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Mobocertinib (TAK-788; AP-32788; Exkivity), a drug used for the treatment of non-small cell lung cancer (NSCLC), is a novel, highly potent, irreversible and orally bioavailable inhibitor of EGFR and HER2 oncogenic mutants (e.g. exon 20 insertions), and exhibits high selectivity over WT EGFR. It has antitumor activity. It functions as an antitumor. For metastatic NSCLC with EGFR exon 20 insertion mutations, the FDA expedites approval of mobocertinib on September 15, 2021.
| Targets |
EGFR (WT); EGFR exon 20 insertion; HER2
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|---|---|
| ln Vitro |
Mobocertinib (TAK-788) is a novel irreversible EGFR TKI that has been carefully engineered to selectively and potently inhibit oncogenic variants with activating EGFRex20ins mutations while leaving wild-type EGFR alone. More potently than approved EGFR TKIs, mobocertinib inhibits the viability of different EGFRex20ins-driven cell lines over time.[1]
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| ln Vivo |
Mobocertinib inhibits EGFR to stop the growth of EGFRex20ins mutant tumors. The head and neck squamous cell carcinoma model (CTG-2130) with EGFRex20ins D770_N771insGL responds better to combination treatment with mobocertinib and cetuximab.
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| Cell Assay |
The cells are seeded into 96-well plates, treated with a series of compounds diluted three times, and allowed to incubate for seven days. For measuring viability, the CellTiter-Glo assay is utilized. IC50 values are determined by creating dose-response curves.
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| Animal Protocol |
Female Athymic Nude-Foxn1nu mice (human NSCLC H1975 LT tumor model)
3, 10, 30 mg/kg Oral; once daily for 20 days. |
| References |
| Molecular Formula |
C₃₂H₃₉N₇O₄
|
|---|---|
| Molecular Weight |
585.6966
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| Exact Mass |
585.31
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| Elemental Analysis |
C, 65.62; H, 6.71; N, 16.74; O, 10.93
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| CAS # |
1847461-43-1
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| Related CAS # |
Mobocertinib succinate;2389149-74-8;Mobocertinib mesylate;2389149-85-1
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| Appearance |
Solid powder
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| SMILES |
CC(C)OC(=O)C1=CN=C(N=C1C2=CN(C3=CC=CC=C32)C)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC
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| InChi Key |
AZSRSNUQCUDCGG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H39N7O4/c1-9-29(40)34-24-16-25(28(42-8)17-27(24)38(6)15-14-37(4)5)35-32-33-18-22(31(41)43-20(2)3)30(36-32)23-19-39(7)26-13-11-10-12-21(23)26/h9-13,16-20H,1,14-15H2,2-8H3,(H,34,40)(H,33,35,36)
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| Chemical Name |
propan-2-yl 2-[4-[2-(dimethylamino)ethyl-methylamino]-2-methoxy-5-(prop-2-enoylamino)anilino]-4-(1-methylindol-3-yl)pyrimidine-5-carboxylate
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| Synonyms |
TAK-788; AP-32788; TAK 788; AP32788; TAK788; AP 32788
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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: ~25 mg/mL (42.7 mM）
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.27 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.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: ≥ 1.25 mg/mL (2.13 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7074 mL | 8.5368 mL | 17.0736 mL | |
| 5 mM | 0.3415 mL | 1.7074 mL | 3.4147 mL | |
| 10 mM | 0.1707 mL | 0.8537 mL | 1.7074 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 | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03807778 | Active Recruiting |
Drug: Mobocertinib | Non-Small Cell Lung Cancer | Takeda | February 4, 2019 | Phase 1 |
| NCT04129502 | Active Recruiting |
Drug: TAK-788 Drug: Pemetrexed |
Advanced/Metastatic Non-Small Cell Lung Cancer (NSCLC) |
Takeda | January 10, 2020 | Phase 3 |
| NCT02716116 | Active Recruiting |
Drug: TAK-788 | Carcinoma, Non-Small-Cell Lung | Takeda | June 16, 2016 | Phase 1 Phase 2 |
| NCT04056455 | Completed | Drug: Mobocertinib | Renal Impairment Healthy Volunteers |
Millennium Pharmaceuticals, Inc. | March 10, 2020 | Phase 1 |
| NCT04056468 | Recruiting | Drug: Mobocertinib | Hepatic Impairment Healthy Volunteers |
Millennium Pharmaceuticals, Inc. | October 9, 2020 | Phase 1 |
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