Pifusertib | CAS#1402602-94-1 | PKB/Akt Inhibitor

Pifusertib
new

featured

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

MedKoo CAT#: 527005

CAS#: 1402602-94-1

Description: Pifusertib, also known as TAS-117, is a PKB/Akt inhibitor potentially for the treatment of solid tumors. TAS-117 induced significant growth inhibition, associated with downregulation of phosphorylated Akt (p-Akt), selectively in MM cell lines with high baseline p-Akt. TAS-117 induced significant cytotoxicity in MM cells even in the presence of BM stromal cells, associated with inhibition of IL6 secretion. TAS-117 significantly inhibited human MM cell growth in murine xenograft models. TAS-117 triggered apoptosis and autophagy, as well as induction of endoplasmic reticulum (ER) stress response with minimal expression of C/EBP homologous protein (CHOP), a fatal ER stress marker. TAS-117 enhanced bortezomib-induced cytotoxicity in vivo, associated with prolonged host survival.

Chemical Structure

Pifusertib

CAS# 1402602-94-1

Instruction

Theoretical Analysis

MedKoo Cat#: 527005
Name: Pifusertib
CAS#: 1402602-94-1
Chemical Formula: C26H24N4O2
Exact Mass: 424.19
Molecular Weight: 424.504
Elemental Analysis: C, 73.56; H, 5.70; N, 13.20; O, 7.54

Price and Availability

Size	Price	Availability
25mg	USD 450	2 Weeks
50mg	USD 750	2 Weeks
100mg	USD 1250	2 Weeks
200mg	USD 2050	2 Weeks
500mg	USD 3850	2 Weeks
1g	USD 5850	2 Weeks
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: TAS-117, TAS 117, TAS117; Pifusertib

IUPAC/Chemical Name: (1r,3r)-3-amino-1-methyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenyl)cyclobutan-1-ol

InChi Key: AIFGVDXMHWGOGJ-DIVCQZSQSA-N

InChi Code: InChI=1S/C26H24N4O2/c1-25(31)14-26(27,15-25)19-9-7-17(8-10-19)22-23(18-5-3-2-4-6-18)30-16-32-21-11-12-28-13-20(21)24(30)29-22/h2-13,31H,14-16,27H2,1H3/t25-,26-

SMILES Code: C[C@]1(O)C[C@@](N)(C2=CC=C(C=C2)C3=C(C4=CC=CC=C4)N5COC6=CC=NC=C6C5=N3)C1

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: The PI3K/Akt pathway plays a crucial role in the pathogenesis of multiple myeloma (MM) in the bone marrow (BM) milieu.

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 424.50 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:
In vitro protocol:
In vivo protocol:

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: Rodón J, Funchain P, Laetsch TW, Arkenau HT, Hervieu A, Singer CF, Murciano- Goroff YR, Chawla SP, Anthony K, Yamamiya I, Liu M, Halim AB, Benhadji KA, Takahashi O, Delaloge S. A phase II study of TAS-117 in patients with advanced solid tumors harboring germline PTEN-inactivating mutations. Future Oncol. 2022 Sep;18(30):3377-3387. doi: 10.2217/fon-2022-0305. Epub 2022 Aug 30. PMID: 36039910; PMCID: PMC10334253.

2: Toson B, Fortes IS, Roesler R, Andrade SF. Targeting Akt/PKB in pediatric tumors: A review from preclinical to clinical trials. Pharmacol Res. 2022 Sep;183:106403. doi: 10.1016/j.phrs.2022.106403. Epub 2022 Aug 18. PMID: 35987481.

3: Mimura N. [Novel epigenetic therapies for multiple myeloma]. Rinsho Ketsueki. 2021;62(4):314-320. Japanese. doi: 10.11406/rinketsu.62.314. PMID: 33967157.

4: Lee JB, Jung M, Beom SH, Kim GM, Kim HR, Choi HJ, Sohn JH, Ahn JB, Rha SY, Chung HC. Phase 2 study of TAS-117, an allosteric akt inhibitor in advanced solid tumors harboring phosphatidylinositol 3-kinase/v-akt murine thymoma viral oncogene homolog gene mutations. Invest New Drugs. 2021 Oct;39(5):1366-1374. doi: 10.1007/s10637-021-01085-7. Epub 2021 Mar 15. PMID: 33723724; PMCID: PMC8426297.

5: Rizk M, Rizq O, Oshima M, Nakajima-Takagi Y, Koide S, Saraya A, Isshiki Y, Chiba T, Yamazaki S, Ma A, Jin J, Iwama A, Mimura N. Akt inhibition synergizes with polycomb repressive complex 2 inhibition in the treatment of multiple myeloma. Cancer Sci. 2019 Dec;110(12):3695-3707. doi: 10.1111/cas.14207. Epub 2019 Oct 22. PMID: 31571328; PMCID: PMC6890440.

6: Mimura N, Hideshima T, Shimomura T, Suzuki R, Ohguchi H, Rizq O, Kikuchi S, Yoshida Y, Cottini F, Jakubikova J, Cirstea D, Gorgun G, Minami J, Tai YT, Richardson PG, Utsugi T, Iwama A, Anderson KC. Selective and potent Akt inhibition triggers anti-myeloma activities and enhances fatal endoplasmic reticulum stress induced by proteasome inhibition. Cancer Res. 2014 Aug 15;74(16):4458-69. doi: 10.1158/0008-5472.CAN-13-3652. Epub 2014 Jun 16. PMID: 24934808; PMCID: PMC4140659.

7: Utsugi T. New challenges and inspired answers for anticancer drug discovery and development. Jpn J Clin Oncol. 2013 Oct;43(10):945-53. doi: 10.1093/jjco/hyt131. Epub 2013 Sep 5. PMID: 24014883; PMCID: PMC3787805.

Your view history

Pifusertib new featured