An ALK5 inhibitor
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BMS 986260

Item No. 42042

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-1H-imidazol-5-yl]-imidazo[1,2-b]pyridazine-3-carbonitrile
CAS Number
2001559-19-7
Molecular Formula
C18H12ClFN6O
Formula Weight
382.8
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
N#CC1=CN=C2N1N=C(C3=C(C4=CC(Cl)=C(F)C=C4)N=CN3CCO)C=C2
InChi Code
InChI=1S/C18H12ClFN6O/c19-13-7-11(1-2-14(13)20)17-18(25(5-6-27)10-23-17)15-3-4-16-22-9-12(8-21)26(16)24-15/h1-4,7,9-10,27H,5-6H2
InChi Key
VZZBCNXVZFAIQX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $102

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    10 mg

    $193

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    50 mg

    $557

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    100 mg

    $1,012

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    Product Description

    BMS 986260 is an inhibitor of activin receptor-like kinase 5 (ALK5), also known as TGF-β receptor type I (TGF-βRI; IC50 = 0.0015 µM).1 It is selective for ALK5 over TGF-βRII (IC50 = >15 µM) and a panel of 213 additional kinases at 1 µM. BMS 986260 inhibits TGF-β-induced increases in the nuclear translocation of phosphorylated SMAD2/3 in Mv 1 Lu mink lung epithelial cells (IC50 = 0.35 µM). It decreases tumor growth in an MC-38 murine colon carcinoma model of tumor rechallenge when administered at a dose of 3.75 mg/kg per day in combination with an antibody against programmed cell death protein 1 (PD-1). BMS 986260 (10 mg/kg per day) induces hyperproliferation of chondrocytes in the femoral epiphysis, thickening of the cardiac atrioventricular valve, and inflammation in the aortic vasculature in rats.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Velaparthi, U., Darne, C.P., Warrier, J., et al. Discovery of BMS-986260, a potent, selective, and orally bioavailable TGFβR1 inhibitor as an immuno-oncology agent. ACS Med. Chem. Lett. 11(2), 172-178 (2020).

    2. Rak, G.D., White, M.R., Augustine-Rauch, K., et al. Intermittent dosing of the transforming growth factor beta receptor 1 inhibitor, BMS-986260, mitigates class-based cardiovascular toxicity in dogs but not rats. J. Appl. Toxicol. 40(7), 931-946 (2020).