An MCT4 inhibitor
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AZD 0095

Item No. 42134

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,5,7-trimethyl-6-[[(3R)-1-[4-[6-(4-morpholinylmethyl)-3-pyridazinyl]phenyl]-3-pyrrolidinyl]oxy]-[1,2,4]triazolo[1,5-a]pyrimidine
CAS Number
2750001-23-9
Molecular Formula
C27H32N8O2
Formula Weight
500.6
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
CC1=NC2=NC(C)=NN2C(C)=C1O[C@@H](C3)CCN3C(C=C4)=CC=C4C(N=N5)=CC=C5CN6CCOCC6
InChi Code
InChI=1S/C27H32N8O2/c1-18-26(19(2)35-27(28-18)29-20(3)32-35)37-24-10-11-34(17-24)23-7-4-21(5-8-23)25-9-6-22(30-31-25)16-33-12-14-36-15-13-33/h4-9,24H,10-17H2,1-3H3/t24-/m1/s1
InChi Key
PHDAGSZQGNWGFE-XMMPIXPASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    10 mg

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    25 mg

    $656

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    50 mg

    $1,066

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    Cayman Chemical
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    Product Description

    AZD 0095 is an inhibitor of monocarboxylate transporter 4 (MCT4; IC50 = 1.3 nM for lactate efflux in SK-BR-3 cells).1 It selectively inhibits lactate influx in NCI H358 non-small cell lung cancer cells (IC50 = 6.1 nM), which highly express MCT4 and do not express MCT1, over lactate influx in K562 chronic myeloid leukemia cells (IC50 = >30 µM), which highly express MCT1 and do not express MCT4. It inhibits the proliferation of NCI H358 cells with an IC50 value of 26 nM. AZD 0095 (100 mg/kg twice per day) in combination with cediranib (Item No. 11495) reduces tumor growth in an NCI H358 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Goldberg, F.W., Kettle, J.G., Lamont, G.M., et al. Discovery of clinical candidate AZD0095, a selective inhibitor of monocarboxylate transporter 4 (MCT4) for oncology. J. Med. Chem. 66(1), 384-397 (2023).