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MedKoo Cat#: 200080 | Name: Aderbasib
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Description:

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

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
Aderbasib
CAS#791828-58-5

Theoretical Analysis

MedKoo Cat#: 200080

Name: Aderbasib

CAS#: 791828-58-5

Chemical Formula: C21H28N4O5

Exact Mass: 416.2060

Molecular Weight: 416.47

Elemental Analysis: C, 60.56; H, 6.78; N, 13.45; O, 19.21

Price and Availability

Size Price Availability Quantity
1mg USD 250.00 Ready to ship
2mg USD 400.00 Ready to ship
5mg USD 850.00 Ready to ship
10mg USD 1,350.00 Ready to ship
25mg USD 2,850.00 Ready to ship
50mg USD 3,950.00 Ready to ship
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No Data
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
Solvent mg/mL mM
Solubility
DMSO 100.0 240.11
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 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.

Recalculate based on batch purity %
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.
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