PT2399 | CAS#1672662-14-4 | HIF-2 inhibitor

PT2399
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 561185

CAS#: 1672662-14-4

Description: PT2399 is a first-in-class, orally available, small molecule inhibitor of HIF-2 that selectively disrupts the heterodimerization of HIF-2α with HIF-1β. Preclinical and clinical data indicate that PT2399 is effective in blocking cancer cell growth, proliferation, and tumor angiogenesis characteristic in ccRCC.

Chemical Structure

PT2399

CAS# 1672662-14-4

Instruction

Theoretical Analysis

MedKoo Cat#: 561185
Name: PT2399
CAS#: 1672662-14-4
Chemical Formula: C17H10F5NO4S
Exact Mass: 419.03
Molecular Weight: 419.322
Elemental Analysis: C, 48.69; H, 2.40; F, 22.65; N, 3.34; O, 15.26; S, 7.65

Price and Availability

Size	Price	Availability
25mg	USD 950	2 Weeks
50mg	USD 1650	2 Weeks
100mg	USD 2950	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: PT2399; PT-2399; PT 2399

IUPAC/Chemical Name: 3-[(1S)-7-(Difluoromethylsulfonyl)-2,2-difluoro-1-hydroxy-indan-4-yl]oxy-5-fluoro-benzonitrile

InChi Key: MXUSGDMIHGLCNC-HNNXBMFYSA-N

InChi Code: InChI=1S/C17H10F5NO4S/c18-9-3-8(7-23)4-10(5-9)27-12-1-2-13(28(25,26)16(19)20)14-11(12)6-17(21,22)15(14)24/h1-5,15-16,24H,6H2/t15-/m0/s1

SMILES Code: N#CC1=CC(F)=CC(OC2=CC=C(S(=O)(C(F)F)=O)C3=C2CC(F)(F)[C@H]3O)=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:

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 419.32 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:

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1: Chen W, Hill H, Christie A, Kim MS, Holloman E, Pavia-Jimenez A, Homayoun F, Ma Y, Patel N, Yell P, Hao G, Yousuf Q, Joyce A, Pedrosa I, Geiger H, Zhang H, Chang J, Gardner KH, Bruick RK, Reeves C, Hwang TH, Courtney K, Frenkel E, Sun X, Zojwalla N, Wong T, Rizzi JP, Wallace EM, Josey JA, Xie Y, Xie XJ, Kapur P, McKay RM, Brugarolas J. Targeting renal cell carcinoma with a HIF-2 antagonist. Nature. 2016 Nov 3;539(7627):112-117. doi: 10.1038/nature19796. Epub 2016 Sep 5. PubMed PMID: 27595394; PubMed Central PMCID: PMC5340502.

2: Martínez-Sáez O, Gajate Borau P, Alonso-Gordoa T, Molina-Cerrillo J, Grande E. Targeting HIF-2 α in clear cell renal cell carcinoma: A promising therapeutic strategy. Crit Rev Oncol Hematol. 2017 Mar;111:117-123. doi: 10.1016/j.critrevonc.2017.01.013. Epub 2017 Jan 28. Review. PubMed PMID: 28259286.

3: Cho H, Du X, Rizzi JP, Liberzon E, Chakraborty AA, Gao W, Carvo I, Signoretti S, Bruick RK, Josey JA, Wallace EM, Kaelin WG. On-target efficacy of a HIF-2α antagonist in preclinical kidney cancer models. Nature. 2016 Nov 3;539(7627):107-111. doi: 10.1038/nature19795. Epub 2016 Sep 5. PubMed PMID: 27595393; PubMed Central PMCID: PMC5499381.

4: Toledo RA. New HIF2A inhibitors: implications for pheochromocytomas and paragangliomas. Endocr Relat Cancer. 2017 Jun 30. pii: ERC-16-0479. doi: 10.1530/ERC-16-0479. [Epub ahead of print] PubMed PMID: 28667082.

5: Ricketts CJ, Crooks DR, Linehan WM. Targeting HIF2α in Clear-Cell Renal Cell Carcinoma. Cancer Cell. 2016 Oct 10;30(4):515-517. doi: 10.1016/j.ccell.2016.09.016. PubMed PMID: 27728802.

6: Cho H, Kaelin WG. Targeting HIF2 in Clear Cell Renal Cell Carcinoma. Cold Spring Harb Symp Quant Biol. 2016;81:113-121. doi: 10.1101/sqb.2016.81.030833. Epub 2016 Dec 8. PubMed PMID: 27932568.

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