Cat. No.: HY-120574

TH1338

고객리뷰

Based on 1 Customer Validation

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.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 98.77%
CAS No.: 1258494-60-8
화학식: C₂₂H₂₁N₃O₄
분자량:391.42

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

TH1338 Chemical Structure

CAS No.: 1258494-60-8

사이즈

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Biological Activity
- 제품 설명
- Cellular Effect
- In Vitro
Chemical Information
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

All ADC Payloads Isoforms :

All Topoisomerase Isoforms :

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	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-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]

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].

MedChemExpress (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.

Chemical Information

CAS No. 1258494-60-8
Appearance Solid
분자량 391.42
화학식 C₂₂H₂₁N₃O₄
Color Light yellow to yellow
SMILES

O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=C(CC)C5=CC=CC=C5N=C4C3=C2N)=O
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

용액&용해도

In Vitro:

DMSO : 10 mg/mL (25.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5548 mL

12.7740 mL

25.5480 mL

5 mM

0.5110 mL

2.5548 mL

5.1096 mL

10 mM

0.2555 mL

1.2774 mL

2.5548 mL

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1.82 mg/mL (4.65 mM); Clear solution

This protocol yields a clear solution of ≥ 1.82 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (18.2 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Jian-Xin Duan, et al. 14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment. J Med Chem. 2011 Mar 24;54(6):1715-23. [Content Brief]

[2]. Xia Cheng, et al. Preparation, Characterization, and In Vivo Study of 7-Ethyl-14-Aminocamptothecin-Loaded Poly(Ethylene Glycol)2000 -Poly(Lactic Acid)2000 Polymeric Micelles Against H460 Human Nonsmall Cell Lung Carcinoma. J Pharm Sci. 2015 Nov;104(11):3934-3942. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	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

Keywords

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TH1338

Toxins for Antibody-Drug Conjugate Research Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Lung Cancer Compound Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

All ADC Payloads Isoforms

All Topoisomerase Isoforms

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

TH1338

Toxins for Antibody-Drug Conjugate Research Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Lung Cancer Compound Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

All ADC Payloads Isoforms

All Topoisomerase Isoforms

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

TH1338 Related Classifications

HY-120574 Related Classifications