MedKoo Cat#: 206781 | Name: Dezapelisib

Description:

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

Dezapelisib, also known as INCB040093, is an orally bioavailable, selective inhibitor of the delta isoform of the 110 kDa catalytic subunit of class I phosphoinositide-3 kinases (PI3K) with potential antineoplastic activity. INCB040093 specifically inhibits PI3Kdelta, which prevents both the production of the second messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and the activation of the PI3K/AKT kinase signaling pathway. This decreases proliferation and induces cell death in PI3K-overexpressing tumor cells.

Chemical Structure

Dezapelisib
Dezapelisib
CAS#1262440-25-4

Theoretical Analysis

MedKoo Cat#: 206781

Name: Dezapelisib

CAS#: 1262440-25-4

Chemical Formula: C20H16FN7OS

Exact Mass: 421.1121

Molecular Weight: 421.45

Elemental Analysis: C, 57.00; H, 3.83; F, 4.51; N, 23.26; O, 3.80; S, 7.61

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Synonym
Dezapelisib; INCB040093; INCB-040093; INCB 040093.
IUPAC/Chemical Name
6-(3-fluorophenyl)-3-methyl-7-((1S)-1-(9H-purin-6-ylamino)ethyl)-5H-(1,3)thiazolo(3,2-a)pyrimidin-5-one
InChi Key
RSIWALKZYXPAGW-NSHDSACASA-N
InChi Code
InChI=1S/C20H16FN7OS/c1-10-7-30-20-27-15(11(2)26-18-16-17(23-8-22-16)24-9-25-18)14(19(29)28(10)20)12-4-3-5-13(21)6-12/h3-9,11H,1-2H3,(H2,22,23,24,25,26)/t11-/m0/s1
SMILES Code
O=C1C(C2=CC=CC(F)=C2)=C([C@@H](NC3=C4N=CNC4=NC=N3)C)N=C5N1C(C)=CS5
Appearance
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
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
Unlike other isoforms of PI3K, PI3Kdelta is often overexpressed in tumor cells, especially those of hematologic origin, and plays a crucial role in tumor cell regulation and survival.

Preparing Stock Solutions

The following data is based on the product molecular weight 421.45 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
1: Shin N, Li YL, Mei S, Wang KH, Hall L, Katiyar K, Wang Q, Yang G, Rumberger B, Leffet L, He X, Rupar M, Bowman K, Favata M, Li J, Liu M, Li Y, Covington M, Koblish H, Soloviev M, Shuey D, Burn T, Diamond S, Fridman J, Combs A, Yao W, Yeleswaram S, Hollis G, Vaddi K, Huber R, Newton R, Scherle P. INCB040093 is a novel PI3Kδinhibitor for the treatment of B cell lymphoid malignancies. J Pharmacol Exp Ther. 2017 Nov 10. pii: jpet.117.244947. doi: 10.1124/jpet.117.244947. [Epub ahead of print] PubMed PMID: 29127109.