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Pralsetinib (Blu667) Sale

(Synonyms: 普拉替尼; BLU-667) 目录号 : GC31780

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).

Pralsetinib (Blu667) Chemical Structure

Cas No.:2097132-94-8

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,150.00
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1mg
¥490.00
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5mg
¥980.00
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10mg
¥1,540.00
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25mg
¥2,599.00
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50mg
¥3,903.00
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Sample solution is provided at 25 µL, 10mM.

Description

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).

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[1].

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[1].

[1] Subbiah V, et al. Cancer Discov. 2018, 8(7):836-849.

实验参考方法

Cell experiment:

KIF5B-RET Ba/F3 cells are exposed to compound concentrations ranging from 25 µM to 95.4 pM for 48 hours, and proliferation is assessed with Cell Titer Glo. TT, MZ-CRC-1, TPC-1 or LC2/ad cells are exposed to compound for 4 days and proliferation is measured by BrdU incorporation[2].

Animal experiment:

Mice[2]BALB/c nude mice are inoculated subcutaneously into the right flank with KIF5B-RET Ba/F3 cells, KIF5B-RET V804L Ba/F3 cells, or TT cells. For all experiments, mice are dosed twice-daily with vehicle, 3 mg/kg, 10 mg/kg, or 30 mg/kg Pralsetinib (Blu667) or once-daily with 60 mg/kg Pralsetinib (Blu667) or 60 mg/kg XL184[2].

References:

[1]. Subbiah V, et al. Precision Targeted Therapy With BLU-667 for RET-Driven Cancers. American Association for Cancer Research. 10.1158/2159-8290.CD-18-0338.

化学性质

Cas No. 2097132-94-8 SDF
别名 普拉替尼; BLU-667
Canonical SMILES 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
分子式 C27H32FN9O2 分子量 533.6
溶解度 DMSO : ≥ 100 mg/mL (187.41 mM);Water : < 0.1 mg/mL (insoluble) 储存条件 Store at 4°C
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1 mg 5 mg 10 mg
1 mM 1.8741 mL 9.3703 mL 18.7406 mL
5 mM 0.3748 mL 1.8741 mL 3.7481 mL
10 mM 0.1874 mL 0.937 mL 1.8741 mL
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