Pralsetinib
Binding Mode- Product Name
- Pralsetinib
- CAS No.
- 2097132-94-8
- Chemical Name
- Pralsetinib
- Synonyms
- PRALSETINIB;BLU-667;Rralsetinib;CPD2049;BLU-667-API;PRALSETINIB (BLU667);Pralsetinib Impurity;BLU-667 (Pralsetinib);Pralsetinib Monohydrate;Pralsetinib, 10 mM in DMSO
- CBNumber
- CB04632289
- Molecular Formula
- C27H32FN9O2
- Formula Weight
- 533.6
- MOL File
- 2097132-94-8.mol
Pralsetinib Property
- Boiling point:
- 799.1±60.0 °C(Predicted)
- Density
- 1.40±0.1 g/cm3(Predicted)
- storage temp.
- Store at 4°C
- solubility
- DMSO : ≥ 100 mg/mL (187.41 mM);Water : < 0.1 mg/mL (insoluble)
- form
- Solid
- pka
- 14.33±0.10(Predicted)
- color
- White to off-white
- InChIKey
- GBLBJPZSROAGMF-BATDWUPUSA-N
- SMILES
- [C@]1(OC)(C(N[C@H](C2=CC=C(N3C=C(F)C=N3)N=C2)C)=O)CC[C@H](C2=NC(NC3C=C(C)NN=3)=CC(C)=N2)CC1
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-0044766
- Product name
- Pralsetinib
- Purity
- 99.56%
- Packaging
- 2mg
- Price
- $65
- Updated
- 2021/12/16
- Product number
- CS-0044766
- Product name
- Pralsetinib
- Purity
- 99.56%
- Packaging
- 5mg
- Price
- $130
- Updated
- 2021/12/16
- Product number
- CS-0044766
- Product name
- Pralsetinib
- Purity
- 99.56%
- Packaging
- 10mg
- Price
- $185
- Updated
- 2021/12/16
- Product number
- INB0009818
- Product name
- PRALSETINIB
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $454.91
- Updated
- 2021/12/16
- Product number
- CS-0044766
- Product name
- Pralsetinib
- Purity
- 99.56%
- Packaging
- 50mg
- Price
- $685
- Updated
- 2021/12/16
Pralsetinib Chemical Properties,Usage,Production
Binding Mode
In the co-crystal structure of pralsetinib in
complex with RET kinase (Fig. 1), the
aminopyrimidinyl and methylaminopyrazolyl
subunits fit into the adenosine pocket, forming three
critical hydrogen bonds with hinge residues Ala807
and Glu805. In addition, one pyrimidine nitrogen,
methoxy oxygen, and one fluoropyrazole nitrogen
also interact with the kinase residues indirectly via
three bound water molecules (Fig. 2).
Description
Pralsetinib is a potent, selective RET inhibitor, and was optimized from a hit compound identified from a compound library that included more than 60 chemical scaffolds. However, as of 2020, detailed medicinal chemistry on the optimization process has yet to be published. Pralsetinib proved to be more potent and selective than cabozantinib or vandertanib against both wild-type and abnormal RET. The agent also showed a level of selectivity against RET relative to VEGFR2, whereas previous agents showed very little selectivity. On September 4, 2020, the Food and Drug Administration granted accelerated approval to pralsetinib (GAVRETO®, Blueprint Medicines Corporation) for adult patients with metastatic RET fusion-positive non-small cell lung cancer (NSCLC) as detected by an FDA-approved test.
Uses
Pralsetinib is a highly potent and selective RET inhibitor designed for RET-driven cancers.
Indications
Pralsetinib is the second selective RET inhibitor approved by the FDA (following Lilly's selpercatinib) for the treatment of adult patients with metastatic RET (rearranged during transfection) fusion-positive non-small cell lung cancer (NSCLC); (2) adult and pediatric patients >=12 years of age with advanced or metastatic RET-mutant medullary thyroid cancer (MTC) who require systemic therapy; and (3) adult and pediatric patients >=12 years of age with advanced or metastatic RET fusion-positive thyroid cancer who require systemic therapy and who are radioactive iodine-refractory.
brand name
Gavreto
Synthesis Reference(s)
[1] GAIKWAD RAJENDRA. Green One-Pot Chemo-Enzymatic Synthesis of a Key Chiral Amine Intermediate: Useful to Pralsetinib Synthesis[J]. ChemistrySelect, 2023. DOI:10.1002/slct.202204409.
[2] HUGHES* D L. Review of Synthetic Routes and Crystalline Forms of the Oncology Drugs Capmatinib, Selpercatinib, and Pralsetinib[J]. Organic Process Research & Development, 2021. DOI:10.1021/acs.oprd.1c00282.
General Description
Class: receptor tyrosine kinase; Treatment: RET-altered lung, thyroid cancers; Other name: BLU-667; Elimination half-life = 22 h; Protein binding = 97%
Side effects
Pralsetinib may cause side effects: Nausea, vomiting, loss of appetite, diarrhea, constipation, extreme tiredness, dizziness, weakness, night sweats, rapid heartbeat, heartburn, shortness of breath, headache, sores in the mouth, confusion, changes in vision, fever, cough, chills, nosebleeds, pale skin, rash, itching, hives, weight changes, hair loss, back pain, muscle pain, joint pain, bone pain, unusual bruising or bleeding, blood in the urine or stool, bloody or black tarry stools, difficulty falling asleep or staying asleep, unusual vaginal bleeding, and other less common effects.
Synthesis
Commercially available bromopyridine 291 was coupled with boronate 292 under Suzuki conditions to generate ketal 293. Ketal 293 was converted to chemicalbook ketone 294 after acidification. Under Takenori homologation conditions, the quaternary carbon center in 295 was established. It was then coupled with amine 296 to finally afford pralsetinib.
target
Primary target: RET
Mode of action
Kinase inhibitor of wild-type RET, oncogenic RET fusions, and select mutations. Pralsetinib may also inhibit other pathways including those through FLT3, JAK1-2, PDGFRB, VEGFR-2, and FGFR1. RET fusion proteins and activating point mutations can act as oncogenic drivers by promoting cell proliferation of tumor cell lines and pralsetinib inhibits this process.
Pralsetinib Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Pralsetinib manufacturers
- Product
- Pralsetinib Impurity 2097132-94-8
- Price
- US $0.00-0.00/mg
- Min. Order
- 10mg
- Purity
- 98
- Supply Ability
- 10000000
- Release date
- 2025-02-20
- Product
- Pralsetinib Monohydrate 2097132-94-8
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- More Than 99%
- Supply Ability
- 100kg/Month
- Release date
- 2024-07-24
- Product
- Pralsetinib Blu-667 2097132-94-8
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- More Than 99%
- Supply Ability
- 100kg/Month
- Release date
- 2024-12-30