Saracatinib | AZD-0530 | CAS#379231-04-6 | Src-Abl inhibitor

MedKoo Cat#: 200410 | Name: Saracatinib free base

Description:

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

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.

Chemical Structure

Saracatinib free base

CAS#379231-04-6 (free base)

Theoretical Analysis

MedKoo Cat#: 200410

Name: Saracatinib free base

CAS#: 379231-04-6 (free base)

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

Price and Availability

Size	Price	Availability
50mg	USD 550.00	2 Weeks
100mg	USD 950.00	2 Weeks
200mg	USD 1,650.00	2 Weeks

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Related CAS #

893428-72-3 (fumarate) 379231-04-6 (free base)

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

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).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Saracatinib is a potent Src family inhibitor with IC50s of 2.7 to 11 nM for c-Src, Lck, c-YES, Lyn, Fyn, Fgr, and Blk. Saracatinib shows high selectivity over other tyrosine kinases.

In vitro activity:

Saracatinib potently inhibited Middle East respiratory syndrome-coronavirus (MERS-CoV) at the early stages of the viral life cycle in Huh-7 cells. Saracatinib exhibited a synergistic effect with gemcitabine. Saracatinib alone or in combination with gemcitabine could provide a new therapeutic option for the treatment of MERS-CoV infection. Reference: Viruses. 2018 May 24;10(6):283. https://pubmed.ncbi.nlm.nih.gov/29795047/

In vivo activity:

Saracatinib displays significant potential for atherosclerotic cardiovascular disease (ASCVD) treatment. Identifying unique ASCVD-related inflammatory signatures led to the recognition of saracatinib as an immunotherapy candidate. In ex vivo screens using human samples, saracatinib reversed inflammatory responses induced by ASCVD plasma. In Apoe-/- mice, saracatinib reduced atherosclerosis progression and in a rabbit model of advanced atherosclerosis, saracatinib reduced plaque inflammation. Reference: Nat Cardiovasc Res. 2023 Jun;2(6):550-571. https://pubmed.ncbi.nlm.nih.gov/37771373/

	Solvent	mg/mL	mM
Solubility
	DMSO	50.0	92.25

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 542.03 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. Shin JS, Jung E, Kim M, Baric RS, Go YY. Saracatinib Inhibits Middle East Respiratory Syndrome-Coronavirus Replication In Vitro. Viruses. 2018 May 24;10(6):283. doi: 10.3390/v10060283. PMID: 29795047; PMCID: PMC6024778. 2. Yamaguchi H, Takanashi M, Yoshida N, Ito Y, Kamata R, Fukami K, Yanagihara K, Sakai R. Saracatinib impairs the peritoneal dissemination of diffuse-type gastric carcinoma cells resistant to Met and fibroblast growth factor receptor inhibitors. Cancer Sci. 2014 May;105(5):528-36. doi: 10.1111/cas.12387. Epub 2014 Mar 24. PMID: 24612061; PMCID: PMC4317844. 3. Amadori L, Calcagno C, Fernandez DM, Koplev S, Fernandez N, Kaur R, Mury P, Khan NS, Sajja S, Shamailova R, Cyr Y, Jeon M, Hill CA, Chong PS, Naidu S, Sakurai K, Ghotbi AA, Soler R, Eberhardt N, Rahman A, Faries P, Moore KJ, Fayad ZA, Ma'ayan A, Giannarelli C. Systems immunology-based drug repurposing framework to target inflammation in atherosclerosis. Nat Cardiovasc Res. 2023 Jun;2(6):550-571. doi: 10.1038/s44161-023-00278-y. Epub 2023 Jun 8. PMID: 37771373; PMCID: PMC10538622. 4. Gage M, Putra M, Wachter L, Dishman K, Gard M, Gomez-Estrada C, Thippeswamy T. Saracatinib, a Src Tyrosine Kinase Inhibitor, as a Disease Modifier in the Rat DFP Model: Sex Differences, Neurobehavior, Gliosis, Neurodegeneration, and Nitro-Oxidative Stress. Antioxidants (Basel). 2021 Dec 28;11(1):61. doi: 10.3390/antiox11010061. PMID: 35052568; PMCID: PMC8773289.

In vitro protocol:

In vivo protocol:

1. Amadori L, Calcagno C, Fernandez DM, Koplev S, Fernandez N, Kaur R, Mury P, Khan NS, Sajja S, Shamailova R, Cyr Y, Jeon M, Hill CA, Chong PS, Naidu S, Sakurai K, Ghotbi AA, Soler R, Eberhardt N, Rahman A, Faries P, Moore KJ, Fayad ZA, Ma'ayan A, Giannarelli C. Systems immunology-based drug repurposing framework to target inflammation in atherosclerosis. Nat Cardiovasc Res. 2023 Jun;2(6):550-571. doi: 10.1038/s44161-023-00278-y. Epub 2023 Jun 8. PMID: 37771373; PMCID: PMC10538622. 2. Gage M, Putra M, Wachter L, Dishman K, Gard M, Gomez-Estrada C, Thippeswamy T. Saracatinib, a Src Tyrosine Kinase Inhibitor, as a Disease Modifier in the Rat DFP Model: Sex Differences, Neurobehavior, Gliosis, Neurodegeneration, and Nitro-Oxidative Stress. Antioxidants (Basel). 2021 Dec 28;11(1):61. doi: 10.3390/antiox11010061. PMID: 35052568; PMCID: PMC8773289.

1: Vidal SI, Menta N, Friedman A. To Acne and Beyond: A Review of Sarecycline's Off-Label Uses. J Drugs Dermatol. 2024 Sep 1;23(9):792-793. PMID: 39231076. 2: Elshenawy EA, Yassin MG, Marie AA. P-doped carbon dot nano-probe for inner filter effect-based determination of sarecycline in pharmaceutical dosage form and human plasma. Luminescence. 2024 Sep;39(9):e4889. doi: 10.1002/bio.4889. PMID: 39223967. 3: Xiong CY, Yang YM, Zhou Y, He TS, Luo XW, Wang J, Mao CX. Systematic analysis of the adverse effects of commonly used clinical tetracycline drugs based on the FAERS database. Expert Opin Drug Saf. 2024 Aug 19:1-9. doi: 10.1080/14740338.2024.2392865. Epub ahead of print. PMID: 39140181. 4: Swenson K, Stern A, Graber E. A Retrospective Review of a Cohort of Patients with Periorificial Dermatitis Treated with Sarecycline. J Clin Aesthet Dermatol. 2024 Jun;17(6):50-54. PMID: 38912196; PMCID: PMC11189645. 5: Baldwin HE, Graber E, Harper JC, Alexis AF, Stein Gold L, Kircik L, Del Rosso J, Hebert AA, Rieder EA, Fried RG, Narayanan S, Koscielny V, Kasujee I. INDIVIDUAL ARTICLE: Sarecycline Improves Acne Severity, Symptoms, and Psychosocial Burden in Non-nodular Acne Vulgaris: PROSES Study. J Drugs Dermatol. 2024 Feb 1;23(2):SF405634s12-SF405634s18. doi: 10.36849/JDD.SF405634. PMID: 38306152. 6: Graber E, Baldwin HE, Fried RG, Rieder EA, Hebert AA, Del Rosso J, Kircik L, Stein Gold L, Harper JC, Alexis AF, Narayanan S, Koscielny V, Kasujee I. INDIVIDUAL ARTICLE: Impact of Acne Vulgaris and Sarecycline on Social/Emotional Functioning and Daily Activities: PROSES Study. J Drugs Dermatol. 2024 Feb 1;23(2):SF405634s5-SF405634s11. doi: 10.36849/JDD.SF405634. PMID: 38306151. 7: Sher A, Kresch M, Bitterman D, Elbogen E, Lebwohl MG. Sarecycline as a Potential Treatment for Steroid-Induced Rosacea/Perioral Dermatitis: A Case Report. J Drugs Dermatol. 2024 Feb 1;23(2):e55-e56. doi: 10.36849/JDD.7638. PMID: 38306126. 8: Reynolds RV, Yeung H, Cheng CE, Cook-Bolden F, Desai SR, Druby KM, Freeman EE, Keri JE, Stein Gold LF, Tan JKL, Tollefson MM, Weiss JS, Wu PA, Zaenglein AL, Han JM, Barbieri JS. Guidelines of care for the management of acne vulgaris. J Am Acad Dermatol. 2024 May;90(5):1006.e1-1006.e30. doi: 10.1016/j.jaad.2023.12.017. Epub 2024 Jan 30. PMID: 38300170. 9: Drugs for acne. Med Lett Drugs Ther. 2024 Feb 5;66(1695):17-20. doi: 10.58347/tml.2024.1695a. PMID: 38294764. 10: Jung E, Gademann K. Clinically Approved Antibiotics from 2010 to 2022. Chimia (Aarau). 2023 Apr 26;77(4):230-234. doi: 10.2533/chimia.2023.230. PMID: 38047802. 11: Singh S, Boorgula GD, Aryal S, Philley JV, Gumbo T, Srivastava S. Sarecycline pharmacokinetics/pharmacodynamics in the hollow-fibre model of Mycobacterium avium complex: so near and yet so far. J Antimicrob Chemother. 2024 Jan 3;79(1):96-99. doi: 10.1093/jac/dkad352. PMID: 37946564; PMCID: PMC11032240. 12: Poplausky D, Young JN, Dubin DP, Tremblay D, Gulati N. Dasatinib-Associated Acneiform Eruption Successfully Treated With Sarecycline in a Patient With Chronic Myeloid Leukemia. Cureus. 2023 Sep 21;15(9):e45697. doi: 10.7759/cureus.45697. PMID: 37868438; PMCID: PMC10590148. 13: Choe J, Barbieri JS. Emerging Medical Therapies in Rosacea: A Narrative Review. Dermatol Ther (Heidelb). 2023 Dec;13(12):2933-2949. doi: 10.1007/s13555-023-01048-1. Epub 2023 Oct 12. PMID: 37824060; PMCID: PMC10689680. 14: Borash J, Bunick CG, Graber E. Ensuring Dermatologists Practice Enhanced Antibiotic Stewardship With Sarecycline Mnemonic. J Drugs Dermatol. 2023 Oct 1;22(10):1061. doi: 10.36849/JDD.7138. PMID: 37801533. 15: Martin V, Bettencourt AF, Santos C, Fernandes MH, Gomes PS. Unveiling the Osteogenic Potential of Tetracyclines: A Comparative Study in Human Mesenchymal Stem Cells. Cells. 2023 Sep 10;12(18):2244. doi: 10.3390/cells12182244. PMID: 37759467; PMCID: PMC10526833. 16: Heymann WR. Acne and rosacea therapies see the light. J Am Acad Dermatol. 2023 Oct;89(4):675-676. doi: 10.1016/j.jaad.2023.07.1019. Epub 2023 Jul 29. PMID: 37524168. 17: Tao RE, Prajapati S, Pixley JN, Grada A, Feldman SR. Oral Tetracycline-Class Drugs in Dermatology: Impact of Food Intake on Absorption and Efficacy. Antibiotics (Basel). 2023 Jul 5;12(7):1152. doi: 10.3390/antibiotics12071152. PMID: 37508248; PMCID: PMC10376323. 18: Harper JC, Armstrong A, Fried RG, Rieder EA, Alexis AF, Salem RJ, Kasujee I, Grada A. Patient-reported outcomes with sarecycline treatment for acne vulgaris: Pooled analysis of phase 3 clinical studies. J Am Acad Dermatol. 2023 Oct;89(4):832-834. doi: 10.1016/j.jaad.2023.04.075. Epub 2023 Jun 13. PMID: 37321481. 19: Li A, He S, Li J, Zhang Z, Li B, Chu H. Omadacycline, Eravacycline, and Tigecycline Express Anti-Mycobacterium abscessus Activity In Vitro. 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