Dezapelisib

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MedKoo CAT#: 206781

CAS#: 1262440-25-4

Description: 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

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Dezapelisib
CAS# 1262440-25-4
Instruction

Theoretical Analysis

MedKoo Cat#: 206781
Name: Dezapelisib
CAS#: 1262440-25-4
Chemical Formula: C20H16FN7OS
Exact Mass: 421.11
Molecular Weight: 421.454
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 not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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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.

Biological target:
In vitro activity:
In vivo activity:

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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.