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MedKoo Cat#: 126081 | Name: Bimiralisib hydrochloride

Description:

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

Bimiralisib, also known as PQR309, is an orally bioavailable pan inhibitor of phosphoinositide-3-kinases (PI3K) and inhibitor of the mammalian target of rapamycin (mTOR), with potential antineoplastic activity.

Chemical Structure

Bimiralisib hydrochloride
Bimiralisib hydrochloride
CAS#1820902-72-4 (HCl)

Theoretical Analysis

MedKoo Cat#: 126081

Name: Bimiralisib hydrochloride

CAS#: 1820902-72-4 (HCl)

Chemical Formula: C17H21ClF3N7O2

Exact Mass: 447.1397

Molecular Weight: 447.85

Elemental Analysis: C, 45.59; H, 4.73; Cl, 7.92; F, 12.73; N, 21.89; O, 7.14

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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Related CAS #
1225037-39-7 (free base) 1820902-72-4 (HCl) 1820902-73-5 (HCl hydrate)
Synonym
Bimiralisib hydrochloride; PQR309; PQR-309; PQR309; Bimiralisib
IUPAC/Chemical Name
5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine hydrochloride
InChi Key
VNBNQGZQKUMKAL-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H20F3N7O2.ClH/c18-17(19,20)12-9-13(21)22-10-11(12)14-23-15(26-1-5-28-6-2-26)25-16(24-14)27-3-7-29-8-4-27;/h9-10H,1-8H2,(H2,21,22);1H
SMILES Code
Cl.NC1=CC(=C(C=N1)C2=NC(=NC(=N2)N3CCOCC3)N4CCOCC4)C(F)(F)F
Appearance
To be determined
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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 447.85 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: Wind SS, Jansen MAA, Rijsbergen M, van Esdonk MJ, Ziagkos D, Cheng WC, Niemeyer-van der Kolk T, Korsten J, Gruszka A, Schmitz-Rohmer D, Bonnel D, Legouffe R, Barré F, Bekkenk MW, de Haas ERM, Quint KD, Rolli M, Streefkerk HJ, Burggraaf J, Vermeer MH, Rissmann R. Topical Bimiralisib Shows Meaningful Cutaneous Drug Levels in Healthy Volunteers and Mycosis Fungoides Patients but No Clinical Activity in a First-in-Human, Randomized Controlled Trial. Cancers (Basel). 2022 Mar 15;14(6):1510. doi: 10.3390/cancers14061510. Erratum in: Cancers (Basel). 2023 Feb 27;15(5): PMID: 35326659; PMCID: PMC8946662. 2: Johnson FM, Janku F, Gouda MA, Tran HT, Kawedia JD, Schmitz D, Streefkerk H, Lee JJ, Andersen CR, Deng D, Rawal S, Shah PA, El-Naggar AK, Johnson JM, Frederick MJ. Inhibition of the Phosphatidylinositol-3 Kinase Pathway Using Bimiralisib in Loss-of-Function NOTCH1-Mutant Head and Neck Cancer. Oncologist. 2022 Dec 9;27(12):1004-e926. doi: 10.1093/oncolo/oyac185. PMID: 36124629; PMCID: PMC9732253. 3: Seipel K, Brügger Y, Mandhair H, Bacher U, Pabst T. Rationale for Combining the BCL2 Inhibitor Venetoclax with the PI3K Inhibitor Bimiralisib in the Treatment of IDH2- and FLT3-Mutated Acute Myeloid Leukemia. Int J Mol Sci. 2022 Oct 20;23(20):12587. doi: 10.3390/ijms232012587. PMID: 36293442; PMCID: PMC9604078. 4: Hsin IL, Shen HP, Chang HY, Ko JL, Wang PH. Suppression of PI3K/Akt/mTOR/c-Myc/mtp53 Positive Feedback Loop Induces Cell Cycle Arrest by Dual PI3K/mTOR Inhibitor PQR309 in Endometrial Cancer Cell Lines. Cells. 2021 Oct 27;10(11):2916. doi: 10.3390/cells10112916. PMID: 34831139; PMCID: PMC8616154. 5: Collins GP, Eyre TA, Schmitz-Rohmer D, Townsend W, Popat R, Giulino-Roth L, Fields PA, Krasniqi F, Soussain C, Stathis A, Andjelkovic N, Cunningham D, Mandic D, Radulovic S, Tijanic I, Horowitz NA, Kurtovic S, Schorb E, Schmidt C, Dimitrijević S, Dreyling M. A Phase II Study to Assess the Safety and Efficacy of the Dual mTORC1/2 and PI3K Inhibitor Bimiralisib (PQR309) in Relapsed, Refractory Lymphoma. Hemasphere. 2021 Oct 27;5(11):e656. doi: 10.1097/HS9.0000000000000656. PMID: 34901759; PMCID: PMC8660000. 6: Munz N, Cascione L, Parmigiani L, Tarantelli C, Rinaldi A, Cmiljanovic N, Cmiljanovic V, Giugno R, Bertoni F, Napoli S. Exon-Intron Differential Analysis Reveals the Role of Competing Endogenous RNAs in Post-Transcriptional Regulation of Translation. Noncoding RNA. 2021 Apr 16;7(2):26. doi: 10.3390/ncrna7020026. PMID: 33923420; PMCID: PMC8167571. 7: Wind SS, Jansen MAA, Rijsbergen M, van Esdonk MJ, Ziagkos D, Cheng WC, Niemeyer-van der Kolk T, Korsten J, Gruszka A, Schmitz-Rohmer D, Bonnel D, Legouffe R, Barré F, Bekkenk MW, de Haas ERM, Quint KD, Schnidar H, Rolli M, Streefkerk HJ, Burggraaf J, Vermeer MH, Rissmann R. Correction: Wind et al. Topical Bimiralisib Shows Meaningful Cutaneous Drug Levels in Healthy Volunteers and Mycosis Fungoides Patients but No Clinical Activity in a First-in-Human, Randomized Controlled Trial. Cancers 2022, 14, 1510. Cancers (Basel). 2023 Feb 27;15(5):1485. doi: 10.3390/cancers15051485. Erratum for: Cancers (Basel). 2022 Mar 15;14(6): PMID: 36900424; PMCID: PMC10001047. 8: Tarantelli C, Gaudio E, Arribas AJ, Kwee I, Hillmann P, Rinaldi A, Cascione L, Spriano F, Bernasconi E, Guidetti F, Carrassa L, Pittau RB, Beaufils F, Ritschard R, Rageot D, Sele A, Dossena B, Rossi FM, Zucchetto A, Taborelli M, Gattei V, Rossi D, Stathis A, Stussi G, Broggini M, Wymann MP, Wicki A, Zucca E, Cmiljanovic V, Fabbro D, Bertoni F. PQR309 Is a Novel Dual PI3K/mTOR Inhibitor with Preclinical Antitumor Activity in Lymphomas as a Single Agent and in Combination Therapy. Clin Cancer Res. 2018 Jan 1;24(1):120-129. doi: 10.1158/1078-0432.CCR-17-1041. Epub 2017 Oct 24. PMID: 29066507. 9: Beaufils F, Cmiljanovic N, Cmiljanovic V, Bohnacker T, Melone A, Marone R, Jackson E, Zhang X, Sele A, Borsari C, Mestan J, Hebeisen P, Hillmann P, Giese B, Zvelebil M, Fabbro D, Williams RL, Rageot D, Wymann MP. 5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology. J Med Chem. 2017 Sep 14;60(17):7524-7538. doi: 10.1021/acs.jmedchem.7b00930. Epub 2017 Sep 1. PMID: 28829592; PMCID: PMC5656176. 10: Choo F, Odintsov I, Nusser K, Nicholson KS, Davis L, Corless CL, Stork L, Somwar R, Ladanyi M, Davis JL, Davare MA. Functional impact and targetability of PI3KCA, GNAS, and PTEN mutations in a spindle cell rhabdomyosarcoma with MYOD1 L122R mutation. Cold Spring Harb Mol Case Stud. 2022 Jan 10;8(1):a006140. doi: 10.1101/mcs.a006140. Erratum in: Cold Spring Harb Mol Case Stud. 2022 Apr 28;8(3): PMID: 35012940; PMCID: PMC8744497.

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