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Chemical Structure| 1005504-62-0 Chemical Structure| 1005504-62-0

Structure of RG3039
CAS No.: 1005504-62-0

Chemical Structure| 1005504-62-0

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RG3039 (PF-06687859) is an orally active, brain-penetrant DcpS inhibitor with an IC50 of 0.069 nM.

Synonyms: PF-06687859; Quinazoline 495; PF 6687859

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Product Details of RG3039

CAS No. :1005504-62-0
Formula : C21H23Cl2N5O
M.W : 432.35
SMILES Code : NC1=NC(N)=C2C(OCC3CCN(CC4=C(Cl)C=CC=C4Cl)CC3)=CC=CC2=N1
Synonyms :
PF-06687859; Quinazoline 495; PF 6687859
MDL No. :MFCD28716151
InChI Key :MNLHFGXIUJNDAF-UHFFFAOYSA-N
Pubchem ID :53258905

Safety of RG3039

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HA1800 8 µM 48 hours To evaluate the toxicity of RG3039 on normal astrocytes, results showed that RG3039 had low toxicity on normal cells. J Transl Med. 2024 Sep 30;22(1):880
U118 6 µM 48 hours To evaluate the effect of RG3039 on GBM cell proliferation and apoptosis, results showed that RG3039 significantly inhibited cell proliferation and induced apoptosis. J Transl Med. 2024 Sep 30;22(1):880
A172 6 µM 48 hours To evaluate the effect of RG3039 on GBM cell proliferation and apoptosis, results showed that RG3039 significantly inhibited cell proliferation and induced apoptosis. J Transl Med. 2024 Sep 30;22(1):880
U251 6 µM 48 hours To evaluate the effect of RG3039 on GBM cell proliferation and apoptosis, results showed that RG3039 significantly inhibited cell proliferation and induced apoptosis. J Transl Med. 2024 Sep 30;22(1):880
U87 6 µM 48 hours To evaluate the effect of RG3039 on GBM cell proliferation and apoptosis, results showed that RG3039 significantly inhibited cell proliferation and induced apoptosis. J Transl Med. 2024 Sep 30;22(1):880
HEK293T cells 100 nM 48 hours Validate RG3039 effects on specific RNAs (e.g., HS370762 and BC011766), confirming DcpS-dependency RNA. 2015 Jul;21(7):1306-12
SH-SY5Y neuroblastoma cells 100 nM 48 hours Examine global mRNA levels upon DcpS decapping inhibition, revealing changes in 222 RNAs RNA. 2015 Jul;21(7):1306-12
CALM/AF10 cells 1 µM 6 hours and 10 hours To assess the effect of RG3039 on pre-mRNA splicing in AML cells. RG3039 treatment increased pre-mRNA mis-splicing in AML cells, particularly at the first exon or the first intron. Cancer Cell. 2018 Mar 12;33(3):386-400. e5
MOLM-13 cells 1 µM 6 hours and 10 hours To evaluate the anti-proliferative and differentiation-inducing effects of RG3039 on AML cells. RG3039 treatment resulted in slowed proliferation, cell cycle arrest, increased apoptosis, and differentiation toward the myelo/monocytic lineage. Cancer Cell. 2018 Mar 12;33(3):386-400. e5

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Taiwanese SMA mouse model and 2B/2SMA mouse model Oral 10 mg/kg, 20 mg/kg, 2.5 mg/kg Once daily for 8 days RG3039 can extend survival and improve function in two SMA mouse models of varying disease severity (Taiwanese 5058 Hemi and 2B/2SMA mice), and positively impacts neuromuscular pathologies. In 2B/2SMA mice, RG3039 provided a >600% survival benefit (median 18 days to >112 days) when dosing began at P4, highlighting the importance of early intervention. Hum Mol Genet. 2013 Oct 15;22(20):4084-101
Mice Severe SMA mouse model Intraperitoneal injection 10 mg/kg/day Daily from postnatal day 1 (P1) until death To evaluate the effects of RG3039 on disease outcomes in SMA mice, results showed that treatment significantly improved survival, weight, and motor function, enhanced motor neuron and neuromuscular junction synaptic connectivity and function, and increased muscle size. Hum Mol Genet. 2013 Oct 15;22(20):4074-83
BALB/c nude mice Orthotopic GBM mouse model Intraperitoneal injection 20 mg/kg Once daily until the endpoint of observation To evaluate the inhibitory effect of RG3039 on GBM tumor growth in vivo, results showed that RG3039 significantly inhibited tumor growth and prolonged mouse survival. J Transl Med. 2024 Sep 30;22(1):880
Mice CALM/AF10 or MLL/AF9 leukemia model Intraperitoneal injection 20 mg/kg Once daily for 14 days To evaluate the anti-leukemia effects of RG3039 in vivo. RG3039 treatment significantly reduced the burden of AML cells in the blood and bone marrow and prolonged the survival of mice. Cancer Cell. 2018 Mar 12;33(3):386-400. e5

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.56mL

2.31mL

1.16mL

23.13mL

4.63mL

2.31mL

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