[CAS NO. 1476074-39-1] VX-984

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PRODUCTS SPECIFICATIONS [1476074-39-1]

Catalog

HY-19939S

Brand

MCE

CAS

1476074-39-1

DESCRIPTION [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

For research use only. We do not sell to patients.

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

In Vitro:

DMSO : 10 mg/mL ( 24.07 mM ; Need ultrasonic)

Preparing
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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 1 mg/mL (2.41 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 1 mg/mL (2.41 mM); Clear solution

* All of the co-solvents are available by MCE.