Crisaborole (AN2728)
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MedKoo CAT#: 200252

CAS#: 906673-24-3

Description: Crisaborole, also known as AN-2728, is a topically administered, boron-containing, anti-inflammatory compound that inhibits PDE4 activity and thereby suppresses the release of TNFalpha, IL-12, IL-23 and other cytokines. At the time of publication, three phase Ib clinical trials, a IIa trial and a IIb trial of AN-2728 in patients with psoriasis had been completed; the compound was also undergoing phase II development for atopic dermatitis, but no data were available for this indication.


Chemical Structure

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Crisaborole (AN2728)
CAS# 906673-24-3

Theoretical Analysis

MedKoo Cat#: 200252
Name: Crisaborole (AN2728)
CAS#: 906673-24-3
Chemical Formula: C14H10BNO3
Exact Mass: 251.07537
Molecular Weight: 251.0451
Elemental Analysis: C, 66.98; H, 4.01; B, 4.31; N, 5.58; O, 19.12

Size Price Shipping out time Quantity
10mg USD 150 2 Weeks
25mg USD 250 2 Weeks
50mg USD 450 2 Weeks
100mg USD 750 2 Weeks
200mg USD 1250 2 Weeks
500mg USD 1950 2 Weeks
1g USD 2650 2 Weeks
2g USD 3450 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-02-26. Prices are subject to change without notice.

Crisaborole (AN2728), purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Related CAS #: 906673-24-3   906673-25-4    

Synonym: AN2728; AN-2728; AN 2728; Crisaborole, Eucrisa;

IUPAC/Chemical Name: 4-((1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)oxy)benzonitrile

InChi Key: IQBSCLXAECVABP-UHFFFAOYSA-N

InChi Code: InChI=1S/C14H10BNO3/c16-8-10-1-4-12(5-2-10)19-13-6-3-11-9-18-15(17)14(11)7-13/h1-7,17H,9H2

SMILES Code: N#CC1=CC=C(OC2=CC=C3C(B(O)OC3)=C2)C=C1

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

Handling Instructions:

Preparing Stock Solutions

The following data is based on the product molecular weight 251.0451 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.

Select a batch to recalculate based on the batch molecular weight:
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

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1: Thombre A, Tse S, Yeoh T, Chen R, North R, Brown M. Ex vivo (human skin) and in vivo (minipig) permeation of propylene glycol applied as topical crisaborole ointment, 2. Int J Pharm. 2019 Nov 21:118847. doi: 10.1016/j.ijpharm.2019.118847. [Epub ahead of print] PubMed PMID: 31759994.

2: Ono R, Yagi M, Shoji A, Fujita K, Yoshida M, Ports WC, Purohit VS. Phase 1 study of crisaborole in Japanese healthy volunteers and patients with atopic dermatitis. J Dermatol. 2019 Oct 27. doi: 10.1111/1346-8138.15123. [Epub ahead of print] PubMed PMID: 31657024.

3: Bissonnette R, Pavel AB, Diaz A, Werth JL, Zang C, Vranic I, Purohit VS, Zielinski MA, Vlahos B, Estrada YD, Saint-Cyr Proulx E, Ports WC, Guttman-Yassky E. Crisaborole and atopic dermatitis skin biomarkers: An intrapatient randomized trial. J Allergy Clin Immunol. 2019 Nov;144(5):1274-1289. doi: 10.1016/j.jaci.2019.06.047. Epub 2019 Aug 13. PubMed PMID: 31419544.

4: Demurtas A, Pescina S, Nicoli S, Santi P, Padula C. Development and validation of a simple method for the extraction and quantification of crisaborole in skin layers. Biomed Chromatogr. 2019 Nov;33(11):e4664. doi: 10.1002/bmc.4664. Epub 2019 Aug 29. PubMed PMID: 31342550.

5: Hashim PW, Chima M, Kim HJ, Bares J, Yao CJ, Singer G, Chen T, Genece J, Baum D, Kimmel GW, Nia JK, Gagliotti M, Lebwohl MG. Crisaborole 2% ointment for the treatment of intertriginous, anogenital, and facial psoriasis: a double-blind, randomized, vehicle-controlled trial. J Am Acad Dermatol. 2019 Jul 3. pii: S0190-9622(19)32287-X. doi: 10.1016/j.jaad.2019.06.1288. [Epub ahead of print] PubMed PMID: 31279028.

6: Callender VD, Alexis AF, Stein Gold LF, Lebwohl MG, Paller AS, Desai SR, Tan H, Ports WC, Zielinski MA, Tallman AM. Efficacy and Safety of Crisaborole Ointment, 2%, for the Treatment of Mild-to-Moderate Atopic Dermatitis Across Racial and Ethnic Groups. Am J Clin Dermatol. 2019 Oct;20(5):711-723. doi: 10.1007/s40257-019-00450-w. PubMed PMID: 31264114; PubMed Central PMCID: PMC6764931.

7: Pharmacoeconomic Review Report: Crisaborole Ointment, 2% (Eucrisa): (Pfizer Canada Inc.): Indication: For topical treatment of mild-to-moderate atopic dermatitis in patients two years of age and older [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2019 Apr. Available from http://www.ncbi.nlm.nih.gov/books/NBK542516/ PubMed PMID: 31211531.

8: Clinical Review Report: Crisaborole Ointment, 2% (Eucrisa): (Pfizer Canada Inc.): Indication: For topical treatment of mild to moderate atopic dermatitis in patients 2 years of age and older [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2019 Apr. Available from http://www.ncbi.nlm.nih.gov/books/NBK542348/ PubMed PMID: 31206290.

9: CADTH Canadian Drug Expert Committee Recommendation: Crisaborole (Eucrisa — Pfizer Canada Inc.): Indication: For topical treatment of mild-to-moderate atopic dermatitis in patients two years of age and older [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2019 Apr. No abstract available. Available from http://www.ncbi.nlm.nih.gov/books/NBK542403/ PubMed PMID: 31206288.

10: Kimyon RS, Schlarbaum JP, Liou YL, Hylwa SA, Warshaw EM. Allergic Contact Dermatitis to Crisaborole. Dermatitis. 2019 Jul/Aug;30(4):272-274. doi: 10.1097/DER.0000000000000488. PubMed PMID: 31136354.

11: Ständer S, Yosipovitch G, Bushmakin AG, Cappelleri JC, Luger T, Tom WL, Ports WC, Zielinski MA, Tallman AM, Tan H, Gerber RA. Examining the association between pruritus and quality of life in patients with atopic dermatitis treated with crisaborole. J Eur Acad Dermatol Venereol. 2019 Sep;33(9):1742-1746. doi: 10.1111/jdv.15712. Epub 2019 Jul 7. PubMed PMID: 31132182.

12: Ramachandran V, Cline A, Feldman SR, Strowd LC. Evaluating crisaborole as a treatment option for atopic dermatitis. Expert Opin Pharmacother. 2019 Jun;20(9):1057-1063. doi: 10.1080/14656566.2019.1604688. Epub 2019 Apr 19. PubMed PMID: 31002539.

13: Woo TE, Kuzel P. Crisaborole 2% Ointment (Eucrisa) for Atopic Dermatitis. Skin Therapy Lett. 2019 Mar;24(2):4-6. Review. PubMed PMID: 30970204.

14: Simpson EL, Yosipovitch G, Bushmakin AG, Cappelleri JC, Luger T, Ständer S, Tom WL, Ports WC, Zielinski MA, Tallman AM, Tan H, Gerber RA. Direct and Indirect Effects of Crisaborole Ointment on Quality of Life in Patients with Atopic Dermatitis: A Mediation Analysis. Acta Derm Venereol. 2019 Jul 1;99(9):756-761. doi: 10.2340/00015555-3181. PubMed PMID: 30896779.

15: Barney E, Prose NS, Ramirez M. Inflammatory linear verrucous epidermal nevus treated successfully with crisaborole ointment in a 5-year-old boy. Pediatr Dermatol. 2019 May;36(3):404-405. doi: 10.1111/pde.13793. Epub 2019 Mar 5. PubMed PMID: 30838675.

16: Pao-Ling Lin C, Gordon S, Her MJ, Rosmarin D. A retrospective study: Application site pain with the use of crisaborole, a topical phosphodiesterase 4 inhibitor. J Am Acad Dermatol. 2019 May;80(5):1451-1453. doi: 10.1016/j.jaad.2018.10.054. Epub 2018 Nov 2. PubMed PMID: 30395914.

17: Simpson EL, Paller AS, Boguniewicz M, Eichenfield LF, Feldman SR, Silverberg JI, Chamlin SL, Zane LT. Crisaborole Ointment Improves Quality of Life of Patients with Mild to Moderate Atopic Dermatitis and Their Families. Dermatol Ther (Heidelb). 2018 Dec;8(4):605-619. doi: 10.1007/s13555-018-0263-0. Epub 2018 Oct 22. PubMed PMID: 30345457; PubMed Central PMCID: PMC6261115.

18: Castelli G, Schaffer M. Crisaborole (Eucrisa) for Mild to Moderate Atopic Dermatitis. Am Fam Physician. 2018 Sep 15;98(6):379-380. PubMed PMID: 30215912.

19: Robbins AB, Gor A, Bui MR. Topical Crisaborole-A Potential Treatment for Recalcitrant Palmoplantar Psoriasis. JAMA Dermatol. 2018 Sep 1;154(9):1096-1097. doi: 10.1001/jamadermatol.2018.2397. PubMed PMID: 30090935.

20: Lee EB, Lebwohl MG, Wu JJ. Treatment of psoriasis with crisaborole. J Dermatolog Treat. 2019 Mar;30(2):156-157. doi: 10.1080/09546634.2018.1480747. Epub 2018 Jun 8. PubMed PMID: 29812961.



Additional Information

 Related CAS#
CAS#906673-24-3
CAS#906673-25-4