Merck
  • SML1693
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SML1693

Sigma-Aldrich

Pz-1

≥98% (HPLC)

Synonym(s):
N-(5-(Tert-Butyl)isoxazol-3-yl)-2-(4-(5-(1-methyl-1H-pyrazol-4-yl)-1H-benzo[d]imidazol-1-yl)phenyl)acetamide
Empirical Formula (Hill Notation):
C26H26N6O2
CAS Number:
Molecular Weight:
454.52
PubChem Substance ID:

品質水準

アッセイ

≥98% (HPLC)

形状

powder

white to beige

溶解性

DMSO: 1 mg/mL, clear (warmed)

保管温度

2-8°C

SMILES string

CN1N=CC(C(C=C2)=CC3=C2N(C4=CC=C(CC(NC5=NOC(C(C)(C)C)=C5)=O)C=C4)C=N3)=C1

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Pz-1 ≥98% (HPLC)

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PZ15227 ≥98% (HPLC)

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SML3180

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SML1596

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SML0775

PZ-II-029

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

form

powder

form

powder

form

powder

form

powder

color

white to beige

color

white to beige

color

white to beige

color

white to light brown

solubility

DMSO: 1 mg/mL, clear (warmed)

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: 5 mg/mL, clear (warmed)

solubility

DMSO: 10 mg/mL, clear

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

生物化学的/生理学的作用

Pz-1 is a cell-permeable, non-cytotoxic (up to 0.1 μM and 6 days; NIH/3T3 cells), and highly potent type II kinase inhibitor that potently inhibits RET and VEGFR2 tyrosine kinase activity (IC50 <1 nM; [ATP] = 190 μM) by targeting the kinases in their inactive DFG-out conformation, displaying significant affinity (Kd <50 nM) toward only TRKB, TRKC, GKA, FYN, SRC, TAK1, MUSK from a panel of 96 other kinases. Pz-1 inhibits cellular RET mutants (C634R, C634Y, V804L, V804M, M918T) and VEGFR2 phosphorylations, and selectively inhibits the growth of RET C634Y- than HRas G12V-transformed NIH/3T3 cultures (IC50 = 0.5 vs. 34.4 nM). Likewise, Pz-1 completely abrogated tumor formation from RET C634Y-transformed NIH/3T3 cells in mice in vivo (1 mg/kg/d, p.o.), while only up to 70% tumor suppression of HRas G12V-transformed cells was achieved with 10 mg/kg daily oral dosage.

保管分類コード

11 - Combustible Solids

WGK

WGK 3

引火点(°F)

Not applicable

引火点(℃)

Not applicable


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