2. Disease Areas
  3. Cancer Neurological, Eye or Ear Disease
  4. CNS Neoplasm Glioma
  5. Glioblastoma
  6. PRMT5-IN-56

PRMT5-IN-56 is a PRMT5⋅MTA complex inhibitor with an IC50 of 0.2 nM, oral activity, and blood-brain barrier penetration. PRMT5-IN-56 inhibits PRMT5 methyltransferase activity in an MTA-cooperative manner, suppresses symmetrical dimethylarginine levels in MTAP-deficient cells. PRMT5-IN-56 suppresses proliferation of MTAP-deleted cancer cells with high selectivity over MTAP-wild type cells. PRMT5-IN-56 induces dose-dependent tumor growth inhibition in subcutaneous xenograft models, inhibits intracranial tumor progression, and prolongs survival in orthotopic brain xenograft models. PRMT5-IN-56 exhibits high intrinsic permeability, good oral bioavailability, and a high brain-to-plasma ratio. PRMT5-IN-56 can be used for the research of MTAP-deleted cancers and glioblastoma.

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

PRMT5-IN-56

PRMT5-IN-56 Chemical Structure

CAS No. : 3062852-59-6

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PRMT5-IN-56 Related Antibodies

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Description

PRMT5-IN-56 is a PRMT5⋅MTA complex inhibitor with an IC50 of 0.2 nM, oral activity, and blood-brain barrier penetration. PRMT5-IN-56 inhibits PRMT5 methyltransferase activity in an MTA-cooperative manner, suppresses symmetrical dimethylarginine levels in MTAP-deficient cells. PRMT5-IN-56 suppresses proliferation of MTAP-deleted cancer cells with high selectivity over MTAP-wild type cells. PRMT5-IN-56 induces dose-dependent tumor growth inhibition in subcutaneous xenograft models, inhibits intracranial tumor progression, and prolongs survival in orthotopic brain xenograft models. PRMT5-IN-56 exhibits high intrinsic permeability, good oral bioavailability, and a high brain-to-plasma ratio. PRMT5-IN-56 can be used for the research of MTAP-deleted cancers and glioblastoma[1].

IC50 & Target[1]

PRMT5

 

In Vitro

PRMT5-IN-56 (compound 21) (6 days) potently and selectively inhibits the proliferation of MTAP-deleted HCT116 cells with an IC50 of 1.1 nM, showing 214-fold selectivity over MTAP-wild type HCT116 cells[1].
PRMT5-IN-56 (6 days) preferentially suppresses the proliferation of MTAP-deleted cancer cells over MTAP-wild type cells across a diverse panel of cancer lines, and demonstrates superior potency over TNG462 (HY-156680) in multiple MTAP-deleted models[1].
PRMT5-IN-56 potently and selectively reduces symmetrical dimethylarginine (SDMA) levels in a concentration- and time-dependent manner in MTAP-deleted HCT116, LN18, and U87MG cells, with more rapid and profound effects than TNG462 (HY-156680) in glioma cell lines[1].
PRMT5-IN-56 (10 μM; 95 min) exhibits high intrinsic membrane permeability with a Papp of 16.94 × 10-6 cm/s and a low efflux ratio of 1.12 in a Caco-2 cell assay[1].
PRMT5-IN-56 (1 μM) exhibits good metabolic stability in human hepatocytes (T1/2 = 118.7 min) and moderate stability in mouse hepatocytes (T1/2 = 62.2 min)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PRMT5-IN-56 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 Vss CL AUClast Tmax Cmax F Plasma Concentration Brain Concentration
Mice[1] 3 mg/kg i.v. 0.42 h 3229 mL/kg 107 mL/min/kg 476 ng·h/mL / / / / /
Mice[1] 30 mg/kg p.o. 0.90 h / / 5119 ng·h/mL 1.33 h 1324 ng/mL 108 % / /
Rat[1] 2 mg/kg i.v. 0.72 h 4143 mL/kg 66.0 mL/min/kg 531 mL/kg / / / / /
Rat[1] 10 mg/kg p.o. 1.95 h / / 1997 ng·h/mL 1.00 h 785 ng/mL 75.3 % / /
Mice[1] 30 mg/kg p.o. / / / / / / / 2010 ng/mL 1636 ng/g
In Vivo

PRMT5-IN-56 (compound 21) (30-50 mg/kg; p.o.; daily; 14 days) induces dose-dependent tumor growth inhibition in MTAP-deleted HCT116 subcutaneous xenografts[1].
PRMT5-IN-56 (10-50 mg/kg; p.o.; daily; 7 days) induces dose-dependent tumor growth inhibition in MTAP-deleted U87MG subcutaneous xenografts[1].
PRMT5-IN-56 (30-60 mg/kg; p.o.; daily; 36 days) induces dose-dependent tumor growth inhibition in MTAP-deleted U87MG orthotopic brain xenografts[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice (female, 6 weeks old, subcutaneous xenograft model using MTAP-deleted HCT116 cells)[1]
Dosage: 30 mg/kg; 50 mg/kg
Administration: p.o.; daily; 14 days
Result: Achieved a tumor growth inhibition (TGI) rate of 74.1% at 30 mg/kg.
Achieved a TGI rate of 84.6% at 50 mg/kg, with complete tumor regression observed in 2 mice.
Caused no significant body weight loss.
Animal Model: BALB/c nude mice (female, 6 weeks old, subcutaneous xenograft model using MTAP-deleted U87MG cells)[1]
Dosage: 10 mg/kg; 50 mg/kg
Administration: p.o.; daily; 7 days
Result: Achieved a TGI rate of 108.1% at 10 mg/kg.
Achieved a TGI rate of 138.6% at 50 mg/kg, with sustained tumor regression observed and tumor growth inhibition remaining stable after treatment discontinuation.
Caused no obvious body weight loss.
Animal Model: BALB/c nude mice (female, 6 weeks old, orthotopic brain xenograft model using luciferase-expressing MTAP-deleted U87MG-luc cells)[1]
Dosage: 30 mg/kg; 60 mg/kg
Administration: p.o.; daily; 36 days
Result: Achieved a TGI rate of 87.75% and prolonged median survival to 45 days at 30 mg/kg.
Achieved a TGI rate of 98.96% (nearly abolishing detectable tumor signals) and prolonged median survival to >62 days at 60 mg/kg.
Caused no overt toxicity.
Molecular Weight

483.49

Formula

C25H24F3N5O2
CAS No.
SMILES

CC1=CC(NC(C(N([C@@H]2CCCC3=CC=CC=C32)CC4=NC=C(C=C4)C(F)(F)F)=O)=O)=CN=C1N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PRMT5-IN-56 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PRMT5-IN-563062852-59-6HCT116 cellssubcutaneous xenograft modelsPRMT5?MTA complexMTAP-wild type cellsPRMT5 methyltransferaseglioblastomaorthotopic brain xenograft modelsMTAP-deficient cellsMTAP-deleted cancer cellsCaco-2 cellInhibitorinhibitorinhibit

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