Selitrectinib
Based on 5 publication(s) in Google Scholar
Selitrectinib (LOXO-195) is a next-generation TRK kinase inhibitor, with IC50s of 0.6 nM and <2.5 nM for TRKA and TRKC, respectively.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.74%
- CAS 番号: 2097002-61-2
- 分子式: C20H21FN6O
- 分子量:380.42
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 Selitrectinib
More-
Cell Proliferation/Viability Assay
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WB
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IF
生物活性
|
TrkA 0.6 nM (IC50) |
TrkC <2.5 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
2.7 nM
Compound: LOXO-195
|
Cytotoxicity against mouse BaF3 cells transfected with TrKA G623R mutant assessed as reduction in cell viability by MTT assay
Cytotoxicity against mouse BaF3 cells transfected with TrKA G623R mutant assessed as reduction in cell viability by MTT assay
|
[PMID: 34253025] |
| BaF3 | IC50 |
24.4 nM
Compound: LOXO-195
|
Cytotoxicity against mouse BaF3 cells transfected with TrKA G667A mutant assessed as reduction in cell viability by MTT assay
Cytotoxicity against mouse BaF3 cells transfected with TrKA G667A mutant assessed as reduction in cell viability by MTT assay
|
[PMID: 34253025] |
| BaF3 | IC50 |
25.4 nM
Compound: LOXO-195
|
Cytotoxicity against mouse BaF3 cells transfected with TrKA F589L mutant assessed as reduction in cell viability by MTT assay
Cytotoxicity against mouse BaF3 cells transfected with TrKA F589L mutant assessed as reduction in cell viability by MTT assay
|
[PMID: 34253025] |
| BaF3 | IC50 |
36.7 nM
Compound: LOXO-195
|
Cytotoxicity against mouse BaF3 cells transfected with SLC34A2-Ros1 assessed as reduction in cell viability by MTT assay
Cytotoxicity against mouse BaF3 cells transfected with SLC34A2-Ros1 assessed as reduction in cell viability by MTT assay
|
[PMID: 34253025] |
| BaF3 | IC50 |
4.9 nM
Compound: LOXO-195
|
Cytotoxicity against mouse BaF3 cells transfected with TrKA assessed as reduction in cell viability by MTT assay
Cytotoxicity against mouse BaF3 cells transfected with TrKA assessed as reduction in cell viability by MTT assay
|
[PMID: 34253025] |
| BaF3 | IC50 |
6.8 nM
Compound: LOXO-195
|
Cytotoxicity against mouse BaF3 cells transfected with TrKA G595R mutant assessed as reduction in cell viability by MTT assay
Cytotoxicity against mouse BaF3 cells transfected with TrKA G595R mutant assessed as reduction in cell viability by MTT assay
|
[PMID: 34253025] |
| BaF3 | IC50 |
1.1 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells transfected with ETV6-wild type TRKA assessed as cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells transfected with ETV6-wild type TRKA assessed as cell viability incubated for 72 hrs by CCK8 assay
|
[PMID: 34668694] |
| BaF3 | IC50 |
1.4 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells transfected with ETV6-wild type TRKB assessed as cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells transfected with ETV6-wild type TRKB assessed as cell viability incubated for 72 hrs by CCK8 assay
|
[PMID: 34668694] |
| BaF3 | IC50 |
1.6 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells transfected with ETV6-wild type TRKC assessed as cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells transfected with ETV6-wild type TRKC assessed as cell viability incubated for 72 hrs by CCK8 assay
|
[PMID: 34668694] |
| BaF3 | IC50 |
12.6 nM
Compound: 3
|
Antiproliferative activity against mouse BAF3 cells transfected with LMNA-TRKA F589L mutant assessed as cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BAF3 cells transfected with LMNA-TRKA F589L mutant assessed as cell viability incubated for 72 hrs by CCK8 assay
|
[PMID: 34668694] |
| BaF3 | IC50 |
13 nM
Compound: 3
|
Antiproliferative activity against mouse BAF3 cells transfected with LMNA-TRKA G595R mutant assessed as cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BAF3 cells transfected with LMNA-TRKA G595R mutant assessed as cell viability incubated for 72 hrs by CCK8 assay
|
[PMID: 34668694] |
| BaF3 | IC50 |
72.6 nM
Compound: 3
|
Antiproliferative activity aganist mouse BAF3 cells transfected with LMNA-TRKA G667C mutant assessed as cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity aganist mouse BAF3 cells transfected with LMNA-TRKA G667C mutant assessed as cell viability incubated for 72 hrs by CCK8 assay
|
[PMID: 34668694] |
| BaF3 | IC50 |
0.018 μM
Compound: LOX0195
|
Cytotoxicity against mouse BaF3 cells harboring TEL fused TrkC G613R mutant assessed as inhibition of cell growth by MTT assay
Cytotoxicity against mouse BaF3 cells harboring TEL fused TrkC G613R mutant assessed as inhibition of cell growth by MTT assay
|
[PMID: 35080890] |
| BaF3 | IC50 |
1 nM
Compound: LOX0195
|
Cytotoxicity against mouse BaF3 cells expressing CD74 fused TrkA assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
Cytotoxicity against mouse BaF3 cells expressing CD74 fused TrkA assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
|
[PMID: 35080890] |
| BaF3 | IC50 |
109 nM
Compound: LOX0195
|
Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G667C mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G667C mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
|
[PMID: 35080890] |
| BaF3 | IC50 |
15 nM
Compound: LOX0195
|
Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G595R mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G595R mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
|
[PMID: 35080890] |
| BaF3 | IC50 |
17 nM
Compound: LOX0195
|
Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA F589L mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA F589L mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
|
[PMID: 35080890] |
| BaF3 | IC50 |
18 nM
Compound: LOX0195
|
Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC G623R assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC G623R assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
|
[PMID: 35080890] |
| BaF3 | IC50 |
30 nM
Compound: LOX0195
|
Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G667S mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G667S mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
|
[PMID: 35080890] |
| BaF3 | IC50 |
4 nM
Compound: LOX0195
|
Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
|
[PMID: 35080890] |
| BaF3 | IC50 |
50 nM
Compound: LOX0195
|
Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC G696C assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC G696C assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
|
[PMID: 35080890] |
| BaF3 | IC50 |
9 nM
Compound: LOX0195
|
Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkA assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkA assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
|
[PMID: 35080890] |
| BaF3 | IC50 |
>10000 nM
Compound: LOX0195
|
Cytotoxicity against mouse BaF3 assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
Cytotoxicity against mouse BaF3 assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
|
[PMID: 35080890] |
| BaF3 | IC50 |
0.001 μM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA assessed as cell growth inhibition incubated for 3 days by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA assessed as cell growth inhibition incubated for 3 days by CCK8 assay
|
[PMID: 35426680] |
| BaF3 | IC50 |
0.001 μM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC assessed as cell growth inhibition incubated for 3 days by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC assessed as cell growth inhibition incubated for 3 days by CCK8 assay
|
[PMID: 35426680] |
| BaF3 | IC50 |
0.013 μM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G595R mutant assessed as cell growth inhibition incubated for 3 days by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G595R mutant assessed as cell growth inhibition incubated for 3 days by CCK8 assay
|
[PMID: 35426680] |
| BaF3 | IC50 |
0.041 μM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667C mutant assessed as cell growth inhibition incubated for 3 days by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667C mutant assessed as cell growth inhibition incubated for 3 days by CCK8 assay
|
[PMID: 35426680] |
| BaF3 | IC50 |
10.5 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667S mutant incubated for 3 days by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667S mutant incubated for 3 days by CCK8 assay
|
[PMID: 35426680] |
| BaF3 | IC50 |
10.7 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC V573M mutant incubated for 3 days by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC V573M mutant incubated for 3 days by CCK8 assay
|
[PMID: 35426680] |
| BaF3 | IC50 |
2.4 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696A mutant incubated for 3 days by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696A mutant incubated for 3 days by CCK8 assay
|
[PMID: 35426680] |
| BaF3 | IC50 |
28.2 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696C mutant incubated for 3 days by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696C mutant incubated for 3 days by CCK8 assay
|
[PMID: 35426680] |
| BaF3 | IC50 |
3.2 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667A mutant incubated for 3 days by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667A mutant incubated for 3 days by CCK8 assay
|
[PMID: 35426680] |
| BaF3 | IC50 |
5.7 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G623E mutant incubated for 3 days by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G623E mutant incubated for 3 days by CCK8 assay
|
[PMID: 35426680] |
| BaF3 | IC50 |
8.2 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696S mutant incubated for 3 days by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696S mutant incubated for 3 days by CCK8 assay
|
[PMID: 35426680] |
| BaF3 | IC50 |
8.5 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G623R mutant incubated for 3 days by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G623R mutant incubated for 3 days by CCK8 assay
|
[PMID: 35426680] |
| BaF3 | IC50 |
>10000 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 3 days by CCK8 assay
Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 3 days by CCK8 assay
|
[PMID: 35426680] |
| BaF3 | IC50 |
0.0082 μM
Compound: LOXO-195
|
Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
|
[PMID: 35617855] |
| BaF3 | IC50 |
0.013 μM
Compound: LOXO-195
|
Antiproliferative activity against mouse BaF3 cells harboring TRKA G667C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells harboring TRKA G667C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
|
[PMID: 35617855] |
| BaF3 | IC50 |
0.018 μM
Compound: LOXO-195
|
Antiproliferative activity against mouse BaF3 cells harboring TRKA G595R mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells harboring TRKA G595R mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
|
[PMID: 35617855] |
| BaF3 | IC50 |
27.8 nM
Compound: selitrectinib
|
Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as cell growth inhibition
Antiproliferative activity against mouse BaF3 cells harboring TRKA F589L mutant assessed as cell growth inhibition
|
[PMID: 36395392] |
| BaF3 | IC50 |
1.2 nM
Compound: 3; LOXO-195
|
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
|
[PMID: 36410169] |
| BaF3 | IC50 |
1.7 nM
Compound: 3; LOXO-195
|
Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
|
[PMID: 36410169] |
| BaF3 | IC50 |
41.4 nM
Compound: 3; LOXO-195
|
Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
|
[PMID: 36410169] |
| BaF3 | IC50 |
5.2 nM
Compound: 3; LOXO-195
|
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
|
[PMID: 36410169] |
| BaF3 | IC50 |
16.7 nM
Compound: Selitrectinib
|
Antiproliferative activity against mouse BaF3 cells expressing TRKA F589L mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells expressing TRKA F589L mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
|
[PMID: 37030091] |
| BaF3 | IC50 |
23.2 nM
Compound: Selitrectinib
|
Antiproliferative activity against mouse BaF3 cells expressing TRKA G595R mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells expressing TRKA G595R mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
|
[PMID: 37030091] |
| BaF3 | IC50 |
95.6 nM
Compound: Selitrectinib
|
Antiproliferative activity against mouse BaF3 cells expressing TRKA G667C mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells expressing TRKA G667C mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
|
[PMID: 37030091] |
| BaF3 | IC50 |
>1000 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
1.35 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 fusion protein incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 fusion protein incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
1.36 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-NTRK3 fusion protein incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-NTRK3 fusion protein incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
10.28 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G595R mutant fusion protein incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G595R mutant fusion protein incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
10.98 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G6968 mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G6968 mutant incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
16.7 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA V573M mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA V573M mutant incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
17.2 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC F617L mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC F617L mutant incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
2.32 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring wild type ETV6-TRKB incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring wild type ETV6-TRKB incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
22.23 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G667C mutant fusion protein incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G667C mutant fusion protein incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
26.11 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRKIF 589L mutant fusion protein incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRKIF 589L mutant fusion protein incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
26.38 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB V617M mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB V617M mutant incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
3.39 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667A mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667A mutant incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
30.66 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC V601M mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC V601M mutant incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
31.5 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring TRKA-F589L fusion protein incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring TRKA-F589L fusion protein incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
35.79 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB F633L mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB F633L mutant incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
37 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G6678 mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G6678 mutant incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
4.15 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
41.06 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G639R mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G639R mutant incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
42.04 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G709C mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G709C mutant incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
423.15 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667A mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667A mutant incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
48.16 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696C mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696C mutant incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
5.08 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623R mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623R mutant incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
7.48 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623E mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623E mutant incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
>1000 nM
Compound: 3
|
Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667C mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667C mutant incubated for 3 days by CCK8 method
|
[PMID: 37676745] |
| BaF3 | IC50 |
>20000 nM
Compound: Selitrectinib
|
Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
|
[PMID: 38029466] |
| BaF3 | IC50 |
15.2 nM
Compound: Selitrectinib
|
Antiproliferative activity against mouse BaF3 cells harboring TRKA G595R mutant assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells harboring TRKA G595R mutant assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
|
[PMID: 38029466] |
| BaF3 | IC50 |
84.5 nM
Compound: Selitrectinib
|
Antiproliferative activity against mouse BaF3 cells harboring TRKA G667C mutant assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells harboring TRKA G667C mutant assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
|
[PMID: 38029466] |
| BaF3 | IC50 |
113.1 nM
Compound: Selitrectinib
|
Antiproliferative activity against mouse BaF3 cells expressing TRKA G667C mutant incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing TRKA G667C mutant incubated for 72 hrs by CCK8 assay
|
[PMID: 39033612] |
| BaF3 | IC50 |
12 nM
Compound: Selitrectinib
|
Antiproliferative activity against mouse BaF3 cells expressing TRKA G595R mutant incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing TRKA G595R mutant incubated for 72 hrs by CCK8 assay
|
[PMID: 39033612] |
| KM12 | IC50 |
<=5 nM
Compound: LOXO-195
|
Inhibition of cell proliferation in TPM3-NTRK1 fusion positive human KM12 cells incubated for 72 hrs by DAPI staining based analysis
Inhibition of cell proliferation in TPM3-NTRK1 fusion positive human KM12 cells incubated for 72 hrs by DAPI staining based analysis
|
[PMID: 28578312] |
| KM12 | IC50 |
<=5 nM
Compound: LOXO-195
|
Antiproliferative activity against TrK fused human KM12 cells
Antiproliferative activity against TrK fused human KM12 cells
|
[PMID: 34253025] |
| KM12 | IC50 |
0.0028 μM
Compound: LOXO-195
|
Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay
|
[PMID: 35617855] |
| KM12 | IC50 |
2.9 nM
Compound: Selitrectinib
|
Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
|
[PMID: 37030091] |
| KM12 | IC50 |
1.7 nM
Compound: Selitrectinib
|
Antiproliferative activity against human KM12 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human KM12 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
|
[PMID: 38029466] |
| KM12 | IC50 |
6.8 nM
Compound: Selitrectinib
|
Antiproliferative activity against human KM12 cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human KM12 cells incubated for 72 hrs by CCK8 assay
|
[PMID: 39033612] |
| MCF7 | IC50 |
>20000 nM
Compound: Selitrectinib
|
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
|
[PMID: 38029466] |
| MCF7 | IC50 |
>10000 nM
Compound: Selitrectinib
|
Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CCK8 assay
|
[PMID: 39033612] |
| NIH3T3 | GI50 |
1.6 nM
Compound: 19; LOXO-195
|
Antiproliferative activity against mouse NIH3T3 cells transfected with wild type TRKA assessed as cell growth inhibition
Antiproliferative activity against mouse NIH3T3 cells transfected with wild type TRKA assessed as cell growth inhibition
|
[PMID: 38389874] |
| NIH3T3 | GI50 |
17.5 nM
Compound: 19; LOXO-195
|
Antiproliferative activity against mouse NIH3T3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method
Antiproliferative activity against mouse NIH3T3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method
|
[PMID: 38389874] |
| NIH3T3 | GI50 |
2 nM
Compound: 19; LOXO-195
|
Antiproliferative activity against mouse NIH3T3 cells expressing wild type TRKC mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse NIH3T3 cells expressing wild type TRKC mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
|
[PMID: 38389874] |
| NIH3T3 | GI50 |
25 nM
Compound: 19; LOXO-195
|
Antiproliferative activity against mouse NIH3T3 cells expressing TRKA G667S mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse NIH3T3 cells expressing TRKA G667S mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
|
[PMID: 38389874] |
| NIH3T3 | GI50 |
29 nM
Compound: 19; LOXO-195
|
Antiproliferative activity against mouse NIH3T3 cells harbouring TRKA V573M mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method
Antiproliferative activity against mouse NIH3T3 cells harbouring TRKA V573M mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method
|
[PMID: 38389874] |
| NIH3T3 | GI50 |
45.5 nM
Compound: 19; LOXO-195
|
Antiproliferative activity against mouse NIH3T3 cells expressing TRKC G623R mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse NIH3T3 cells expressing TRKC G623R mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
|
[PMID: 38389874] |
| NIH3T3 | GI50 |
64 nM
Compound: 19; LOXO-195
|
Antiproliferative activity against mouse NIH3T3 cells transfected with TRKA G667C mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method
Antiproliferative activity against mouse NIH3T3 cells transfected with TRKA G667C mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method
|
[PMID: 38389874] |
| NIH3T3 | GI50 |
7 nM
Compound: 19; LOXO-195
|
Antiproliferative activity against mouse NIH3T3 cells harbouring TRKC G595R mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method
Antiproliferative activity against mouse NIH3T3 cells harbouring TRKC G595R mutant assessed as cell growth inhibition incubated for 3 days by CCK8 method
|
[PMID: 38389874] |
| NIH3T3 | GI50 |
9 nM
Compound: 19; LOXO-195
|
Antiproliferative activity against mouse NIH3T3 cells expressing TRKA F589L mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse NIH3T3 cells expressing TRKA F589L mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
|
[PMID: 38389874] |
Selitrectinib (LOXO-195) demonstrates strong binding to the wild-type TRKA, TRKB and TRKC kinase domains. Selitrectinib (LOXO-195) has potent (IC50<1 nM) inhibitory activity in kinase enzyme assays. Importantly, Selitrectinib (LOXO-195) achieves low nanomolar inhibitory activity against TRKA G595R, TRKC G623R, and TRKA G667C, with IC50s ranging from 2.0-9.8 nM. 228 individual kinases in vitro are profiled at a Selitrectinib (LOXO-195) concentration of 1 μM, which is ~1667-fold higher than its IC50 for TRKA (0.6 nM). Selitrectinib (LOXO-195) is more than 1000-fold selective for 98% of non-TRK kinases tested. Selitrectinib (LOXO-195) demonstrates potent inhibition of cell proliferation in TRK fusion-containing KM12, CUTO-3, and MO-91 cell lines (IC50≤5 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2097002-61-2
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性状 Solid
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分子量 380.42
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分子式 C20H21FN6O
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Color White to yellow
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SMILES
FC1=CN=C(CC[C@H](N2)C)C([C@](CCC3)([H])N3C(C=CN4N=C5)=NC4=C5C2=O)=C1
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別名
LOXO-195
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Mol Cancer Ther
Molecular Characteristics of Repotrectinib That Enable Potent Inhibition of TRK Fusion Proteins and Resistant Mutations. [Abstract]2021 Dec;20(12):2446-2456. PMID: 34625502 -
Cancers (Basel)
The Impact of ETV6-NTRK3 Oncogenic Gene Fusions on Molecular and Signaling Pathway Alterations. [Abstract]2023 Aug 24;15(17):4246. PMID: 37686522
Selitrectinib purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2023 Aug 24;15(17):4246. [Abstract]
Western blot analysis showing the influence of Selitrectinib (LOXO-195) (100 nM) on the protein levels of EN variants in stable cell lines.
Selitrectinib purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2023 Aug 24;15(17):4246. [Abstract]
Fluorescence microscopy images portraying the subcellular localization of EN variants under two conditions: cells untreated and cells treated with Selitrectinib (LOXO-195) (100 nM).
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Cancer Med
Induction of resistance to neurotrophic tropomyosin-receptor kinase inhibitors by HMGCS2 via a mevalonate pathway. [Abstract]2024 Jun;13(12):e7393. PMID: 38923428
Selitrectinib purchased from MedChemExpress. Usage Cited in: Cancer Med. 2024 Jun;13(12):e7393. [Abstract]
Cell viabilities were significantly reduced in NTRK‐TKI resistant cells after silibinin and NTRK‐TKIs treatment compared to NTRK‐TKIs alone. Treatments were with 100 nM NTRK‐TKIs (KM12‐LR: Larotrectinib, KM12‐ER: Entrectinib and KM12‐SR: Selitrectinib) and 20 μM silibinin for 72 h.
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溶剤 & 溶解度
DMSO : 62.5 mg/mL (164.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.47 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.47 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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-
-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
For assessment of cellular inhibition potency, cells are harvested per a standard protocol, counted and added to flat-bottom, collagen I-coated 96-well assay plates at 3×104 cells/well (wild-type cell line) or 5×104 cells/well (mutant cell lines) in 100 μL/well of DMEM growth medium containing 10% FBS. Plates are then incubated at room temperature for 30 minutes prior to an overnight incubation at 37°C with 5% CO2. Next, cells are treated for 1 hour at 37°C, 5% CO2 with TRK inhibitor compounds (e.g., Selitrectinib (LOXO-195)). Control wells contain either 0.25% DMSO alone or 1 μM larotrectinib or LOXO-195. Following compound incubation, growth medium is discarded and cells are lysed by addition of 60 μL/well of ice-cold lysis buffer containing protease and phosphatase inhibitors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
The ΔTRKA, ΔTRKA-G595R, and ΔTRKA -G667C NIH-3T3 tumor cell lines (~2-3x106 cells) and KM12 cells (5x106 cells) are injected subcutaneously into the right flank of female nu/nu NCr mice. Tumors are allowed to grow to ~100-200 mm3 or ~500 mm3, and animals are randomized by tumor size into dosing groups of 5 (KM12), 7 (NIH 3T3 ΔTRKA variants) or 3-4 (for PK-PD) animals. Animals are dosed by oral gavage with vehicle, Selitrectinib (LOXO-195) in 1% carboxymethylcellulose/0.5% Tween-80 or larotrectinib in 100% Labrafac lipophile. All animals are obtained at 6-8 weeks of age, housed in groups of 5 and allowed a one-week acclimation period before cancer cell injection. Animals are dosed with vehicle twice daily, Selitrectinib (LOXO-195) at 30 mg/kg, 100 mg/kg and 300 mg/kg twice daily and larotrectinib at 60 mg/kg daily for 9-12 days. Body weight and tumor size are monitored after cell implantation and at regular intervals during dosing[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (280 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6287 mL | 13.1434 mL | 26.2867 mL | 65.7168 mL |
| 5 mM | 0.5257 mL | 2.6287 mL | 5.2573 mL | 13.1434 mL | |
| 10 mM | 0.2629 mL | 1.3143 mL | 2.6287 mL | 6.5717 mL | |
| 15 mM | 0.1752 mL | 0.8762 mL | 1.7524 mL | 4.3811 mL | |
| 20 mM | 0.1314 mL | 0.6572 mL | 1.3143 mL | 3.2858 mL | |
| 25 mM | 0.1051 mL | 0.5257 mL | 1.0515 mL | 2.6287 mL | |
| 30 mM | 0.0876 mL | 0.4381 mL | 0.8762 mL | 2.1906 mL | |
| 40 mM | 0.0657 mL | 0.3286 mL | 0.6572 mL | 1.6429 mL | |
| 50 mM | 0.0526 mL | 0.2629 mL | 0.5257 mL | 1.3143 mL | |
| 60 mM | 0.0438 mL | 0.2191 mL | 0.4381 mL | 1.0953 mL | |
| 80 mM | 0.0329 mL | 0.1643 mL | 0.3286 mL | 0.8215 mL | |
| 100 mM | 0.0263 mL | 0.1314 mL | 0.2629 mL | 0.6572 mL |