An Akt1 and Akt2 inhibitor
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Borussertib

Item No. 33387

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[1-[[4-(5,6-dihydro-5-oxo-3-phenyl-1,6-naphthyridin-2-yl)phenyl]methyl]-4-piperidinyl]-2,3-dihydro-2-oxo-1H-benzimidazol-5-yl]-2-propenamide
CAS Number
1800070-77-2
Molecular Formula
C36H32N6O3
Formula Weight
596.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly Soluble: 0.1-1 mg/ml
SMILES
O=C1NC=CC2=NC(C(C=C3)=CC=C3CN(CC4)CCC4N5C(NC6=CC=C(NC(C=C)=O)C=C65)=O)=C(C7=CC=CC=C7)C=C12
InChi Code
InChI=1S/C36H32N6O3/c1-2-33(43)38-26-12-13-31-32(20-26)42(36(45)40-31)27-15-18-41(19-16-27)22-23-8-10-25(11-9-23)34-28(24-6-4-3-5-7-24)21-29-30(39-34)14-17-37-35(29)44/h2-14,17,20-21,27H,1,15-16,18-19,22H2,(H,37,44)(H,38,43)(H,40,45)
InChi Key
HXBRBOYWXDLHDC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $81

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    5 mg

    $341

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    10 mg

    $603

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    25 mg

    $1,005

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    Product Description

    Borussertib is a covalent and allosteric Akt1 and Akt2 inhibitor (Kis = 2 and 6 nM, respectively).1 It is selective for Akt1 and Akt2 over Akt3 (Ki = 91 nM). Borussertib (5 µM) reduces viability in Ba/F3 cells expressing human Akt1 or Akt2 but not Ba/F3 cells expressing human Akt3. It decreases the levels of phosphorylated Akt1, Akt2, proline-rich Akt substrate 40 kDa (PRAS40), and ribosomal protein S6 in PANC-1 pancreatic cancer cells when used at concentrations ranging from 0.3 to 5 µM. In vivo, borussertib (20 mg/kg per day), in combination with the MEK1 and MEK2 inhibitor trametinib (Item No. 16292), prevents tumor growth in three patient-derived xenografts (PDX) mouse models of K-Ras-mutant colorectal cancer.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Quambusch, L., Depta, L., Landel, I., et al. Cellular model system to dissect the isoform-selectivity of Akt inhibitors. Nat. Commun. 12(1), 5297 (2021).

    2. Weisner, J., Landel, I., Reintjes, C., et al. Preclinical efficacy of covalent-allosteric AKT inhibitor borussertib in combination with trametinib in KRAS-mutant pancreatic and colorectal cancer. Cancer Res. 79(9), 2367-2378 (2019).