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MedKoo Cat#: 206980 | Name: Pralsetinib HCl

Description:

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

Pralsetinib, also known as BLU-667, is a highly potent, selective, next generation RET inhibitor with IC50 of 0.3-0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion.. BLU-667 is a potent and selective inhibitor of RET mutations, fusions, and predicted resistant mutants. RET fusions are key drivers of multiple cancers, including lung and thyroid cancer, and our research suggests that RET also plays a key role in some colon and breast cancers. By simultaneously targeting the primary driver and predicted resistant mutants that render cancer cells insensitive to treatment with currently approved drugs,

Chemical Structure

Pralsetinib HCl
Pralsetinib HCl
CAS#Pralsetinib HCl

Theoretical Analysis

MedKoo Cat#: 206980

Name: Pralsetinib HCl

CAS#: Pralsetinib HCl

Chemical Formula: C27H33ClFN9O2

Exact Mass: 532.2711

Molecular Weight: 570.07

Elemental Analysis: C, 56.89; H, 5.84; Cl, 6.22; F, 3.33; N, 22.11; O, 5.61

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 #
2097132-94-8 (free base) 2097132-93-7 (trans-isomer) Pralsetinib HCl
Synonym
BLU-667; BLU 667; BLU667; Pralsetinib HCl; Pralsetinib hydrochloride
IUPAC/Chemical Name
(1s,4R)-N-((S)-1-(4-(4-fluoro-1H-pyrazol-1-yl)phenyl)ethyl)-1-methoxy-4-(4-methyl-6-((5-methyl-1H-pyrazol-3-yl)amino)pyrimidin-2-yl)cyclohexane-1-carboxamide hydrochloride
InChi Key
CCYKAXKRSKSMNX-MJFWUJRASA-N
InChi Code
InChI=1S/C27H32FN9O2.ClH/c1-16-11-22(33-23-12-17(2)35-36-23)34-25(31-16)19-7-9-27(39-4,10-8-19)26(38)32-18(3)20-5-6-24(29-13-20)37-15-21(28)14-30-37;/h5-6,11-15,18-19H,7-10H2,1-4H3,(H,32,38)(H2,31,33,34,35,36);1H/t18-,19-,27-;/m0./s1
SMILES Code
O=C([C@@]1(OC)CC[C@@H](C2=NC(NC3=NNC(C)=C3)=CC(C)=N2)CC1)N[C@H](C4=CC=C(N5N=CC(F)=C5)N=C4)C.[H]Cl
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 570.07 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: Monaca F, Vita E, Lococo F, Tortora G, Bria E. Lazarus Response to Selpercatinib for Bleeding Colic Metastasis in a Patient With RET Fusion- Positive Pulmonary Sarcomatoid Carcinoma: A Case Report. Cureus. 2024 Jul 23;16(7):e65186. doi: 10.7759/cureus.65186. PMID: 39176355; PMCID: PMC11340252. 2: Poumeaud F, Jaffrelot M, Gomez-Roca C, Korakis I, Leonardi G, Joly M, Mazières J, Guimbaud R, Fares N, Alouani E. A double-edged sword: unusual multiple severe infections with pralsetinib: a case report and literature review. Front Med (Lausanne). 2024 Jul 30;11:1402902. doi: 10.3389/fmed.2024.1402902. PMID: 39139787; PMCID: PMC11319124. 3: Hou Y, Ren X, Chen Y, Wang Y. Cardiovascular toxicities of selective ret- specific tyrosine kinase inhibitors: a pharmacovigilance study based on the United States Food and Drug Administration Adverse Event Reporting System database. Expert Opin Drug Saf. 2024 Aug 19:1-9. doi: 10.1080/14740338.2024.2392003. Epub ahead of print. PMID: 39137926. 4: Kojima A, Nadai M, Murayama N, Yamazaki H, Katoh M. Effects of tyrosine kinase inhibitors used for the treatment of non-small cell lung carcinoma on cytochrome P450 2J2 activities. Xenobiotica. 2024 Aug 12:1-6. doi: 10.1080/00498254.2024.2389401. Epub ahead of print. PMID: 39105612. 5: Chang Z, Zhu T, Jiang H, Ou W, Wang S. A Locally Advanced NSCLC Patient Harboring a Rare KIF13A-RET Fusion Benefited from Pralsetinib: A Case Report. Curr Oncol. 2024 Jun 30;31(7):3808-3814. doi: 10.3390/curroncol31070281. PMID: 39057153; PMCID: PMC11275379. 6: Dolton MJ, Bowman C, Ma F, Cheeti S, Kuruvilla D, Kassir N, Chen Y, Liu J, Chiang PC. Integrating Dynamic in vitro Systems and Mechanistic Absorption Modeling: Case Study of Pralsetinib. J Pharm Sci. 2024 Jul 26:S0022-3549(24)00252-1. doi: 10.1016/j.xphs.2024.07.006. Epub ahead of print. PMID: 39002726. 7: Chen MF, Repetto M, Wilhelm C, Drilon A. RET Inhibitors in RET Fusion- Positive Lung Cancers: Past, Present, and Future. Drugs. 2024 Jul 13. doi: 10.1007/s40265-024-02040-5. Epub ahead of print. PMID: 38997570. 8: Velasquez E, Kassir N, Cheeti S, Kuruvilla D, Sane R, Dang S, Miles D, Lu J. Predicting overall survival from tumor dynamics metrics using parametric statistical and machine learning models: application to patients with RET-altered solid tumors. Front Artif Intell. 2024 Jun 11;7:1412865. doi: 10.3389/frai.2024.1412865. PMID: 38919267; PMCID: PMC11196751. 9: Lee ATM, Ou SI. LIBRETTO-431: Confirming the Superiority of Selpercatinib to Chemotherapy and the Lack of Efficacy of Immune Checkpoint Inhibitors in Advanced RET Fusion-Positive (RET+) NSCLC, Another Unique Never- Smoker Predominant Molecular Subtype of NSCLC. Lung Cancer (Auckl). 2024 May 23;15:75-80. doi: 10.2147/LCTT.S460147. PMID: 38807655; PMCID: PMC11130712. 10: Suchomel J, Agarwal P, Anders D, Hughes K, Tang Y, Sane R, Scalori A, Sharma S, Cheeti S. Impact of P-gp inhibition on systemic exposure of pralsetinib and dosing considerations. Clin Transl Sci. 2024 Jun;17(6):e13818. doi: 10.1111/cts.13818. PMID: 38807449; PMCID: PMC11133961. 11: Mehdi M, Szabo A, Shreenivas A, Thomas JP, Tsai S, Christians KK, Evans DB, Clarke CN, Hall WA, Erickson B, Ahmed G, Thapa B, McFall T, George B, Kurzrock R, Kamgar M. Chemotherapy-free treatment targeting fusions and driver mutations in KRAS wild-type pancreatic ductal adenocarcinoma, a case series. Ther Adv Med Oncol. 2024 May 19;16:17588359241253113. doi: 10.1177/17588359241253113. PMID: 38770091; PMCID: PMC11104030. 12: Acharya B, Saha D, Garcia Garcia N, Armstrong D, Jabali B, Hanafi M, Frett B, Ryan KR. Discovery of 9H-pyrimido[4,5-b]indole derivatives as dual RET/TRKA inhibitors. Bioorg Med Chem. 2024 May 15;106:117749. doi: 10.1016/j.bmc.2024.117749. Epub 2024 May 9. PMID: 38744018; PMCID: PMC11144469. 13: Yan H, Zeng L, Zhang Y. RET rearrangement as a mechanism of resistance to ALK-TKI in non-small cell lung cancer patient with EML4-ALK fusion: A case report. Heliyon. 2024 Apr 22;10(9):e29928. doi: 10.1016/j.heliyon.2024.e29928. PMID: 38698976; PMCID: PMC11064130. 14: Barsouk A, Elghawy O, Stone S, Singh A. Patient with mediastinal carcinoma of unknown primary with RET fusion achieves durable response with RET inhibition. Anticancer Drugs. 2024 Aug 1;35(7):653-657. doi: 10.1097/CAD.0000000000001618. Epub 2024 Apr 29. PMID: 38696710. 15: Jara MA. Management of Advanced Medullary Thyroid Carcinoma: Current Systemic Therapy Options. Crit Rev Oncog. 2024;29(3):83-90. doi: 10.1615/CritRevOncog.2024051588. PMID: 38683155. 16: Cheung KWK, Tang Y, Anders D, Barata T, Scalori A, Agarwal P, Sane R, Cheeti S. Exploring the Impact of Hepatic Impairment on Pralsetinib Pharmacokinetics. Pharmaceutics. 2024 Apr 20;16(4):564. doi: 10.3390/pharmaceutics16040564. PMID: 38675225; PMCID: PMC11053887. 17: Correction to: Pralsetinib in Patients with Advanced/Metastatic Rearranged During Transfection (RET)-Altered Thyroid Cancer: Updated Efficacy and Safety Data from the ARROW Study'' by Subbiah et al. Thyroid 2024;34(1):26-40; doi: 10.1089/thy.2023.0363. Thyroid. 2024 Apr 16. doi: 10.1089/thy.2023.0363.correx. Epub ahead of print. Erratum for: Thyroid. 2024 Jan;34(1):26-40. doi: 10.1089/thy.2023.0363. PMID: 38625021. 18: Zhao Z, Pu Q, Sun T, Huang Q, Tong L, Fan T, Kang J, Chen Y, Zhang Y. Determination of Pralsetinib in Human Plasma and Cerebrospinal Fluid for Therapeutic Drug Monitoring by Ultra-performance Liquid Chromatography-Tandem Mass Spectrometry (UPLC-MS/MS). Anticancer Agents Med Chem. 2024;24(11):867-877. doi: 10.2174/0118715206290110240326071909. PMID: 38584556. 19: Nishikawa G, Klein MA. Targeting RET alterations in non-small cell lung cancer. Curr Probl Cancer. 2024 Apr;49:101074. doi: 10.1016/j.currproblcancer.2024.101074. Epub 2024 Mar 16. PMID: 38494387. 20: Bowman C, Dolton M, Ma F, Cheeti S, Kuruvilla D, Sane R, Kassir N, Chen Y. Understanding CYP3A4 and P-gp mediated drug-drug interactions through PBPK modeling - Case example of pralsetinib. CPT Pharmacometrics Syst Pharmacol. 2024 Apr;13(4):660-672. doi: 10.1002/psp4.13114. Epub 2024 Mar 13. PMID: 38481038; PMCID: PMC11015073.

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