AZ10397767 | AZ-10397767 | CAS#333742-63-5 | CXCR2 antagonist

AZ10397767
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 407412

CAS#: 333742-63-5

Description: AZ10397767 is a potent CXCR2 antagonist (IC50 = 1 nM). AZ10397767 significantly reduced the numbers of infiltrating neutrophils into both in vitro and in vivo tumor models, which was associated with slower growing tumors. AZ10397767 increased 17-AAG-induced apoptosis and necrosis and decreased NF-kappaB activity/CXCL8 expression in 17-AAG-treated PC3 cells.

Chemical Structure

AZ10397767

CAS# 333742-63-5

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 407412
Name: AZ10397767
CAS#: 333742-63-5
Chemical Formula: C15H14ClFN4O2S2
Exact Mass: 400.02
Molecular Weight: 400.871
Elemental Analysis: C, 44.94; H, 3.52; Cl, 8.84; F, 4.74; N, 13.98; O, 7.98; S, 16.00

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 375
50mg	USD 1450
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: AZ-10397767; AZ 10397767; AZ10397767.

IUPAC/Chemical Name: 5-[[(3-Chloro-2-fluorophenyl)methyl]thio]-7-[[(1R)-2-hydroxy-1-methylethyl]amino]thiazolo[4,5-d]pyrimidin-2(3H)-one

InChi Key: KHTUORKUWBDRBX-SSDOTTSWSA-N

InChi Code: InChI=1S/C15H14ClFN4O2S2/c1-7(5-22)18-12-11-13(21-15(23)25-11)20-14(19-12)24-6-8-3-2-4-9(16)10(8)17/h2-4,7,22H,5-6H2,1H3,(H2,18,19,20,21,23)/t7-/m1/s1

SMILES Code: O=C1SC2=C(N[C@H](C)CO)N=C(SCC3=CC=CC(Cl)=C3F)N=C2N1

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:

Product Data:

Product Data

Instruction:

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Biological target:	Potent CXCR2 antagonist.
In vitro activity:	The addition of AZ10397767, used at a final concentration of 20 nM in order to exercise its selectivity for the CXCR2 receptor increased the potency of 5-FU-induced cytotoxicity in PC3 cells. Non-linear regression analysis of the data confirmed that the inhibition of CXCR2 signaling enhanced the potency of 5-FU by 3.8-fold, increasing the calculated IC30 value from 4.2 µM to 1.1 µM (n = 4). Reference: PLoS One. 2012; 7(5): e36545. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3348872/
In vivo activity:	The mean tumor volume in AZ10397767-treated tumors started to diverge from control tumor volume by day 21 (11 days after commencement of antagonist dosing). At day 25 there was a significant difference (p < 0.05) in the volume of AZ10397767-treated compared to control tumors (Fig. 5a), this difference was more pronounced over the next several days and by day 31 AZ10397767-treated tumors were 36% smaller than their control counterparts (p < 0.01; Fig. 6a). Gr-1-positive neutrophils were abundant and distributed throughout A549 xenograft control mouse tumors when analyzed by immunohistochemistry (Fig. 5b). However, administration of AZ10397767 significantly (p < 0.01) reduced the number of tumor-infiltrating neutrophils compared to mice receiving vehicle control (Fig. 5b). Reference: Int J Cancer. 2011 Aug 15;129(4):847-58. https://pubmed.ncbi.nlm.nih.gov/21328342/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	40.1	100.01

Preparing Stock Solutions

The following data is based on the product molecular weight 400.87 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.

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. Wilson C, Maxwell PJ, Longley DB, Wilson RH, Johnston PG, Waugh DJ. Constitutive and treatment-induced CXCL8-signalling selectively modulates the efficacy of anti-metabolite therapeutics in metastatic prostate cancer. PLoS One. 2012;7(5):e36545. doi: 10.1371/journal.pone.0036545. Epub 2012 May 9. PMID: 22590561; PMCID: PMC3348872. 2. Tazzyman S, Barry ST, Ashton S, Wood P, Blakey D, Lewis CE, Murdoch C. Inhibition of neutrophil infiltration into A549 lung tumors in vitro and in vivo using a CXCR2-specific antagonist is associated with reduced tumor growth. Int J Cancer. 2011 Aug 15;129(4):847-58. doi: 10.1002/ijc.25987. Epub 2011 Apr 13. PMID: 21328342.
In vitro protocol:	1. Wilson C, Maxwell PJ, Longley DB, Wilson RH, Johnston PG, Waugh DJ. Constitutive and treatment-induced CXCL8-signalling selectively modulates the efficacy of anti-metabolite therapeutics in metastatic prostate cancer. PLoS One. 2012;7(5):e36545. doi: 10.1371/journal.pone.0036545. Epub 2012 May 9. PMID: 22590561; PMCID: PMC3348872. 2. Tazzyman S, Barry ST, Ashton S, Wood P, Blakey D, Lewis CE, Murdoch C. Inhibition of neutrophil infiltration into A549 lung tumors in vitro and in vivo using a CXCR2-specific antagonist is associated with reduced tumor growth. Int J Cancer. 2011 Aug 15;129(4):847-58. doi: 10.1002/ijc.25987. Epub 2011 Apr 13. PMID: 21328342.
In vivo protocol:	1. Tazzyman S, Barry ST, Ashton S, Wood P, Blakey D, Lewis CE, Murdoch C. Inhibition of neutrophil infiltration into A549 lung tumors in vitro and in vivo using a CXCR2-specific antagonist is associated with reduced tumor growth. Int J Cancer. 2011 Aug 15;129(4):847-58. doi: 10.1002/ijc.25987. Epub 2011 Apr 13. PMID: 21328342.

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1: Tazzyman S, Barry ST, Ashton S, Wood P, Blakey D, Lewis CE, Murdoch C. Inhibition of neutrophil infiltration into A549 lung tumors in vitro and in vivo using a CXCR2-specific antagonist is associated with reduced tumor growth. Int J Cancer. 2011 Aug 15;129(4):847-58. doi: 10.1002/ijc.25987. PubMed PMID: 21328342.

2: Seaton A, Maxwell PJ, Hill A, Gallagher R, Pettigrew J, Wilson RH, Waugh DJ. Inhibition of constitutive and cxc-chemokine-induced NF-kappaB activity potentiates ansamycin-based HSP90-inhibitor cytotoxicity in castrate-resistant prostate cancer cells. Br J Cancer. 2009 Nov 3;101(9):1620-9. doi: 10.1038/sj.bjc.6605356. PubMed PMID: 19809428; PubMed Central PMCID: PMC2778515.

3: Wilson C, Maxwell PJ, Longley DB, Wilson RH, Johnston PG, Waugh DJ. Constitutive and treatment-induced CXCL8-signalling selectively modulates the efficacy of anti-metabolite therapeutics in metastatic prostate cancer. PLoS One. 2012;7(5):e36545. doi: 10.1371/journal.pone.0036545. PubMed PMID: 22590561; PubMed Central PMCID: PMC3348872.

4: Wilson C, Wilson T, Johnston PG, Longley DB, Waugh DJ. Interleukin-8 signaling attenuates TRAIL- and chemotherapy-induced apoptosis through transcriptional regulation of c-FLIP in prostate cancer cells. Mol Cancer Ther. 2008 Sep;7(9):2649-61. doi: 10.1158/1535-7163.MCT-08-0148. PubMed PMID: 18790747.

5: Seaton A, Scullin P, Maxwell PJ, Wilson C, Pettigrew J, Gallagher R, O'Sullivan JM, Johnston PG, Waugh DJ. Interleukin-8 signaling promotes androgen-independent proliferation of prostate cancer cells via induction of androgen receptor expression and activation. Carcinogenesis. 2008 Jun;29(6):1148-56. doi: 10.1093/carcin/bgn109. PubMed PMID: 18487223.

6: Wilson C, Purcell C, Seaton A, Oladipo O, Maxwell PJ, O'Sullivan JM, Wilson RH, Johnston PG, Waugh DJ. Chemotherapy-induced CXC-chemokine/CXC-chemokine receptor signaling in metastatic prostate cancer cells confers resistance to oxaliplatin through potentiation of nuclear factor-kappaB transcription and evasion of apoptosis. J Pharmacol Exp Ther. 2008 Dec;327(3):746-59. doi: 10.1124/jpet.108.143826. PubMed PMID: 18780829.

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