AZD4635
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MedKoo CAT#: 206930

CAS#: 1321514-06-0

Description: AZD-4635, also known as HTL-1071, is an orally available, small molecule adenosine A2A receptor antagonist.

Chemical Structure

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AZD4635
CAS# 1321514-06-0
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 206930
Name: AZD4635
CAS#: 1321514-06-0
Chemical Formula: C15H11ClFN5
Exact Mass: 315.07
Molecular Weight: 315.736
Elemental Analysis: C, 57.06; H, 3.51; Cl, 11.23; F, 6.02; N, 22.18

Price and Availability

Size Price Availability Quantity
5mg USD 90 Ready to ship
10mg USD 150 Ready to ship
25mg USD 250 Ready to ship
50mg USD 400 Ready to ship
100mg USD 700 Ready to ship
200mg USD 1250 Ready to ship
500mg USD 2650 Ready to ship
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Synonym: imaradenant; AZD-4635; AZD 4635; AZD4635; HTL-1071; HTL 1071; HTL1071.

IUPAC/Chemical Name: 6-(2-chloro-6-methylpyridin-4-yl)-5-(4-fluorophenyl)-1,2,4-triazin-3-amine

InChi Key: NCWQLHHDGDXIJN-UHFFFAOYSA-N

InChi Code: InChI=1S/C15H11ClFN5/c1-8-6-10(7-12(16)19-8)14-13(20-15(18)22-21-14)9-2-4-11(17)5-3-9/h2-7H,1H3,(H2,18,20,22)

SMILES Code: NC1=NC(C2=CC=C(F)C=C2)=C(C3=CC(C)=NC(Cl)=C3)N=N1

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target: AZD4635 binds to human A2AR with a Ki of 1.7 nM and shows >30-fold selectivity over other adenosine receptors. In the presence of 0.1, 1 and 10 μM adenosine, the IC50s of AZD4635 for inhibition of cAMP production are 0.79, 10.0 and 142.9 nM, respectively.
In vitro activity: The A2A receptor is a member of the G-coupled receptor family with activation leading to increased intracellular levels of cAMP. The potency of AZD4635 in inhibiting A2AR signaling was determined in a cAMP accumulation assay using CHO cells stably transfected with human A2AR (figure 1D) and stimulated with adenosine (100, 10, 1 and 0.1 µM). Owing to the competitive binding mechanism of inhibition, the antagonist activity (IC50) of AZD4635 was impacted by the adenosine concentration. As the concentration of adenosine was increased, the potency of AZD4635 antagonist activity was reduced, with a linear relationship. AZD4635 demonstrated an IC50 of 0.000794, 0.0123, 0.155 and 2.69 µM at concentrations of 0.1, 1, 10 and 100 µM adenosine. Reference: J Immunother Cancer. 2020 Jul;8(2):e000417. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7394305/
In vivo activity: AZD4635 is an oral antagonist of the high-affinity A2A receptor, which reversed T-cell suppression ex vivo when incubated with the adenosine analog 5′-N-ethylcarboxamidoadenosine. In addition, AZD4635 partially restored CADO-mediated inhibition of T-cell proliferation (figure 4E, online supplementary figure S3C). Reference: J Immunother Cancer. 2020 May;8(1):e000610. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7239696/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 56.7 179.42
DMSO:PBS(pH 7.2) (1:3) 0.3 0.79
DMF 30.0 95.01

Preparing Stock Solutions

The following data is based on the product molecular weight 315.74 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Borodovsky A, Barbon CM, Wang Y, Ye M, Prickett L, Chandra D, Shaw J, Deng N, Sachsenmeier K, Clarke JD, Linghu B, Brown GA, Brown J, Congreve M, Cheng RK, Dore AS, Hurrell E, Shao W, Woessner R, Reimer C, Drew L, Fawell S, Schuller AG, Mele DA. Small molecule AZD4635 inhibitor of A2AR signaling rescues immune cell function including CD103+ dendritic cells enhancing anti-tumor immunity. J Immunother Cancer. 2020 Jul;8(2):e000417. doi: 10.1136/jitc-2019-000417. PMID: 32727810; PMCID: PMC7394305. 2. Yang R, Elsaadi S, Misund K, Abdollahi P, Vandsemb EN, Moen SH, Kusnierczyk A, Slupphaug G, Standal T, Waage A, Slørdahl TS, Rø TB, Rustad E, Sundan A, Hay C, Cooper Z, Schuller AG, Woessner R, Borodovsky A, Menu E, Børset M, Sponaas AM. Conversion of ATP to adenosine by CD39 and CD73 in multiple myeloma can be successfully targeted together with adenosine receptor A2A blockade. J Immunother Cancer. 2020 May;8(1):e000610. doi: 10.1136/jitc-2020-000610. PMID: 32409420; PMCID: PMC7239696.
In vitro protocol: 1. Borodovsky A, Barbon CM, Wang Y, Ye M, Prickett L, Chandra D, Shaw J, Deng N, Sachsenmeier K, Clarke JD, Linghu B, Brown GA, Brown J, Congreve M, Cheng RK, Dore AS, Hurrell E, Shao W, Woessner R, Reimer C, Drew L, Fawell S, Schuller AG, Mele DA. Small molecule AZD4635 inhibitor of A2AR signaling rescues immune cell function including CD103+ dendritic cells enhancing anti-tumor immunity. J Immunother Cancer. 2020 Jul;8(2):e000417. doi: 10.1136/jitc-2019-000417. PMID: 32727810; PMCID: PMC7394305.
In vivo protocol: 1. Yang R, Elsaadi S, Misund K, Abdollahi P, Vandsemb EN, Moen SH, Kusnierczyk A, Slupphaug G, Standal T, Waage A, Slørdahl TS, Rø TB, Rustad E, Sundan A, Hay C, Cooper Z, Schuller AG, Woessner R, Borodovsky A, Menu E, Børset M, Sponaas AM. Conversion of ATP to adenosine by CD39 and CD73 in multiple myeloma can be successfully targeted together with adenosine receptor A2A blockade. J Immunother Cancer. 2020 May;8(1):e000610. doi: 10.1136/jitc-2020-000610. PMID: 32409420; PMCID: PMC7239696.

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1: Jazayeri A, Andrews SP, Marshall FH. Structurally Enabled Discovery of
Adenosine A(2A) Receptor Antagonists. Chem Rev. 2017 Jan 11;117(1):21-37. doi:
10.1021/acs.chemrev.6b00119. Epub 2016 Jun 22. Review. PubMed PMID: 27333206.

2. http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=9236