An inhibitor of VPS34
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SB-02024

Item No. 41231

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[(3R)-3-methyl-4-morpholinyl]-6-[(2R)-2-(trifluoromethyl)-1-piperidinyl]-2(1H)-pyridinone
CAS Number
2126737-28-6
Molecular Formula
C16H22F3N3O2
Formula Weight
345.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Sparingly soluble: 1-10 mg/ml
SMILES
C[C@H](COCC1)N1C2=CC(NC(N(CCCC3)[C@H]3C(F)(F)F)=C2)=O
InChi Code
InChI=1S/C16H22F3N3O2/c1-11-10-24-7-6-21(11)12-8-14(20-15(23)9-12)22-5-3-2-4-13(22)16(17,18)19/h8-9,11,13H,2-7,10H2,1H3,(H,20,23)/t11-,13-/m1/s1
InChi Key
IARAUFAUVKBTEM-DGCLKSJQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $124

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    5 mg

    $493

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    Product Description

    SB-02024 is an inhibitor of vacuolar protein sorting 34 (VPS34; IC50 = 5 nM).1 It selectively binds to VPS34 (Kd = 0.0011 µM) over eight other PI3K kinases (Kds = 1.2693->30 µM), mTOR (Kd = 1.0199 µM), a panel of 468 kinases at 1 µM, and an additional panel of 97 kinases at 1 µM.2 SB-02024 (0.7 µM) inhibits autophagic flux in H1299 cells. In vivo, SB-02024 (20 mg/kg) enhances increases in survival when used in combination with an antibody targeting programmed cell death protein 1 (PD-1) or PD-1 ligand (PD-L1) in B16/F10 murine melanoma and CT26 murine colorectal cancer models.3 SB-02024 (20 mg/kg) also enhances increases in survival and decreases in tumor volume when used in combination with the STING agonist ADU-S100 (Item No. 27901) in a B16/F10 murine melanoma model.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yu, Y., Bogdan, M., Noman, M.Z., et al. Combining VPS34 inhibitors with STING agonists enhances type I interferon signaling and anti-tumor efficacy. Mol. Oncol. 18(8), 1904-1922 (2024).

    2. Dyczynski, M., Yu, Y., Otrocka, M., et al. Targeting autophagy by small molecule inhibitors of vacuolar protein sorting 34 (Vps34) improves the sensitivity of breast cancer cells to Sunitinib. Cancer Lett. 435, 32-43 (2018).

    3. Noman, M.Z., Parpal, S., Van More, K., et al. Inhibition of Vps34 reprograms cold into hot inflamed tumors and improves anti-PD-1/PD-L1 immunotherapy. Sci. Adv. 6(18), eaax7881 (2020).