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Chemical Structure| 459868-92-9 Chemical Structure| 459868-92-9
Chemical Structure| 459868-92-9

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CAS No.: 459868-92-9

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Rucaparib phosphate is an inhibitor of PARP with Ki of 1.4 nM for PARP1, also showing binding affinity to eight other PARP domains.

Synonyms: PF-01367338 phosphate; AG-014699 phosphate; PF-01367338

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Product Details of Rucaparib phosphate

CAS No. :459868-92-9
Formula : C19H21FN3O5P
M.W : 421.36
SMILES Code : O=C1NCCC2=C(C3=CC=C(CNC)C=C3)NC4=C2C1=CC(F)=C4.O=P(O)(O)O
Synonyms :
PF-01367338 phosphate; AG-014699 phosphate; PF-01367338
MDL No. :MFCD17010269
InChI Key :FCCGJTKEKXUBFZ-UHFFFAOYSA-N
Pubchem ID :9931953

Safety of Rucaparib phosphate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H332-H335
Precautionary Statements:P280-P305+P351+P338-P310

Related Pathways of Rucaparib phosphate

epigenetics
DNA

Isoform Comparison

Biological Activity

Target

  • PARP

    PARP, Ki:1.4 nM

In Vitro:

Cell Line
Concentration Treated Time Description Reference
GBM12 cells 1 μM and 3 μM 14 days To evaluate the efficacy of Rucaparib in combination with TMZ, results showed that Rucaparib significantly enhanced the efficacy of TMZ. PMC4674360
MDCKII cells 2 μM 60 min To evaluate the accumulation of Rucaparib in MDCKII cells, results showed that Rucaparib is a substrate for both MDR1 and BCRP1 efflux pumps. PMC4674360
MEFs 100 nM 2 weeks To evaluate the sensitivity of MEFs to Rucaparib, results showed that Brca1CC/Δ11 cells formed more colonies in the presence of 100 nM Rucaparib, but significantly fewer colonies at 1000 nM Rucaparib. PMC7418109
RPE1-hTERT TP53?/? BRCA1 KO 10 μM 2 h To observe the sensitivity of BRCA1-deficient cells to PARPi, results showed that BRCA1 KO cells had significantly longer replication tracks after PARPi treatment PMC9089372
RPE1-hTERT TP53?/? FANCJ KO 10 μM 2 h To observe the sensitivity of FANCJ-deficient cells to PARPi, results showed that FANCJ KO cells did not display DNA tract lengthening after PARPi treatment PMC9089372
T47D 1 μM 24 h To evaluate the degradation effect of 180055 on PARP1, the results showed that 180055 significantly reduced PARP1 expression. PMC11655542
MDA-MB-231 1 μM 24 h To evaluate the degradation effect of 180055 on PARP1, the results showed that 180055 significantly reduced PARP1 expression. PMC11655542
CD4+ T cells 10 μM 12 h Inhibition of PARP enzyme activity, reducing IL-17 release and ROS levels PMC10518596
GEA PDX-derived primary cells 1.25 –40μM 6 days To evaluate the growth inhibitory effect of Rucaparib on GEA PDX-derived primary cells, results showed that cells with BRCA2 mutations were sensitive to Rucaparib PMC10183806
MDA-MB-231 cells 15 μM 4, 8, 24 h To study the effect of Rucaparib on the transcriptomic dynamics of MDA-MB-231 cells, revealing transcriptomic changes at different time points. PMC8022202
IB114 1.488 μM 72 h To study the antiproliferative activity of Rucaparib on IB114 cells, IC50 value was 1.488 μM PMC5387279
IB115 1.104 μM 72 h To study the antiproliferative activity of Rucaparib on IB115 cells, IC50 value was 1.104 μM PMC5387279
IB111 1.364 μM 72 h To study the antiproliferative activity of Rucaparib on IB111 cells, IC50 value was 1.364 μM PMC5387279
IB133 58.08 μM 72 h To study the antiproliferative activity of Rucaparib on IB133 cells, IC50 value was 58.08 μM PMC5387279
IB134 40.88 μM 72 h To study the antiproliferative activity of Rucaparib on IB134 cells, IC50 value was 40.88 μM PMC5387279
IB136 31.35 μM 72 h To study the antiproliferative activity of Rucaparib on IB136 cells, IC50 value was 31.35 μM PMC5387279
IB112 29.5 μM 72 h To study the antiproliferative activity of Rucaparib on IB112 cells, IC50 value was 29.5 μM PMC5387279
IB128 12.036 μM 72 h To study the antiproliferative activity of Rucaparib on IB128 cells, IC50 value was 12.036 μM PMC5387279
93T449 19.2 μM 72 h To study the antiproliferative activity of Rucaparib on 93T449 cells, IC50 value was 19.2 μM PMC5387279
GBM U251 cells 0.2, 0.5, 1, 2, 5, 10, 25, 50, 100 μM 96 h To evaluate the antiproliferative effect of Rucaparib on GBM U251 cells, results showed that Rucaparib inhibited cell proliferation in a dose-dependent manner with an IC50 value of 14.36 μM. PMC8150626
GBM U87MG cells 0.2, 0.5, 1, 2, 5, 10, 25, 50, 100 μM 96 h To evaluate the antiproliferative effect of Rucaparib on GBM U87MG cells, results showed that Rucaparib inhibited cell proliferation in a dose-dependent manner with an IC50 value of 15.00 μM. PMC8150626

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
Mice GBM12 flank xenograft model Intraperitoneal injection 1 mg/kg Every 28 days × 3 cycles, daily for 5 days To evaluate the efficacy of Rucaparib in combination with TMZ in the GBM12 flank xenograft model, results showed that Rucaparib significantly prolonged the time to tumor regrowth. PMC4674360
Mice Brca1CC/Δ11 mice Oral 200 mg/kg Twice daily for 5 days To evaluate the tolerability of Rucaparib in Brca1CC/Δ11 mice, results showed that Rucaparib treatment led to a reduction in blood lymphocytes, but was unaffected and mice survived. PMC7418109
Mouse BRCA1-deficient mouse ovarian tumor cell line BR5 Oral 150 mg/kg Twice daily for 5 days, 2 days off, then 5 days To evaluate the sensitivity of BRCA1-deficient tumors to PARPi, results showed that BRCA1-deficient tumors were sensitive to PARPi and exhibited replication tract lengthening after treatment PMC9089372
NSG mice MOLT4 tumor xenograft model Intraperitoneal injection 40 mg/kg Twice daily for 16 days To evaluate the anti-tumor efficacy of 180055 in BRCA1-mutated tumor models, the results showed that 180055 significantly inhibited tumor growth with fewer side effects. PMC11655542
Mice IB115 cell xenograft model Intraperitoneal injection 10 mg/kg Five times per week for 3 weeks To evaluate the antitumor effect of Rucaparib on the IB115 cell xenograft model, the results showed that Rucaparib significantly prolonged progression-free survival PMC5387279

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00457470 Diabetes Mellitus|Diabetic Ret... More >>inopathy Less << PHASE2 WITHDRAWN - -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.37mL

0.47mL

0.24mL

11.87mL

2.37mL

1.19mL

23.73mL

4.75mL

2.37mL
Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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