Aderbasib | INCB-7839 | INCB007839 | CAS#791828-58-5 | ADAM Inhibitor

Aderbasib
featured

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

MedKoo CAT#: 200080

CAS#: 791828-58-5

Description: Aderbasib, also known as INCB007839, is a sheddase inhibitor, is also an orally bioavailable inhibitor of the ADAM (A Disintegrin And Metalloprotease) family of multifunctional membrane-bound proteins with potential antineoplastic activity. Aderbasib represses the metalloproteinase "sheddase" activities of ADAM10 and ADAM17, which may result in the inhibition of tumor cell proliferation. The metalloproteinase domains of ADAMs cleave cell surface proteins at extracellular sites proximal to the cell membrane, releasing or "shedding" soluble protein etcodomains from the cell surface; the disintegrin domains of these multifunctional proteins interact with various components of the extracellular matrix (ECM).

Chemical Structure

Aderbasib

CAS# 791828-58-5

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 200080
Name: Aderbasib
CAS#: 791828-58-5
Chemical Formula: C21H28N4O5
Exact Mass: 416.21
Molecular Weight: 416.471
Elemental Analysis: C, 60.56; H, 6.78; N, 13.45; O, 19.21

Price and Availability

Size	Price	Availability
1mg	USD 350	Ready to ship
2mg	USD 550	Ready to ship
5mg	USD 1050	Ready to ship
10mg	USD 1750	Ready to ship
25mg	USD 2950	Ready to ship
50mg	USD 3950	Ready to ship
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: INCB7839; INCB 7839; INCB-7839; INCB007839; INCB 007839; INCB-007839; Aderbasib.

IUPAC/Chemical Name: (6S,7S)-7-[(Hydroxyamino)carbonyl]-6-[(4-phenyl-1-piperazinyl)carbonyl]-5-azaspiro[2.5]octane-5-carboxylic acid methyl ester

InChi Key: DJXMSZSZEIKLQZ-IRXDYDNUSA-N

InChi Code: InChI=1S/C21H28N4O5/c1-30-20(28)25-14-21(7-8-21)13-16(18(26)22-29)17(25)19(27)24-11-9-23(10-12-24)15-5-3-2-4-6-15/h2-6,16-17,29H,7-14H2,1H3,(H,22,26)/t16-,17-/m0/s1

SMILES Code: O=C(N([C@H](C(N1CCN(C2=CC=CC=C2)CC1)=O)[C@@H](C(NO)=O)C3)CC43CC4)OC

Appearance: Solid powder

Purity: >95% (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: >5 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: Aderbasib was being developed by Incyte as a potential adjunctive treatment for metastatic breast cancer. Development was halted in 2011 after positive findings from Phase II trials were contradicted by further research. (http://en.wikipedia.org/wiki/Aderbasib).

Product Data:

Product Data

Certificate of Analysis:

View CoA: current batch, Lot#A21T10T04

Safety Data Sheet (SDS):

View Safety Data Sheet (SDS)

Instruction:

View handling instruction

Biological target:	Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17 that exhibits robust antineoplastic activity.
In vitro activity:	TBD
In vivo activity:	HER-2/neu+ BT474-SC1 human breast cancer xenografts were established. INCB7839 was administered at a dose capable of achieving steady-state levels of 500 nmol/L to 1 μmol/L in plasma. This concentration was previously determined to be above the IC50 for HER-2/neu and EGFR ligand shedding. Treatment with the INCB7839 sheddase inhibitor resulted in a decrease in mean tumor volume compared with animals treated with the vehicle. Reference: Cancer Res. 2008 Sep 1;68(17):7083-9. https://cancerres.aacrjournals.org/content/68/17/7083.long

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	100.0	240.11

Preparing Stock Solutions

The following data is based on the product molecular weight 416.47 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. Witters L, Scherle P, Friedman S, Fridman J, Caulder E, Newton R, Lipton A. Synergistic inhibition with a dual epidermal growth factor receptor/HER-2/neu tyrosine kinase inhibitor and a disintegrin and metalloprotease inhibitor. Cancer Res. 2008 Sep 1;68(17):7083-9. doi: 10.1158/0008-5472.CAN-08-0739. PMID: 18757423.
In vitro protocol:	TBD
In vivo protocol:	1. Witters L, Scherle P, Friedman S, Fridman J, Caulder E, Newton R, Lipton A. Synergistic inhibition with a dual epidermal growth factor receptor/HER-2/neu tyrosine kinase inhibitor and a disintegrin and metalloprotease inhibitor. Cancer Res. 2008 Sep 1;68(17):7083-9. doi: 10.1158/0008-5472.CAN-08-0739. PMID: 18757423.

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt* g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1

Volume 1

Concentration 2

Volume 2

1: Melani RD, Gerbasi VR, Anderson LC, Sikora JW, Toby TK, Hutton JE, Butcher DS, Negrão F, Seckler HS, Srzentić K, Fornelli L, Camarillo JM, LeDuc RD, Cesnik AJ, Lundberg E, Greer JB, Fellers RT, Robey MT, DeHart CJ, Forte E, Hendrickson CL, Abbatiello SE, Thomas PM, Kokaji AI, Levitsky J, Kelleher NL. The Blood Proteoform Atlas: A reference map of proteoforms in human hematopoietic cells. Science. 2022 Jan 28;375(6579):411-418. doi: 10.1126/science.aaz5284. Epub 2022 Jan 27. PMID: 35084980; PMCID: PMC9097315.

2: Gumiero JL, Oliveira BMS, Neto PAO, Pandini RV, Gerbasi LS, Figueiredo MN, Kruger JAP, Seid VE, Araujo SEA, Tustumi F. Timing of resection of synchronous colorectal liver metastasis: A systematic review and meta-analysis. J Surg Oncol. 2022 Jul;126(1):175-188. doi: 10.1002/jso.26868. PMID: 35689576.

3: Aguayo-Estremera R, Miragaya-Casillas C, Correa M, Ruiz-Villaverde A. Spanish Adaptation of the Self- and Other-Interest Inventory in Academic Settings. Span J Psychol. 2021 Jun 10;24:e36. doi: 10.1017/SJP.2021.29. PMID: 34108065.

4: Araujo SEA, Seid VE, Portilho AS, Marcante MT, Pandini RV, Gerbasi LS, Figueiredo MN. Robotic Ventral Mesh Rectopexy. Dis Colon Rectum. 2022 Jan 1;65(1):e4. doi: 10.1097/DCR.0000000000002073. PMID: 34882635.

5: RIECKE H. Perniziosiforme Anämie (Gerbasi) im Säuglingsalter [Gerbasi's perniciosiform anemia in infants]. Arch Kinderheilkd. 1954;148(1):71-4. Undetermined Language. PMID: 13181445.

6: Eldar-Lissai A, Cohen JT, Meltzer-Brody S, Gerbasi ME, Chertavian E, Hodgkins P, Bond JC, Johnson SJ. Cost-Effectiveness of Brexanolone Versus Selective Serotonin Reuptake Inhibitors for the Treatment of Postpartum Depression in the United States. J Manag Care Spec Pharm. 2020 May;26(5):627-638. doi: 10.18553/jmcp.2020.19306. Epub 2020 Mar 19. PMID: 32191592.

7: Leonard B, Danna V, Gorham L, Davison M, Chrisler W, Kim DN, Gerbasi VR. Shaping Nanobodies and Intrabodies against Proteoforms. Anal Chem. 2023 May 26. doi: 10.1021/acs.analchem.3c00958. Epub ahead of print. PMID: 37235478.

8: Fonti FE, Rizzoni G. Anémie pseudopernicieuse du nourrisson (Gerbasi) dans le cadre des anémies mégaloblastiques du premier âge [Pseudopernicious (Gerbasi's) anemia in infants in the framework of megaloblastic anemias of infancy]. Arch Fr Pediatr. 1967 Feb;24(2):217-27. French. PMID: 6032020.

9: GATTO I. Perniziosiforme Anämie des Säuglings (Gerbasi-Anämie) [Pernicious anemia in infants (Gerbasi anemia)]. Blut. 1957 Jan;3(1):31-40. German. doi: 10.1007/BF01630343. PMID: 13412775.

10: Golden DE, Gerbasi VR, Sontheimer EJ. An inside job for siRNAs. Mol Cell. 2008 Aug 8;31(3):309-12. doi: 10.1016/j.molcel.2008.07.008. PMID: 18691963; PMCID: PMC2675693.

11: Berlin FS. Sex offender treatment and legislation. J Am Acad Psychiatry Law. 2003;31(4):510-3. PMID: 14974807.

12: Pandini RV, Seid VE, Gerbasi LS, Figuereiredo MN, Portilho AS, Marcelino M, Araújo SEA. Pushing the limits for the treatment of anal canal cancer. Tech Coloproctol. 2021 Jan;25(1):143-145. doi: 10.1007/s10151-020-02288-5. Epub 2020 Jul 3. PMID: 32621154.

13: BURGIO GR, RUSSO G, LO JACONO F. Die hämatologische Reaktion auf kleine perorale Dosen von Vitamin B12 bei der perniziosiformen Anämie des Säuglings (Gerbasi) [Hematological reaction to small peroral doses of vitamin B12 in pernicious anemia in infants (Gerbasi)]. Arch Kinderheilkd. 1956;152(2):109-21. German. PMID: 13340751.

14: Karacić GJ. Magaloblastna anemija dojenceta (pernicioziformna anemia Gerbasi [Megaloblastic anemia in an infant (pernicious form anemia Gerbasi)]. Med Arh. 1970 Jan-Feb;24(1):19-24. Croatian. PMID: 5520013.

15: Schneider CG, Fey J, Zou X, Gerbasi V, Savransky T, Batt C, Bergmann-Leitner E, Angov E. Norovirus-VLPs expressing pre-erythrocytic malaria antigens induce functional immunity against sporozoite infection. Vaccine. 2022 Jul 29;40(31):4270-4280. doi: 10.1016/j.vaccine.2022.05.076. Epub 2022 Jun 10. PMID: 35697572.

16: Gerbasi JB. Managed care and ERISA: synopsis and case law review. J Am Acad Psychiatry Law. 2003;31(3):364-71. PMID: 14584538.

17: Gerbasi ME, Prentice DA. The Self- and Other-Interest Inventory. J Pers Soc Psychol. 2013 Sep;105(3):495-514. doi: 10.1037/a0033483. Epub 2013 Jun 24. PMID: 23795908.

18: Gerbasi LS, Tustumi F, Pandini RV, de Souza Novo R, Seid VE, Araujo SEA. Laparoscopic rectosigmoidectomy for cancer in a pregnant patient-a video vignette. Colorectal Dis. 2023 Apr 28. doi: 10.1111/codi.16588. Epub ahead of print. PMID: 37118870.

19: Gerbasi JB, Scott CL. Sell v. U.S.: involuntary medication to restore trial competency--a workable standard? J Am Acad Psychiatry Law. 2004;32(1):83-90. PMID: 15497635.

20: Gerbasi ME, Gilman SE, Bitton A, Becker AE. Social Norms and Smoking Risk in iTaukei Fijian Adolescent Women. Health Behav Policy Rev. 2019 May;6(3):242-255. doi: 10.14485/HBPR.6.3.4. PMID: 31157285; PMCID: PMC6541446.

Your view history

Aderbasib featured