A selective PI3Kβ inhibitor
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SAR260301

Item No. 17391

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[2-[(2S)-2,3-dihydro-2-methyl-1H-indol-1-yl]-2-oxoethyl]-6-(4-morpholinyl)-4(3H)-pyrimidinone
CAS Number
1260612-13-2
Molecular Formula
C19H22N4O3
Formula Weight
354.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS (pH 7.2) (1:7): 0.12 mg/mlEthanol: 15 mg/ml
λmax
233, 254 nm
SMILES
O=C1N=C(CC(N2[C@@H](C)CC3=C2C=CC=C3)=O)NC(N4CCOCC4)=C1
InChi Code
InChI=1S/C19H22N4O3/c1-13-10-14-4-2-3-5-15(14)23(13)19(25)11-16-20-17(12-18(24)21-16)22-6-8-26-9-7-22/h2-5,12-13H,6-11H2,1H3,(H,20,21,24)/t13-/m0/s1
InChi Key
UAXHPOBBKRWJGA-ZDUSSCGKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $42

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    5 mg

    $183

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    10 mg

    $322

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    25 mg

    $702

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    Product Description

    SAR260301 is an inhibitor of phosphatidylinositol 3-kinase (PI3K) isoform β (IC50 = 52 nM).1 It is selective for p110β over other PI3K isoforms.1 SAR260301 demonstrates significant in vivo activity in a UACC-62 xenograft model in mice.1 It has synergistic antitumor activity when combined with the BRAF inhibitor vemurafenib (PLX4032; Item No. 10618) or the MEK inhibitor selumetinib (AZD 6244; Item No. 11599) in PTEN-deficient/BRAF-mutated human melanoma tumor models.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Certal, V., Carry, J.C., Halley, F., et al. Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers. J. Med. Chem. 57(3), 903-920 (2014).

    2. Bonnevaux, H., Lemaitre, O., Vincent, L., et al. Concomitant inhibition of PI3Kβ and BRAF or MEK in PTEN-deficient/BRAF-mutant melanoma treatment: Preclinical assessment of SAR260301 oral PI3Kβ-selective inhibitor. Mol. Cancer Ther. 15(7), 1460-1471 (2016).