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  2. Antibody-drug Conjugate/ADC Related Cell Cycle/DNA Damage
  3. Topoisomerase ADC Cytotoxin
  4. TH1338

TH1338 (compound 3b) 是具有口服活性的喜樹堿的衍生物，是有潛力的抗癌化合物，在體外表現(xiàn)出優(yōu)異的腫瘤細胞毒性的效果。TH1338 (compound 3b) 具有顯著的血腦屏障透過性，良好的外排泵特性和低血液學(xué)毒性。

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TH1338 Chemical Structure

TH1338 Chemical Structure

CAS No. : 1258494-60-8

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥2407
In-stock
1 mg ￥1000
In-stock
5 mg ￥2188
In-stock
10 mg ￥3500
In-stock
25 mg 現(xiàn)貨 詢價
50 mg   詢價  
100 mg   詢價  

* Please select Quantity before adding items.

Customer Review

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

TH1338 (compound 3b), an orally active camptothecin derivative and a potent chemotherapeutic agent for cancer, demonstrates excellent cytotoxic potency against human tumor cell lines in vitro. TH1338 (compound 3b) possesses significant brain penetration, favorable efflux pump properties, and hematological toxicity profile[1][2].

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-375 IC50
7 nM
Compound: 3b
Cytotoxicity against human A375 cells after 72 hrs by alamar blue assay
Cytotoxicity against human A375 cells after 72 hrs by alamar blue assay
[PMID: 21341674]
Bone marrow cell IC50
110 nM
Compound: 3b
Cytotoxicity against mouse bone marrow cell by CFU-GM assay
Cytotoxicity against mouse bone marrow cell by CFU-GM assay
[PMID: 21341674]
Bone marrow cell IC50
620 nM
Compound: 3b
Cytotoxicity against human bone marrow cell by CFU-GM assay
Cytotoxicity against human bone marrow cell by CFU-GM assay
[PMID: 21341674]
DU-145 IC50
1200 nM
Compound: 3b
Cytotoxicity against human DU145 cells after 72 hrs by alamar blue assay
Cytotoxicity against human DU145 cells after 72 hrs by alamar blue assay
[PMID: 21341674]
H69AR IC50
240 nM
Compound: 3b
Cytotoxicity against human H69AR cells overexpressing MDR1 after 72 hrs by alamar blue assay
Cytotoxicity against human H69AR cells overexpressing MDR1 after 72 hrs by alamar blue assay
[PMID: 21341674]
HT-29 IC50
300 nM
Compound: 3b
Cytotoxicity against human HT-29 cells after 72 hrs by alamar blue assay
Cytotoxicity against human HT-29 cells after 72 hrs by alamar blue assay
[PMID: 21341674]
IGROV-1 IC50
20 nM
Compound: 3b
Cytotoxicity against human IGROV1 cells after 72 hrs by alamar blue assay
Cytotoxicity against human IGROV1 cells after 72 hrs by alamar blue assay
[PMID: 21341674]
LNCaP IC50
120 nM
Compound: 3b
Cytotoxicity against human LNCAP cells after 72 hrs by alamar blue assay
Cytotoxicity against human LNCAP cells after 72 hrs by alamar blue assay
[PMID: 21341674]
Malme-3M IC50
1200 nM
Compound: 3b
Cytotoxicity against human MALME-3M cells after 72 hrs by alamar blue assay
Cytotoxicity against human MALME-3M cells after 72 hrs by alamar blue assay
[PMID: 21341674]
MES-SA IC50
4 nM
Compound: 3b
Cytotoxicity against human MESSA cells after 72 hrs by alamar blue assay
Cytotoxicity against human MESSA cells after 72 hrs by alamar blue assay
[PMID: 21341674]
MES-SA/Dx5 IC50
12 nM
Compound: 3b
Cytotoxicity against human MES-SA/Dx5 cells overexpressing MDR1 after 72 hrs by alamar blue assay
Cytotoxicity against human MES-SA/Dx5 cells overexpressing MDR1 after 72 hrs by alamar blue assay
[PMID: 21341674]
NCI-H460 IC50
12 nM
Compound: 3b
Cytotoxicity against human H460 cells after 72 hrs by alamar blue assay
Cytotoxicity against human H460 cells after 72 hrs by alamar blue assay
[PMID: 21341674]
NCI-H460 IC50
120 nM
Compound: 3b
Cytotoxicity against human H460 cells after 72 hrs by alamar blue assay in presence of 40 mg/ml HSA
Cytotoxicity against human H460 cells after 72 hrs by alamar blue assay in presence of 40 mg/ml HSA
[PMID: 21341674]
NCI-H460 IC50
7 nM
Compound: 3b
Cytotoxicity against human H460 cells after 72 hrs by alamar blue assay
Cytotoxicity against human H460 cells after 72 hrs by alamar blue assay
[PMID: 21341674]
NCI-H69 IC50
110 nM
Compound: 3b
Cytotoxicity against human H69 cells after 72 hrs by alamar blue assay
Cytotoxicity against human H69 cells after 72 hrs by alamar blue assay
[PMID: 21341674]
PC-3 IC50
24 nM
Compound: 3b
Cytotoxicity against human PC3 cells after 72 hrs by alamar blue assay
Cytotoxicity against human PC3 cells after 72 hrs by alamar blue assay
[PMID: 21341674]
SK-MEL-2 IC50
130 nM
Compound: 3b
Cytotoxicity against human SK-MEL-2 cells after 72 hrs by alamar blue assay
Cytotoxicity against human SK-MEL-2 cells after 72 hrs by alamar blue assay
[PMID: 21341674]
體外研究
(In Vitro)

TH1338 (compound 3b) demonstrates significant brain penetration when dosed orally in mice[1].
TH1338 (compound 3b) exhibits potent anti-tumor activity in H460 (NSCLC) human tumor xenograft model[1].

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

Cell Viability Assay[1]

Cell Line: H460 (NSCLC) human tumor xenograft model.
Concentration: 40 mg/kg.
Incubation Time: Oral gavage.
Result: Exhibited superior antitumor activity.
分子量

391.42

Formula

C22H21N3O4
CAS 號
性狀

固體

顏色

Light yellow to yellow

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 10 mg/mL (25.55 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.5548 mL 12.7740 mL 25.5480 mL
5 mM 0.5110 mL 2.5548 mL 5.1096 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

動物實驗：

請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，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；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

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

    Solubility: ≥ 1.82 mg/mL (4.65 mM); 澄清溶液

    此方案可獲得 ≥ 1.82 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 18.2 mg/mL 的澄清 DMSO 儲備液加到 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。
動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動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 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，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)給藥周期超過半月以上，請謹慎選擇該方案。
請確保第一步儲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
參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(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 2.5548 mL 12.7740 mL 25.5480 mL 63.8700 mL
5 mM 0.5110 mL 2.5548 mL 5.1096 mL 12.7740 mL
10 mM 0.2555 mL 1.2774 mL 2.5548 mL 6.3870 mL
15 mM 0.1703 mL 0.8516 mL 1.7032 mL 4.2580 mL
20 mM 0.1277 mL 0.6387 mL 1.2774 mL 3.1935 mL
25 mM 0.1022 mL 0.5110 mL 1.0219 mL 2.5548 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：
TH1338
目錄號：
HY-120574
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