An inhibitor of SIK2
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ARN3261

Item No. 45729

Technical Information
Formal Name
3-(3,5-difluoro-2-methoxyphenyl)-5-[1[1-(methylsulfonyl)-4-piperidinyl]-1H-pyrazol-4-yl]-1H-pyrrolo[2,3-b]pyridine
CAS Number
1613711-28-6
Synonyms
  • GRN-300
Molecular Formula
C23H23F2N5O3S
Formula Weight
Purity
≥98%
A solid
DMSO: Slightly Soluble: 0.1-1 mg/ml
SMILES
O=S(N1CCC(CC1)N2N=CC(C3=CN=C4NC=C(C5=CC(F)=CC(F)=C5OC)C4=C3)=C2)(C)=O
InChi Code
InChI=1S/C23H23F2N5O3S/c1-33-22-18(8-16(24)9-21(22)25)20-12-27-23-19(20)7-14(10-26-23)15-11-28-30(13-15)17-3-5-29(6-4-17)34(2,31)32/h7-13,17H,3-6H2,1-2H3,(H,26,27)
InChi Key
NIFLRVAYOHHDFN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    ARN3261 is an inhibitor of salt-inducible kinase 2 (SIK2).1 It induces apoptosis in OVCAR-8, SKOV3, and OC 316 ovarian cancer cells and inhibits growth in ten ovarian cancer cell lines (IC50s = 0.8-2.6 µM). ARN3261 enhances sensitivity to carboplatin (Item No. 13112) in both carboplatin-sensitive and -resistant ovarian cancer cells and increases carboplatin-induced DNA damage and apoptosis in OVCAR-8, SKOV3, and OC 316 cells. It reduces tumor weight in a SKOV3 mouse xenograft model when administered at a dose of 40 mg/kg with carboplatin.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fan, D., Yang, H., Mao, W., et alA novel salt inducible kinase 2 inhibitor, ARN-3261, sensitizes ovarian cancer cell lines and xenografts to carboplatin. Cancers 13, 446 (2021).