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  2. Neuronal Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. Trk Receptor Apoptosis
  4. Larotrectinib

Larotrectinib  (Synonyms: LOXO-101; ARRY-470)

目錄號(hào): HY-12866 純度: 99.95%
COA 產(chǎn)品使用指南

Larotrectinib (LOXO-101) 是一種 ATP 競(jìng)爭(zhēng)性的、口服選擇性抑制劑，對(duì)原肌凝蛋白相關(guān)激酶 (TRK) 家族受體的三個(gè)亞型 (TRKA，B 和C) 具有納摩爾級(jí)別的 50% 抑制濃度。

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Larotrectinib Chemical Structure

Larotrectinib Chemical Structure

CAS No. : 1223403-58-4

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3.  試用裝只面向終端客戶。

規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥880
In-stock
1 mg ￥363
In-stock
5 mg ￥800
In-stock
10 mg ￥980
In-stock
50 mg ￥2600
In-stock
100 mg ￥3880
In-stock
200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

Other Forms of Larotrectinib:

查看 Trk Receptor 亞型特異性產(chǎn)品:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).

IC50 & Target[1][2]

TrkA

 

TrkB

 

TrkC

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 10 μM
Compound: 1
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 35007864]
BaF3 GI50
> 10 μM
Compound: 1; LOXO-101
Antiproliferative activity in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Antiproliferative activity in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
[PMID: 32949955]
BaF3 IC50
> 10 μM
Compound: 1
Antiproliferative activity against mouse BaF3 cells assessed as cell viability measured after 72 hrs by Micro plate reader method
Antiproliferative activity against mouse BaF3 cells assessed as cell viability measured after 72 hrs by Micro plate reader method
[PMID: 32702585]
BaF3 IC50
> 1000 nM
Compound: 1
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
> 3 μM
Compound: 1
Antiproliferative activity against mouse BaF3 cells habouring TRKA G595R mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells habouring TRKA G595R mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 35007864]
BaF3 IC50
0.007 μM
Compound: 1
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
0.009 μM
Compound: 1
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
0.013 μM
Compound: 1
Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method
Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method
[PMID: 32702585]
BaF3 IC50
0.016 μM
Compound: 1
Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method
Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method
[PMID: 32702585]
BaF3 IC50
0.04 μM
Compound: 1
Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK2 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method
Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK2 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method
[PMID: 32702585]
BaF3 IC50
0.054 μM
Compound: 1
Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) harbouring G696A mutation assessed as cell viability measured after 72 hrs by Micro plate reader method
Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) harbouring G696A mutation assessed as cell viability measured after 72 hrs by Micro plate reader method
[PMID: 32702585]
BaF3 IC50
0.11 μM
Compound: 1
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
0.184 μM
Compound: 1
Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) harbouring G667C mutation assessed as cell viability measured after 72 hrs by Micro plate reader method
Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) harbouring G667C mutation assessed as cell viability measured after 72 hrs by Micro plate reader method
[PMID: 32702585]
BaF3 IC50
0.539 μM
Compound: 1
Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) harbouring G595R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method
Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) harbouring G595R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method
[PMID: 32702585]
BaF3 IC50
1 nM
Compound: Larotrectinib
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
1.201 μM
Compound: 1
Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) harbouring G623R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method
Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) harbouring G623R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method
[PMID: 32702585]
BaF3 IC50
1.55 μM
Compound: 1
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
10.1 nM
Compound: 1
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
11 nM
Compound: Larotrectinib
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
1256 nM
Compound: Larotrectinib
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
14.8 nM
Compound: 1
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
1487 nM
Compound: Larotrectinib
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
173 nM
Compound: 1
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
18.4 nM
Compound: LOX0-101
Antiproliferative activity against mouse BaF3-LMNA-NTRK1 cells assessed as cell viability measured after 72 hrs
Antiproliferative activity against mouse BaF3-LMNA-NTRK1 cells assessed as cell viability measured after 72 hrs
[PMID: 33069129]
BaF3 IC50
2.24 μM
Compound: 1
Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK2 (unknown origin) harbouring G639R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method
Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK2 (unknown origin) harbouring G639R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method
[PMID: 32702585]
BaF3 IC50
2504.7 nM
Compound: LOX0-101
Antiproliferative activity against mouse BaF3-LMNA-NTRK1-G595 mutant cells assessed as cell viability measured after 72 hrs
Antiproliferative activity against mouse BaF3-LMNA-NTRK1-G595 mutant cells assessed as cell viability measured after 72 hrs
[PMID: 33069129]
BaF3 IC50
321 nM
Compound: Larotrectinib
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
332 nM
Compound: 1
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
3570 nM
Compound: Larotrectinib
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
38.2 nM
Compound: 1
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
4060 nM
Compound: Larotrectinib
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
46 nM
Compound: 1
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
547 nM
Compound: Larotrectinib
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
586 nM
Compound: Larotrectinib
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
59 nM
Compound: Larotrectinib
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
96 nM
Compound: 1
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]
KM12 IC50
0.005 μM
Compound: 1
Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 35007864]
KM12 IC50
0.012 μM
Compound: 1; LOXO-101
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: 36760745]
MCF7 IC50
> 10 μM
Compound: 1
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 35007864]
MCF7 IC50
> 40 μM
Compound: 1; LOXO-101
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: 36760745]
體外研究
(In Vitro)

Larotrectinib (LOXO-101) 是原肌球蛋白相關(guān)激酶 (TRK) 受體激酶家族 (TRKA、B 和 C) 的 ATP 競(jìng)爭(zhēng)性口服抑制劑，對(duì)所有三種亞型具有低納摩爾半抑制濃度，以及相對(duì)于其他激酶的選擇性大于 1,000 倍[1][2]。用 Larotrectinib (LOXO-101) 處理后的增殖測(cè)量表明，所有三種細(xì)胞系的細(xì)胞增殖都受到劑量依賴性抑制。對(duì) CUTO-3.29 的 IC50 小于 100 nM，KM12 和 MO-91 的 IC50 小于 10 nM，這與該藥物對(duì) TRK 激酶家族的已知效力一致[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

在大鼠和猴子研究中，Larotrectinib (LOXO-101) 表現(xiàn)出 33-100% 的口服生物利用度和 60-65% 的血漿蛋白結(jié)合率。它具有低腦滲透性，并且在 28 天 (d) GLP 毒理學(xué)研究中具有良好的耐受性。單劑量 (30 mg/kg) Larotrectinib (LOXO-101) 可降低腫瘤中 TRKA 的酪氨酸磷酸化和下游信號(hào)轉(zhuǎn)導(dǎo) (pERK) >80%[1]。注射 KM12 細(xì)胞的無(wú)胸腺裸鼠每天口服 Larotrectinib (LOXO-101)，持續(xù) 2 周。觀察到劑量依賴性腫瘤抑制，證明了這種選擇性化合物在體內(nèi)抑制腫瘤生長(zhǎng)的能力[4]。與媒介物處理的小鼠相比，Larotrectinib (LOXO-101) (200 mg/kg/天，口服給藥，持續(xù)六周) 可將骨髓和脾臟中的白血病浸潤(rùn)減少到檢測(cè)不到的水平。根據(jù) Xenogen 成像的測(cè)定，接受 Larotrectinib (LOXO-101) 處理的小鼠在停止處理 4 周后仍然存活并且沒(méi)有白血病[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

428.44

Formula

C21H22F2N6O2
CAS 號(hào)
性狀

固體

顏色

White to yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : ≥ 4.6 mg/mL (10.74 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.3340 mL 11.6702 mL 23.3405 mL
5 mM 0.4668 mL 2.3340 mL 4.6681 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.84 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.84 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.95%

參考文獻(xiàn)
Animal Administration
[4]

Mice[4]
Athymic nude mice are used throughout the study. 5×105 KM12 cells are injected subcutaneously into the dorsal flank area of the mice. Tumor volume is monitored by direct measurement with calipers and calculated by the formula: length × (width2)/2. Following the establishment of tumor and when the tumor size is between 150-200 mm2, mice are randomly selected to receive diluent, 60 mg/kg/dose or 200 mg/kg/dose of Larotrectinib (LOXO-101). Larotrectinib (LOXO-101) is administered by oral gavage once daily for 14 days. After the last dose, tissue and blood are collected at 3, 6 and 24 hours post-treatment[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3340 mL 11.6702 mL 23.3405 mL 58.3512 mL
5 mM 0.4668 mL 2.3340 mL 4.6681 mL 11.6702 mL
10 mM 0.2334 mL 1.1670 mL 2.3340 mL 5.8351 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱：
Larotrectinib
目錄號(hào)：
HY-12866
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