2. GPCR/G Protein
  3. Adenosine Receptor
  4. MK-1088

MK-1088 is an orally active A2A/A2B adenosine receptor antagonist with human A2A Ki of 0.31 nM, human A2B Ki 5.3 nM. MK-1088 blocks receptor downstream signaling, inhibits CREB phosphorylation and reverses adenosine-mediated immunosuppression. MK-1088 restores TNF−α release and enhances tumor immune surveillance. MK-1088 can be used for the research of cancer[1].

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MK-1088

MK-1088 Chemical Structure

CAS No. : 2433765-51-4

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MK-1088 Related Antibodies

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Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

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Description

MK-1088 is an orally active A2A/A2B adenosine receptor antagonist with human A2A Ki of 0.31 nM, human A2B Ki 5.3 nM. MK-1088 blocks receptor downstream signaling, inhibits CREB phosphorylation and reverses adenosine-mediated immunosuppression. MK-1088 restores TNF−α release and enhances tumor immune surveillance. MK-1088 can be used for the research of cancer[1].

IC50 & Target[1]

hA2AAR

0.31 nM (Ki)

hA2B

5.3 nM (Ki)

hA1AR

82 nM (Ki)

hA3

233 nM (Ki)

In Vitro

MK-1088 (Compound 46) (60 min at room temperature) potently binds to hA2AR expressed in CHO cell membranes with a Ki of 0.31 nM[1].
MK-1088 (60 min at room temperature) binds to hA2BR with a Ki of 5.3 nM, showing a 16-fold lower potency relative to hA2BR[1].
MK-1088 (60 min at room temperature) binds to hA1R expressed in CHO-K1 cell membranes with a Ki of 82 nM, showing 259-fold lower potency relative to hA2AR[1].
MK-1088 (0.1 nM-100 μM) dose-dependently inhibits NECA-stimulated CREB phosphorylation in human CD4+ T cells with an IC50 of 70 nM[1].
MK-1088 dose-dependently recovers LPS (HY-D1056)-stimulated, NECA (HY-103173)-suppressed TNF-α release in human whole blood[1].
MK-1088 has a clean off-target profile for cardiac ion channels and most CYP enzymes, with only moderate inhibition of CYP3A4-midazolam (IC50 = 4.1 μM) and no time-dependent CYP3A4 inhibition[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MK-1088 Related Antibodies
Parmacokinetics
Species Dose Route CLunbound Vd T1/2 Bioavailability
Rat[1] 0.5 mg/kg i.v. 45.4 mL/min/kg 9.3 L/kg 2.3 h /
Rat[1] 3 mg/kg p.o. / / / 36.8 %
Dog[1] 0.1 mg/kg i.v. 6.6 mL/min/kg 5.7 L/kg 9.2 h /
Dog[1] 3 mg/kg p.o. / / / 42.4 %
Rhesus monkey[1] 0.5 mg/kg i.v. 45.2 mL/min/kg 8.9 L/kg 2.2 h /
Rhesus monkey[1] 3 mg/kg p.o. / / / 51.4 %
In Vivo

MK-1088 (Compound 46) (30 mg/kg; p.o.; twice daily; 16 days) delivers 54% tumor growth inhibition in BALB/c mice bearing CT26 syngeneic tumors, with 97% A2AR target engagement[1].
MK-1088 (30 mg/kg; p.o.; twice daily; 21 days) delivers 47% tumor growth inhibition as a single agent in mice bearing CM3 syngeneic tumors[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c mice (syngeneic tumor model)[1]
Dosage: 30 mg/kg
Administration: p.o.; twice daily; 16 days
Result: Achieved 54% tumor growth inhibition (TGI) relative to control tumors at day 16, p < 0.0001 by one-way ANOVA.
Reached 97% A2AR target engagement based on mouse A2AR affinity (Ki = 6 nM) and 10 h unbound plasma exposure.
Animal Model: Mice (10 animals per group; syngeneic tumor model)[1]
Dosage: 30 mg/kg
Administration: p.o.; twice daily; 21 days
Result: Afforded 47% tumor growth inhibition (TGI) as a single agent on study day 14.
Molecular Weight

468.53

Formula

C23H29FN8O2
CAS No.
SMILES

NC1=NC2=C(C=C(C(OC)=C2)F)C3=NC([C@@H]4CC[C@@H](N(C4)C5=CN(N=C5)CC(O)(C)C)C)=NN31
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MK-1088 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MK-10882433765-51-4MK1088MK 1088Adenosine ReceptorP1 receptoradenosine A2A receptortumor immune surveillanceadenosine A2B receptorBALB/c miceCREB phosphorylationCHO cell membranesCHO-K1 cell membraneshuman CD4+ T cellsTNF-αadenosine-mediated immunosuppressionInhibitorinhibitorinhibit

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