An inhibitor of IAPs
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GDC-0152

Item No. 17810

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-methyl-L-alanyl-(2S)-2-cyclohexylglycyl-N-(4-phenyl-1,2,3-thiadiazol-5-yl)-L-prolinamide
CAS Number
873652-48-3
Molecular Formula
C25H34N6O3S
Formula Weight
498.6
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 10 mg/mlEthanol: 10 mg/ml
λmax
230, 255, 293 nm
SMILES
O=C(N[C@@H](C1CCCCC1)C(N2CCC[C@H]2C(NC3=C(C4=CC=CC=C4)N=NS3)=O)=O)[C@@H](NC)C
InChi Code
InChI=1S/C25H34N6O3S/c1-16(26-2)22(32)27-21(18-12-7-4-8-13-18)25(34)31-15-9-14-19(31)23(33)28-24-20(29-30-35-24)17-10-5-3-6-11-17/h3,5-6,10-11,16,18-19,21,26H,4,7-9,12-15H2,1-2H3,(H,27,32)(H,28,33)/t16-,19-,21-/m0/s1
InChi Key
WZRFLSDVFPIXOV-LRQRDZAKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

    $329

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    Cayman Chemical
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    Product Description

    GDC-0152 is a potent inhibitor of specific IAPs that binds baculoviral IAP repeat (BIR) domains (Kis = 28, 14, 17, and 43 nM for XIAP BIR3, NL-IAP BIR, BIRC2 (c-IAP1) BIR3, and BIRC3 (c-IAP2) BIR3, respectively).1 GDC-0152 induces activation of caspases, decreasing the viability of cancer cells without affecting normal cells.1,2 It is orally bioavailable and suppresses tumor growth in breast cancer xenografts in mice.1 GDC-0152 also induces NF-κB transcriptional activity, resulting in the expression of several cytokines, including TNF-α.3 In dogs and rats, but not humans, this leads to a pronounced inflammatory response.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Flygare, J.A., Beresini, M., Budha, N., et al. Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152). J. Med. Chem. 55(9), 4101-4113 (2012).

    2. Hu, R., Li, J., Liu, Z., et al. GDC-0152 induces apoptosis through down-regulation of IAPs in human leukemia cells and inhibition of PI3K/Akt signaling pathway. Tumour Biol. 36(2), 577-584 (2015).

    3. Erickson, R.I., Tarrant, J., Cain, G., et al. Toxicity profile of small-molecule IAP antagonist GDC-0152 is linked to TNF-α pharmacology. Toxicol. Sci. 131(1), 247-258 (2013).