Pralsetinib (BLU-667) - Moligand™, 10mM in DMSO , Inhibitor of kinase insert domain receptor;Inhibitor of ret proto-oncogene, CAS No.2097132-94-8, Inhibitor of kinase insert domain receptor;Inhibitor of ret proto-oncogene

CAS: 2097132-94-8 Cat. No.: P408403 분자식: C₂₇H₃₂FN₉O₂ 분자량: 533.6 EC 번호: 861-037-3 PubChem CID: 129073603

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

CS 3009, Gavreto | Cyclohexanecarboxami​de, N-​[(1S)​-​1-​[6-​(4-​fluoro-​1H-​pyrazol-​1-​yl)​-​3-​pyridinyl]​ethyl]​-​1-​methoxy-​4-​[4-​methyl-​6-​[(5-​methyl-​1H-​pyrazol-​3-​yl)​amino]​-​2-​pyrimidinyl]​-​, cis-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

개요

Information

Pralsetinib (BLU-667) Pralsetinib (BLU-667, CS 3009, Gavreto) is a highly potent and selective RET (c-RET) inhibitor with an IC50 of 0.4 nM for WT RET. It also demonstrates potent activity (IC50 0.4 nmol/L) against common oncogenic RET alterations, incl
In vitro

BLU-667 is at least 100-fold more selective for RET over 96% of kinases tested (a panel of 371 kinases). BLU-667 specifically abrogates RET signaling in RET-altered cancers from diverse lineages. RET pathway inhibition with BLU-667 also more potently inhibits proliferation of RET-altered cell lines relative to multikinase inhibitors.

In vivo

In vivo, BLU-667 potently inhibits growth of NSCLC and thyroid cancer xenografts driven by various RET mutations and fusions without inhibiting VEGFR2. BLU-667 is well tolerated throughout the in vivo studies.
Cell Data

cell lines：

Concentrations：0-1 μM

Incubation Time：90 minutes

Powder Purity:≥98%

Specifications

동의어

CS 3009, Gavreto | Cyclohexanecarboxami​de, N-​[(1S)​-​1-​[6-​(4-​fluoro-​1H-​pyrazol-​1-​yl)​-​3-​pyridinyl]​ethyl]​-​1-​methoxy-​4-​[4-​methyl-​6-​[(5-​methyl-​1H-​pyrazol-​3-​yl)​amino]​-​2-​pyrimidinyl]​-​, cis-

사양 및 순도

Moligand™, 10mM in DMSO

생화학 및 생리적 메커니즘

Pralsetinib (BLU-667, CS 3009, Gavreto) is a highly potent and selective RET (c-RET) inhibitor with an IC50 of 0.4 nM for WT RET. It also demonstrates potent activity (IC50 0.4 nmol/L) against common oncogenic RET alterations, including RET (M918T).

보관 조건

Store at -80°C

배송

Dry ice packs + Cold packs

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등급

Moligand™

작업 유형

INHIBITOR

작동 메커니즘

Inhibitor of kinase insert domain receptor;Inhibitor of ret proto-oncogene

이름과 식별자

이성체 SMILES

CC1=CC(=NN1)NC2=NC(=NC(=C2)C)C3CCC(CC3)(C(=O)N[C@@H](C)C4=CN=C(C=C4)N5C=C(C=N5)F)OC

PubChem CID

129073603

분자량

533.6

관련 대상(인간)

RET Tclin Proto-oncogene tyrosine-protein kinase receptor Ret (1 Activities)

Discover Target: RET

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KDR Tclin Vascular endothelial growth factor receptor 2 (1 Activities)

Discover Target: KDR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

자주 묻는 질문

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2097132-94-8, the molecular formula is C27H32FN9O2, and the molecular weight is 533.6 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.