TH1338

Name: TH1338
Brand: MedChemExpress
SKU: HY-120574
Rating: 4.5 (1 reviews)

Cat. No.: HY-120574 Purity: 98.77%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

TH1338 Chemical Structure

CAS No. : 1258494-60-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 440	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 440	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 680	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1350	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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]

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.

Molecular Weight

391.42

Formula

C₂₂H₂₁N₃O₄

CAS No.

1258494-60-8

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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
10 mM	0.2555 mL	1.2774 mL	2.5548 mL

View the 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, 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 98.77%

Select Batch:

Data Sheet (279 KB) SDS (251 KB)

COA (258 KB) RP-HPLC (282 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]

Complete Stock Solution Preparation Table

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

TH1338 Related Classifications

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.

Keywords:

TH13381258494-60-8TH 1338TH-1338TopoisomeraseADC CytotoxinADC PayloadHT29coloncancerPC-3prostateNSCLClungInhibitorinhibitorinhibit

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TH1338

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TH1338 Related Antibodies

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Biological Activity

Purity & Documentation

References

Customer Review

TH1338 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

TH1338 Related Classifications

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