An mTOR inhibitor
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CZ415

Item No. 27668

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[5,7-dihydro-7,7-dimethyl-4-[(3S)-3-methyl-4-morpholinyl]-6,6-dioxidothieno[3,4-d]pyrimidin-2-yl]phenyl]-N'-ethyl-urea
CAS Number
1429639-50-8
Molecular Formula
C22H29N5O4S
Formula Weight
459.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:6): 0.1 mg/mlEthanol: 10 mg/ml
λmax
303 nm
SMILES
C[C@H]1COCCN1C2=C3C(C(C)(C)S(C3)(=O)=O)=NC(C4=CC=C(NC(NCC)=O)C=C4)=N2
InChi Code
InChI=1S/C22H29N5O4S/c1-5-23-21(28)24-16-8-6-15(7-9-16)19-25-18-17(13-32(29,30)22(18,3)4)20(26-19)27-10-11-31-12-14(27)2/h6-9,14H,5,10-13H2,1-4H3,(H2,23,24,28)/t14-/m0/s1
InChi Key
IZLPVLBNRGPOHA-AWEZNQCLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $190

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    10 mg

    $354

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    25 mg

    $645

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    Product Description

    CZ415 is an inhibitor of mammalian target of rapamycin (mTOR; Kd = 6.3 nM).1 It is 1,000-fold selective for mTOR over a panel of 285 kinases. CZ415 inhibits phosphorylation of S6 ribosomal protein (S6RP) and Akt in HEK293T cells (IC50s = 14.5 and 14.8 nM, respectively). It inhibits IFN-γ secretion in IL-2, anti-CD3, and anti-CD28 antibody-stimulated human whole blood (IC50 = 226 nM). CZ415 (10 mg/kg) reduces fore paw joint erythema and swelling in a mouse model of collagen-induced arthritis. It also inhibits intratumor mTOR activity and reduces tumor growth in an OCC-1 oral cavity carcinoma mouse xenograft model when administered at a dose of 20 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cansfield, A.D., Ladduwahetty, T., Sunose, M., et al. CZ415, a highly selective mTOR inhibitor showing in vivo efficacy in a collagen induced arthritis model. ACS Med. Chem. Lett. 7(8), 768-773 (2016).

    2. Xie, J., Li, Q., Ding, X., et al. Targeting mTOR by CZ415 inhibits head and neck squamous cell carcinoma cells. Cell Physiol. Biochem. 46(2), 676-686 (2018).