MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 561185 | Name: PT2399
Featured New

Description:

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

PT2399 is a selective antagonist of hypoxia-inducible factor 2α (HIF-2α) that has been studied for its potential anticancer effects, particularly in clear cell renal cell carcinoma (ccRCC). In vitro studies demonstrate that PT2399 effectively disrupts HIF-2α heterodimerization with ARNT, leading to reduced transcription of HIF-2α target genes, including VEGF and cyclin D1. This inhibition results in decreased cell proliferation and increased apoptosis in ccRCC cell lines that are dependent on HIF-2α signaling. Notably, PT2399 exhibits selectivity for HIF-2α over HIF-1α, minimizing off-target effects

Chemical Structure

PT2399
PT2399
CAS#1672662-14-4

Theoretical Analysis

MedKoo Cat#: 561185

Name: PT2399

CAS#: 1672662-14-4

Chemical Formula: C17H10F5NO4S

Exact Mass: 419.0251

Molecular Weight: 419.32

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 Quantity
25mg USD 950.00 2 Weeks
50mg USD 1,650.00 2 Weeks
100mg USD 2,950.00 2 Weeks
Bulk Inquiry
Buy Now
Add to Cart
Related CAS #
No Data
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

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.

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: Mello RM, Ceballos DG, Sandate CR, Agudelo D, Jouffe C, Uhlenhaut NH, Thomä NH, Simon MC, Lamia KA. BMAL1-HIF2α heterodimers contribute to ccRCC. Res Sq [Preprint]. 2024 Jul 16:rs.3.rs-4651047. doi: 10.21203/rs.3.rs-4651047/v1. PMID: 39070610; PMCID: PMC11275985. 2: Mello RM, Ceballos DG, Sandate CR, Agudelo D, Jouffe C, Uhlenhaut NH, Thomä NH, Simon MC, Lamia KA. BMAL1-HIF2α heterodimers contribute to ccRCC. bioRxiv [Preprint]. 2024 Jun 9:2024.06.07.597806. doi: 10.1101/2024.06.07.597806. PMID: 38895384; PMCID: PMC11185709. 3: Wang J, Ma W, Huang J, Qiu G, Zhang T, Wei Q, He C, Zhou D, Zhao M, Chen C, Xu X. HIF-2α inhibition disrupts leukemia stem cell metabolism and impairs vascular microenvironment to enhance chronic myeloid leukemia treatment. Cancer Lett. 2024 Aug 10;597:217060. doi: 10.1016/j.canlet.2024.217060. Epub 2024 Jun 14. PMID: 38880225. 4: Wang LL, Lu ZJ, Luo SK, Li Y, Yang Z, Lu HY. Unveiling the role of hypoxia- inducible factor 2alpha in osteoporosis: Implications for bone health. World J Stem Cells. 2024 Apr 26;16(4):389-409. doi: 10.4252/wjsc.v16.i4.389. PMID: 38690514; PMCID: PMC11056635. 5: Li Z, Zhang W, Huang S, Dai Z, Liang J, Qiu Q, Chen S, Guo W, Wang Z, Wei J. Poly-3-hydroxybutyrate-co-3-hydroxyvalerate(PHBV)-Polyethylene glycol 20k(PEG20k) as a promising delivery system for PT2399 in the treatment of disc degeneration. J Biol Eng. 2024 Jan 22;18(1):11. doi: 10.1186/s13036-024-00407-6. PMID: 38254196; PMCID: PMC10804636. 6: Guo W, Hoque J, Garcia Garcia CJ, Spiller KV, Leinroth AP, Puviindran V, Potnis CK, Gunn KA, Newman H, Ishikawa K, Fujimoto TN, Neill DW, Delahoussaye AM, Williams NT, Kirsch DG, Hilton MJ, Varghese S, Taniguchi CM, Wu C. Radiation-induced bone loss in mice is ameliorated by inhibition of HIF-2α in skeletal progenitor cells. Sci Transl Med. 2023 Nov 29;15(724):eabo5217. doi: 10.1126/scitranslmed.abo5217. Epub 2023 Nov 29. PMID: 38019933; PMCID: PMC10804914. 7: Ma Y, Joyce A, Brandenburg O, Saatchi F, Stevens C, Toffessi Tcheuyap V, Christie A, Do QN, Fatunde O, Macchiaroli A, Wong SC, Woolford L, Yousuf Q, Miyata J, Carrillo D, Onabolu O, McKenzie T, Mishra A, Hardy T, He W, Li D, Ivanishev A, Zhang Q, Pedrosa I, Kapur P, Schluep T, Kanner SB, Hamilton J, Brugarolas J. HIF2 Inactivation and Tumor Suppression with a Tumor-Directed RNA- Silencing Drug in Mice and Humans. Clin Cancer Res. 2022 Dec 15;28(24):5405-5418. doi: 10.1158/1078-0432.CCR-22-0963. PMID: 36190432; PMCID: PMC9771962. 8: Yang Z, Li T, Xian J, Chen J, Huang Y, Zhang Q, Lin X, Lu H, Lin Y. SGLT2 inhibitor dapagliflozin attenuates cardiac fibrosis and inflammation by reverting the HIF-2α signaling pathway in arrhythmogenic cardiomyopathy. FASEB J. 2022 Jul;36(7):e22410. doi: 10.1096/fj.202200243R. Erratum in: FASEB J. 2022 Sep;36(9):e22503. doi: 10.1096/fsb2.22503. PMID: 35713937. 9: Qin L, Chung YM, Berk M, Naelitz B, Zhu Z, Klein E, Chakraborty AA, Sharifi N. Hypoxia-Reoxygenation Couples 3βHSD1 Enzyme and Cofactor Upregulation to Facilitate Androgen Biosynthesis and Hormone Therapy Resistance in Prostate Cancer. Cancer Res. 2022 Jul 5;82(13):2417-2430. doi: 10.1158/0008-5472.CAN-21-4256. PMID: 35536859; PMCID: PMC9256813. 10: Stransky LA, Vigeant SM, Huang B, West D, Denize T, Walton E, Signoretti S, Kaelin WG Jr. Sensitivity of VHL mutant kidney cancers to HIF2 inhibitors does not require an intact p53 pathway. Proc Natl Acad Sci U S A. 2022 Apr 5;119(14):e2120403119. doi: 10.1073/pnas.2120403119. Epub 2022 Mar 31. PMID: 35357972; PMCID: PMC9168943. 11: Garcia Garcia CJ, Huang Y, Fuentes NR, Turner MC, Monberg ME, Lin D, Nguyen ND, Fujimoto TN, Zhao J, Lee JJ, Bernard V, Yu M, Delahoussaye AM, Jimenez Sacarello I, Caggiano EG, Phan JL, Deorukhkar A, Molkentine JM, Saur D, Maitra A, Taniguchi CM. Stromal HIF2 Regulates Immune Suppression in the Pancreatic Cancer Microenvironment. Gastroenterology. 2022 Jun;162(7):2018-2031. doi: 10.1053/j.gastro.2022.02.024. Epub 2022 Feb 22. PMID: 35216965; PMCID: PMC9278556. 12: Hoefflin R, Harlander S, Abhari BA, Peighambari A, Adlesic M, Seidel P, Zodel K, Haug S, Göcmen B, Li Y, Lahrmann B, Grabe N, Heide D, Boerries M, Köttgen A, Heikenwalder M, Frew IJ. Therapeutic Effects of Inhibition of Sphingosine-1-Phosphate Signaling in HIF-2α Inhibitor-Resistant Clear Cell Renal Cell Carcinoma. Cancers (Basel). 2021 Sep 25;13(19):4801. doi: 10.3390/cancers13194801. PMID: 34638286; PMCID: PMC8508537. 13: Guo S, Zhang D, Lu X, Zhang Q, Gu R, Sun B, Sun Y. Hypoxia and its possible relationship with endometrial receptivity in adenomyosis: a preliminary study. Reprod Biol Endocrinol. 2021 Jan 8;19(1):7. doi: 10.1186/s12958-020-00692-y. PMID: 33419445; PMCID: PMC7791798. 14: Nicholson HE, Tariq Z, Housden BE, Jennings RB, Stransky LA, Perrimon N, Signoretti S, Kaelin WG Jr. HIF-independent synthetic lethality between CDK4/6 inhibition and VHL loss across species. Sci Signal. 2019 Oct 1;12(601):eaay0482. doi: 10.1126/scisignal.aay0482. PMID: 31575731; PMCID: PMC6913182. 15: Feng Z, Zou X, Chen Y, Wang H, Duan Y, Bruick RK. Modulation of HIF-2α PAS-B domain contributes to physiological responses. Proc Natl Acad Sci U S A. 2018 Dec 26;115(52):13240-13245. doi: 10.1073/pnas.1810897115. Epub 2018 Dec 6. PMID: 30523118; PMCID: PMC6310796. 16: Sun DR, Wang ZJ, Zheng QC, Zhang HX. Exploring the inhibition mechanism on HIF-2 by inhibitor PT2399 and 0X3 using molecular dynamics simulations. J Mol Recognit. 2018 Oct;31(10):e2730. doi: 10.1002/jmr.2730. Epub 2018 May 23. PMID: 29797434. 17: Yoshino H, Nohata N, Miyamoto K, Yonemori M, Sakaguchi T, Sugita S, Itesako T, Kofuji S, Nakagawa M, Dahiya R, Enokida H. PHGDH as a Key Enzyme for Serine Biosynthesis in HIF2α-Targeting Therapy for Renal Cell Carcinoma. Cancer Res. 2017 Nov 15;77(22):6321-6329. doi: 10.1158/0008-5472.CAN-17-1589. Epub 2017 Sep 26. PMID: 28951458; PMCID: PMC5893502. 18: Tella SH, Taïeb D, Pacak K. HIF-2alpha: Achilles' heel of pseudohypoxic subtype paraganglioma and other related conditions. Eur J Cancer. 2017 Nov;86:1-4. doi: 10.1016/j.ejca.2017.08.023. Epub 2017 Sep 22. PMID: 28946040; PMCID: PMC6287501. 19: Toledo RA. New HIF2α inhibitors: potential implications as therapeutics for advanced pheochromocytomas and paragangliomas. Endocr Relat Cancer. 2017 Sep;24(9):C9-C19. doi: 10.1530/ERC-16-0479. Epub 2017 Jun 30. PMID: 28667082. 20: 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. PMID: 28259286.