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[CAS NO. 1476074-39-1] VX-984
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-19939S |
| Brand: | MCE |
| CAS: | 1476074-39-1 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 415.49 |
| Molecular Formula | C23H21D2N7O |
| SMILES | O=C(C1=CC=NC2=C([C@H](C)CNC3=CC(C4=C([2H])N=C(C)N=C4[2H])=NC=N3)C=CC=C12)NC |
2 Publications Citing Use of MCE
Summary
VX-984 (M9831) is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research [1] [2] [3] .
In Vitro
VX-984 (0-500 nM, 30 min) inhibits radiation-induced DNA-PKcs phosphorylation in U251 and NSC11 cells
[1]
.
VX-984 (0-500 nM) enhances the radiosensitivity of U251 and NSC11 cells in a concentration-dependent manner
[1]
.
VX-984 inhibits the repair of radiation-induced DNA double-strand breaks (DSBs)
[1]
.
VX-984 (0-1 μM) increases alternate pathways of DSB repair, including HR (homologous recombination) and mutagenic NHEJ (mNHEJ)
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| Cell Line: | U251 and NSC11 cells |
| Concentration: | 0, 100, 250, and 500 nM |
| Incubation Time: | 30 min |
| Result: | Showed a concentration-dependent decrease in radiation-induced DNA-PKcs phosphorylation in each glioma line, when VX-984 was delivered 1 hour before irradiation. VX-984 treatment alone had no effect. |
In Vivo
VX-984 (0-100 mg/kg, Oral gavage, daily) inhibits radiation-induced DNA-PKcs phosphorylation in orthotopic brain tumor xenografts
[1]
.
VX-984 (0-50 mg/kg, Oral gavage, twice a day for 2 days) enhances the radiosensitivity of brain tumor xenografts
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Athymic female nude mice (6-8 weeks old, 7-8 mice/group, U251 intracerebral xenografts) [1] |
| Dosage: | 0, 50, and 100 mg/kg |
| Administration: | Oral gavage, daily, 1 or 4 hours before irradiation (10 Gy) |
| Result: | Reduced the levels DNA-PKcs phosphorylation after irradiation. |
| Animal Model: | Athymic female nude mice (6-8 weeks old, 7 mice/group, U251 intracerebral xenografts) [1] |
| Dosage: | 0, 50 mg/kg |
| Administration: | Oral gavage, twice a day, 30 minutes before and 4 hours following local irradiation of the tumor (3 Gy) for 3 consecutive days (3×3 Gy) |
| Result: | VX-984 treatment of U251 tumors alone had no significant effect on overall survival as compared with vehicle; radiation alone resulted in an increase in survival. VX-984 and radiation combination protocol increased tumor radiosensitivity, and significantly increased the survival of mice compared with radiation alone. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02644278 | EMD Serono Research & Development Institute, Inc.|Merck KGaA, Darmstadt, Germany|EMD Serono |
Advanced Solid Tumor
|
February 29, 2016 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 10 mg/mL ( 24.07 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4068 mL | 12.0340 mL | 24.0680 mL |
| 5 mM | 0.4814 mL | 2.4068 mL | 4.8136 mL |
| 10 mM | 0.2407 mL | 1.2034 mL | 2.4068 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 1 mg/mL (2.41 mM); Clear solution
References
- [1] Timme CR, et al. The DNA-PK Inhibitor VX-984 Enhances the Radiosensitivity of Glioblastoma Cells Grown In Vitro and as Orthotopic Xenografts. Mol Cancer Ther. 2018 Jun;17(6):1207-1216.
- [2] Khan AJ, et al. VX-984 is a selective inhibitor of non-homologous end joining, with possible preferential activity in transformed cells. Oncotarget. 2018 May 25;9(40):25833-25841.
- [3] Diane Boucher, et al. Abstract 3716: Potent radiation enhancement with VX-984, a selective DNA-PKcs inhibitor for the treatment of NSCLC. Cancer Res (2016) 76 (14_Supplement): 3716.
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