Saracatinib (AZD0530)
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MedKoo CAT#: 200410

CAS#: 379231-04-6

Description: Saracatinib, also known as AZD0530, is an orally available dual-specific inhibitor of Src and Abl with anti-invasive and anti-tumor activities. Src and Abl are protein tyrosine kinases that are overexpressed in chronic myeloid leukemia cells. Saracatinib binds to and inhibits these tyrosine kinases and their effects on cell motility, cell migration, adhesion, invasion, proliferation, differentiation, and survival.


Price and Availability

Size
Price

10mg
USD 110
100mg
USD 550
1g
USD 1650
10g
USD 6750
Size
Price

25mg
USD 180
200mg
USD 850
2g
USD 2650
20g
Ask price
Size
Price

50mg
USD 320
500mg
USD 1150
5g
USD 4650
50g
Ask price

Saracatinib, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 200410
Name: Saracatinib (AZD0530)
CAS#: 379231-04-6
Chemical Formula: C27H32ClN5O5
Exact Mass: 541.2092
Molecular Weight: 542.03
Elemental Analysis: C, 59.83; H, 5.95; Cl, 6.54; N, 12.92; O, 14.76


Synonym: AZD-0530; AZD0530; AZD 0530; Saracatinib.

IUPAC/Chemical Name: N-(5-Chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methyl-1-piperazinyl)ethoxy]-5-[(tetrahydro-2H-pyran-4-yl)oxy]-4-quinazolinamine

InChi Key: OUKYUETWWIPKQR-UHFFFAOYSA-N

InChi Code: InChI=1S/C27H32ClN5O5/c1-32-6-8-33(9-7-32)10-13-35-19-14-21-24(23(15-19)38-18-4-11-34-12-5-18)27(30-16-29-21)31-25-20(28)2-3-22-26(25)37-17-36-22/h2-3,14-16,18H,4-13,17H2,1H3,(H,29,30,31)

SMILES Code: CN1CCN(CCOC2=CC3=NC=NC(NC4=C5OCOC5=CC=C4Cl)=C3C(OC6CCOCC6)=C2)CC1


Technical Data

Appearance:
white 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, not in water

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).

Harmonized System Code:
293490


References

1: Huang RY, Wong MK, Tan TZ, Kuay KT, Ng AH, Chung VY, Chu YS, Matsumura N, Lai HC, Lee YF, Sim WJ, Chai C, Pietschmann E, Mori S, Low JJ, Choolani M, Thiery JP. An EMT spectrum defines an anoikis-resistant and spheroidogenic intermediate mesenchymal state that is sensitive to e-cadherin restoration by a src-kinase inhibitor, saracatinib (AZD0530). Cell Death Dis. 2013 Nov 7;4:e915. doi: 10.1038/cddis.2013.442. PubMed PMID: 24201814; PubMed Central PMCID: PMC3847320.

2: de Wispelaere M, LaCroix AJ, Yang PL. The small molecules AZD0530 and dasatinib inhibit dengue virus RNA replication via Fyn kinase. J Virol. 2013 Jul;87(13):7367-81. doi: 10.1128/JVI.00632-13. Epub 2013 Apr 24. PubMed PMID: 23616652; PubMed Central PMCID: PMC3700292.

3: Gangadhar TC, Clark JI, Karrison T, Gajewski TF. Phase II study of the Src kinase inhibitor saracatinib (AZD0530) in metastatic melanoma. Invest New Drugs. 2013 Jun;31(3):769-73. doi: 10.1007/s10637-012-9897-4. Epub 2012 Nov 15. PubMed PMID: 23151808; PubMed Central PMCID: PMC3600382.

4: Nam HJ, Im SA, Oh DY, Elvin P, Kim HP, Yoon YK, Min A, Song SH, Han SW, Kim TY, Bang YJ. Antitumor activity of saracatinib (AZD0530), a c-Src/Abl kinase inhibitor, alone or in combination with chemotherapeutic agents in gastric cancer. Mol Cancer Ther. 2013 Jan;12(1):16-26. doi: 10.1158/1535-7163.MCT-12-0109. Epub 2012 Nov 9. PubMed PMID: 23144237.

5: Liu KJ, He JH, Su XD, Sim HM, Xie JD, Chen XG, Wang F, Liang YJ, Singh S, Sodani K, Talele TT, Ambudkar SV, Chen ZS, Wu HY, Fu LW. Saracatinib (AZD0530) is a potent modulator of ABCB1-mediated multidrug resistance in vitro and in vivo. Int J Cancer. 2013 Jan 1;132(1):224-35. doi: 10.1002/ijc.27649. Epub 2012 Jun 13. PubMed PMID: 22623106; PubMed Central PMCID: PMC3459133.

6: Kaye S, Aamdal S, Jones R, Freyer G, Pujade-Lauraine E, de Vries EG, Barriuso J, Sandhu S, Tan DS, Hartog V, Kuenen B, Ruijter R, Kristensen GB, Nyakas M, Barrett S, Burke W, Pietersma D, Stuart M, Emeribe U, Boven E. Phase I study of saracatinib (AZD0530) in combination with paclitaxel and/or carboplatin in patients with solid tumours. Br J Cancer. 2012 May 22;106(11):1728-34. doi: 10.1038/bjc.2012.158. Epub 2012 Apr 24. PubMed PMID: 22531637; PubMed Central PMCID: PMC3364128.

7: Fujisaka Y, Onozawa Y, Kurata T, Yasui H, Goto I, Yamazaki K, Machida N, Watanabe J, Shimada H, Shi X, Boku N. First report of the safety, tolerability, and pharmacokinetics of the Src kinase inhibitor saracatinib (AZD0530) in Japanese patients with advanced solid tumours. Invest New Drugs. 2013 Feb;31(1):108-14. doi: 10.1007/s10637-012-9809-7. Epub 2012 Mar 14. PubMed PMID: 22415795.

8: Hannon RA, Finkelman RD, Clack G, Iacona RB, Rimmer M, Gossiel F, Baselga J, Eastell R. Effects of Src kinase inhibition by saracatinib (AZD0530) on bone turnover in advanced malignancy in a Phase I study. Bone. 2012 Apr;50(4):885-92. doi: 10.1016/j.bone.2011.12.017. Epub 2012 Jan 8. PubMed PMID: 22245630.

9: Gucalp A, Sparano JA, Caravelli J, Santamauro J, Patil S, Abbruzzi A, Pellegrino C, Bromberg J, Dang C, Theodoulou M, Massague J, Norton L, Hudis C, Traina TA. Phase II trial of saracatinib (AZD0530), an oral SRC-inhibitor for the treatment of patients with hormone receptor-negative metastatic breast cancer. Clin Breast Cancer. 2011 Oct;11(5):306-11. doi: 10.1016/j.clbc.2011.03.021. Epub 2011 May 3. PubMed PMID: 21729667; PubMed Central PMCID: PMC3222913.

10: Mackay HJ, Au HJ, McWhirter E, Alcindor T, Jarvi A, MacAlpine K, Wang L, Wright JJ, Oza AM. A phase II trial of the Src kinase inhibitor saracatinib (AZD0530) in patients with metastatic or locally advanced gastric or gastro esophageal junction (GEJ) adenocarcinoma: a trial of the PMH phase II consortium. Invest New Drugs. 2012 Jun;30(3):1158-63. doi: 10.1007/s10637-011-9650-4. Epub 2011 Mar 12. PubMed PMID: 21400081.

11: Fury MG, Baxi S, Shen R, Kelly KW, Lipson BL, Carlson D, Stambuk H, Haque S, Pfister DG. Phase II study of saracatinib (AZD0530) for patients with recurrent or metastatic head and neck squamous cell carcinoma (HNSCC). Anticancer Res. 2011 Jan;31(1):249-53. PubMed PMID: 21273606; PubMed Central PMCID: PMC3705960.

12: Renouf DJ, Moore MJ, Hedley D, Gill S, Jonker D, Chen E, Walde D, Goel R, Southwood B, Gauthier I, Walsh W, McIntosh L, Seymour L. A phase I/II study of the Src inhibitor saracatinib (AZD0530) in combination with gemcitabine in advanced pancreatic cancer. Invest New Drugs. 2012 Apr;30(2):779-86. doi: 10.1007/s10637-010-9611-3. Epub 2010 Dec 18. PubMed PMID: 21170669.

13: Dalton RN, Chetty R, Stuart M, Iacona RB, Swaisland A. Effects of the Src inhibitor saracatinib (AZD0530) on renal function in healthy subjects. Anticancer Res. 2010 Jul;30(7):2935-42. PubMed PMID: 20683035.

14: Arcaroli JJ, Touban BM, Tan AC, Varella-Garcia M, Powell RW, Eckhardt SG, Elvin P, Gao D, Messersmith WA. Gene array and fluorescence in situ hybridization biomarkers of activity of saracatinib (AZD0530), a Src inhibitor, in a preclinical model of colorectal cancer. Clin Cancer Res. 2010 Aug 15;16(16):4165-77. doi: 10.1158/1078-0432.CCR-10-0066. Epub 2010 Aug 3. PubMed PMID: 20682712; PubMed Central PMCID: PMC3805460.

15: Morrow CJ, Ghattas M, Smith C, Bönisch H, Bryce RA, Hickinson DM, Green TP, Dive C. Src family kinase inhibitor Saracatinib (AZD0530) impairs oxaliplatin uptake in colorectal cancer cells and blocks organic cation transporters. Cancer Res. 2010 Jul 15;70(14):5931-41. doi: 10.1158/0008-5472.CAN-10-0694. Epub 2010 Jun 15. PubMed PMID: 20551056; PubMed Central PMCID: PMC2906706.

16: Hannon RA, Clack G, Rimmer M, Swaisland A, Lockton JA, Finkelman RD, Eastell R. Effects of the Src kinase inhibitor saracatinib (AZD0530) on bone turnover in healthy men: a randomized, double-blind, placebo-controlled, multiple-ascending-dose phase I trial. J Bone Miner Res. 2010 Mar;25(3):463-71. doi: 10.1359/jbmr.090830. Erratum in: J Bone Miner Res. 2012 Jun;27(6):1435. PubMed PMID: 19775203.

17: Rajeshkumar NV, Tan AC, De Oliveira E, Womack C, Wombwell H, Morgan S, Warren MV, Walker J, Green TP, Jimeno A, Messersmith WA, Hidalgo M. Antitumor effects and biomarkers of activity of AZD0530, a Src inhibitor, in pancreatic cancer. Clin Cancer Res. 2009 Jun 15;15(12):4138-46. doi: 10.1158/1078-0432.CCR-08-3021. Epub 2009 Jun 9. PubMed PMID: 19509160.

18: Chen Y, Guggisberg N, Jorda M, Gonzalez-Angulo A, Hennessy B, Mills GB, Tan CK, Slingerland JM. Combined Src and aromatase inhibition impairs human breast cancer growth in vivo and bypass pathways are activated in AZD0530-resistant tumors. Clin Cancer Res. 2009 May 15;15(10):3396-405. doi: 10.1158/1078-0432.CCR-08-3127. PubMed PMID: 19451593.

19: Lara PN Jr, Longmate J, Evans CP, Quinn DI, Twardowski P, Chatta G, Posadas E, Stadler W, Gandara DR. A phase II trial of the Src-kinase inhibitor AZD0530 in patients with advanced castration-resistant prostate cancer: a California Cancer Consortium study. Anticancer Drugs. 2009 Mar;20(3):179-84. doi: 10.1097/CAD.0b013e328325a867. PubMed PMID: 19396016; PubMed Central PMCID: PMC3225398.

20: Green TP, Fennell M, Whittaker R, Curwen J, Jacobs V, Allen J, Logie A, Hargreaves J, Hickinson DM, Wilkinson RW, Elvin P, Boyer B, Carragher N, Plé PA, Bermingham A, Holdgate GA, Ward WH, Hennequin LF, Davies BR, Costello GF. Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530. Mol Oncol. 2009 Jun;3(3):248-61. doi: 10.1016/j.molonc.2009.01.002. Epub 2009 Feb 7. PubMed PMID: 19393585.