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Chemical Structure| 1242156-23-5 Chemical Structure| 1242156-23-5

Structure of RN486
CAS No.: 1242156-23-5

Chemical Structure| 1242156-23-5

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RN486 is an effective, selective, orally active inhibitor of Bruton's tyrosine kinase (Btk) with an IC50 of 4.0 nM and a Kd of 0.31 nM, with lower activity against other kinases. RN486 can be used in research on rheumatoid arthritis and systemic lupus erythematosus.

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Product Details of RN486

CAS No. :1242156-23-5
Formula : C35H35FN6O3
M.W : 606.69
SMILES Code : O=C1N(C2=CC=CC(C(C=C3NC4=NC=C(N5CCN(C)CC5)C=C4)=CN(C)C3=O)=C2CO)C=CC6=C1C(F)=CC(C7CC7)=C6
MDL No. :MFCD24682729
InChI Key :ZTUJNJAKTLHBEX-UHFFFAOYSA-N
Pubchem ID :46908026

Safety of RN486

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

Related Pathways of RN486

RTK

Isoform Comparison

Biological Activity

Target
  • BTK

    BTK, IC50:4 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HEK293/B1G2 0.3, 1, 3 μM 68 hours To evaluate the reversal effect of RN486 on ABCG2-overexpressing cancer cells, results showed that RN486 significantly increased the sensitivity of ABCG2-overexpressing cells to mitoxantrone and topotecan. J Transl Int Med. 2024 Jul 27;12(3):288-298.
HEK293/G2 0.3, 1, 3 μM 68 hours To evaluate the reversal effect of RN486 on ABCG2-overexpressing cancer cells, results showed that RN486 significantly increased the sensitivity of ABCG2-overexpressing cells to mitoxantrone and topotecan. J Transl Int Med. 2024 Jul 27;12(3):288-298.
HEK293/B1 0.3, 1, 3 μM 68 hours To evaluate the reversal effect of RN486 on ABCG2-overexpressing cancer cells, results showed that RN486 significantly increased the sensitivity of ABCG2-overexpressing cells to mitoxantrone and topotecan. J Transl Int Med. 2024 Jul 27;12(3):288-298.
HEK293/PEL 0.3, 1, 3 μM 68 hours To evaluate the reversal effect of RN486 on ABCG2-overexpressing cancer cells, results showed that RN486 significantly increased the sensitivity of ABCG2-overexpressing cells to mitoxantrone and topotecan. J Transl Int Med. 2024 Jul 27;12(3):288-298.
S1-M1-80 0.3, 1, 3 μM 68 hours To evaluate the reversal effect of RN486 on ABCG2-overexpressing cancer cells, results showed that RN486 significantly increased the sensitivity of ABCG2-overexpressing cells to mitoxantrone and topotecan. J Transl Int Med. 2024 Jul 27;12(3):288-298.
S1 0.3, 1, 3 μM 68 hours To evaluate the reversal effect of RN486 on ABCG2-overexpressing cancer cells, results showed that RN486 significantly increased the sensitivity of ABCG2-overexpressing cells to mitoxantrone and topotecan. J Transl Int Med. 2024 Jul 27;12(3):288-298.
NCI-H460/MX20 0.3, 1, 3 μM 68 hours To evaluate the reversal effect of RN486 on ABCG2-overexpressing cancer cells, results showed that RN486 significantly increased the sensitivity of ABCG2-overexpressing cells to mitoxantrone and topotecan. J Transl Int Med. 2024 Jul 27;12(3):288-298.
NCI-H460 0.3, 1, 3 μM 68 hours To evaluate the reversal effect of RN486 on ABCG2-overexpressing cancer cells, results showed that RN486 significantly increased the sensitivity of ABCG2-overexpressing cells to mitoxantrone and topotecan. J Transl Int Med. 2024 Jul 27;12(3):288-298.
NCI-H2228 10 μM 72 hours Evaluate the effect of RN486 on cell viability, results showed RN486 significantly decreased cell viability J Exp Clin Cancer Res. 2019 Jun 14;38(1):260.
NCI-H1975 10 μM 72 hours Evaluate the effect of RN486 on cell viability, results showed RN486 significantly decreased cell viability J Exp Clin Cancer Res. 2019 Jun 14;38(1):260.
Calu-6 10 μM 72 hours Evaluate the effect of RN486 on cell viability, results showed RN486 significantly decreased cell viability J Exp Clin Cancer Res. 2019 Jun 14;38(1):260.
SK-Lu-1 10 μM 72 hours Evaluate the effect of RN486 on cell viability, results showed RN486 significantly decreased cell viability J Exp Clin Cancer Res. 2019 Jun 14;38(1):260.
Murine neonatal cardiomyocytes (CMs) 25 μM 24 hours To evaluate the protective effect of NG-R1 on hypoxia/reoxygenation-induced apoptosis. Results showed that NG-R1 significantly inhibited apoptosis, reduced LDH release, and improved cell viability. Front Cell Dev Biol. 2020 Aug 27;8:865.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57/BL6 mice Myocardial ischemia/reperfusion injury model Intraperitoneal injection 25 mg/kg Every 2 hours for a total of 3 times, starting 30 minutes before ischemic surgery To evaluate the protective effect of NG-R1 on myocardial ischemia/reperfusion injury. Results showed that NG-R1 significantly reduced myocardial infarction area, alleviated myocardial cell damage, and improved cardiac function. Front Cell Dev Biol. 2020 Aug 27;8:865.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.65mL

0.33mL

0.16mL

8.24mL

1.65mL

0.82mL

16.48mL

3.30mL

1.65mL

References

 

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