon cancer cell lines treated with GDC-0077 at gradient concentrations for 24 hours underwent a Western blot to measure the levels of the protein p110a and pAKT signaling.
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| Animal Protocol |
Female NCR nude mice inoculated with HCC1954 tumor cells, female NOD-SCID gamma mice inoculated with WHIM20 tumor cells, female NOD-SCID gamma mice inoculated with HCI-003 tumor cells
25 mg/kg Oral gavage |
| References |
| Molecular Formula |
C18H19F2N5O4
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|---|---|
| Molecular Weight |
407.3714
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| Exact Mass |
407.1405
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| Elemental Analysis |
C, 53.07; H, 4.70; F, 9.33; N, 17.19; O, 15.71
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| CAS # |
2060571-02-8
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| Related CAS # |
2060571-02-8
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| Appearance |
Solid powder
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| SMILES |
C[C@@H](C(=O)N)NC1=CC2=C(C=C1)C3=NC(=CN3CCO2)N4[C@@H](COC4=O)C(F)F
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| InChi Key |
SGEUNORSOZVTOL-CABZTGNLSA-N
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| InChi Code |
InChI=1S/C18H19F2N5O4/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
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| Chemical Name |
(2S)-2-[[2-[(4S)-4-(difluoromethyl)-2-oxo-1,3-oxazolidin-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]amino]propanamide
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| Synonyms |
GDC-0077; RG-6114; GDC 0077; RG 6114; GDC0077; RG6114
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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: 81~110 mg/mL (198.8~270 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (6.75 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (6.75 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.11 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.08 mg/mL (5.11 mM) (saturation unknown) 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. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. Solubility in Formulation 5: ≥ 0.55 mg/mL (1.35 mM) (saturation unknown) in 1% DMSO 99% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4548 mL | 12.2739 mL | 24.5477 mL | |
| 5 mM | 0.4910 mL | 2.4548 mL | 4.9095 mL | |
| 10 mM | 0.2455 mL | 1.2274 mL | 2.4548 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 |
| NCT04632992 | Active Recruiting |
Drug: Inavolisib Drug: Alectinib |
Advanced Unresectable | Genentech, Inc. | January 13, 2021 | Phase 2 |
| NCT05646862 | Recruiting | Drug: Inavolisib Drug: Alpelisib |
Breast Cancer | Hoffmann-La Roche | June 7, 2023 | Phase 3 |
| NCT04191499 | Recruiting | Drug: Inavolisib Drug: Placebo |
Breast Cancer | Hoffmann-La Roche | January 29, 2020 | Phase 2 Phase 3 |
| NCT03006172 | Recruiting | Drug: Inavolisib Drug: Fulvestrant |
Breast Cancer Solid Tumor |
Genentech, Inc. | December 13, 2016 | Phase 1 |
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