Cyproheptadine (hydrochloride sesquihydrate)

Name: Cyproheptadine (hydrochloride sesquihydrate)
Brand: MedChemExpress
SKU: HY-B1165
Rating: 5.0 (3 reviews)

Cat. No.: HY-B1165 Purity: 99.74%: Data Sheet
COA

SDS
Handling Instructions
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Cyproheptadine hydrochloride sesquihydrate acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine hydrochloride sesquihydrate mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine hydrochloride sesquihydrate induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine hydrochloride sesquihydrate inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine hydrochloride sesquihydrate can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia.

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

Cyproheptadine (hydrochloride sesquihydrate) Chemical Structure

CAS No. : 41354-29-4

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

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Cyproheptadine (hydrochloride sesquihydrate):

Cyproheptadine hydrochloride In-stock
Cyproheptadine In-stock
Cyproheptadine hydrochloride sesquihydrate (Standard) In-stock

3 Publications Citing Use of MCE Cyproheptadine (hydrochloride sesquihydrate)

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

View All Checkpoint Kinase (Chk) Isoform Specific Products:

View All Isoforms

Chk1 Chk2 BUBR1

View All Histamine Receptor Isoform Specific Products:

View All Isoforms

H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

View All 5-HT Receptor Isoform Specific Products:

View All Isoforms

5-HT Receptor 5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor

View All CDK Isoform Specific Products:

View All Isoforms

CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

View All PARP Isoform Specific Products:

View All Isoforms

PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

H₁ Receptor

Chk2

CDK1

CDK2

CDK3

In Vitro

Cyproheptadine (0-30 μM; 3-24 h) hydrochloride sesquihydrate reduces cyclin D1, D2, and D3 protein and mRNA levels in human multiple myeloma (LP-1, KMS11, OCI-MY5, U266, MM1.R, OPM1, KMS12) and leukemia (OCI-AML2, OCI-AML3, HL60, OCI-M2, NB4, Jurkat) cell lines in a time- and concentration-dependent manner^[2].
Cyproheptadine (0-20 μM) hydrochloride sesquihydrate arrests human multiple myeloma (LP-1, MM1.S, MM1.R, KMS11) and leukemia (OCI-AML2, Jurkat) cell lines in the G0/G1 phase, reduces cellular proliferation, increases p21 expression, and decreases AP2A expression in a time- and concentration-dependent manner^[2].
Cyproheptadine (0-30 μM; 24-72 h; 7-14 days) hydrochloride sesquihydrate reduces viability and induces apoptosis in human multiple myeloma and leukemia cell lines and primary patient samples, inhibits clonogenic growth of primary AML samples, and exhibits reduced toxicity toward normal human hematopoietic stem cells, with cytotoxic effects occurring in a time- and concentration-dependent manner^[2].
Cyproheptadine (0-30 μM; 24-48 h) hydrochloride sesquihydrate induces caspase-dependent apoptosis in human multiple myeloma (OCI-MY5, OPM1, U266, LP-1) and leukemia (OCI-AML2, CEM, NB4) cell lines and murine leukemia (MDAY-D2) cells via activation of the mitochondrial pathway of caspase activation^[2].

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

Cell Viability Assay^[1]

Cell Line:	HepG2 and Huh-7 cells
Concentration:	20, 40, 60, 80, 100, 120 μM
Incubation Time:	24 h
Result:	Inhibited cell proliferation in a dose-dependent manner. Showed IC₅₀ of 44.4 and 44.7 μM in HepG2 cells and Huh-7 cells, respectively.

In Vivo

Cyproheptadine (36 mg/kg; i.p.; daily; 7 weeks) hydrochloride sesquihydrate reduces tumor volume in a subcutaneous multiple myeloma xenograft model^[2].
Cyproheptadine (10 mg/kg; i.p.; once daily; for 10 consecutive days) hydrochloride sesquihydrate reduces the expression level of Cyclin D2 protein in a subcutaneous multiple myeloma xenograft model^[2].
Cyproheptadine (10 mg/kg; i.p.; once daily; for 5 consecutive days) hydrochloride sesquihydrate reduces the protein expression levels of cyclin D2 and cyclin D3 in subcutaneous leukemia xenograft models^[2].
Cyproheptadine (40 mg/kg; i.p.; once daily for 7 consecutive days) hydrochloride sesquihydrate completely eliminates malignant ascites formation in a mouse intraperitoneal leukemia model^[2].

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

Animal Model:	NOD/SCID (sublethally irradiated with 3.5 Gy)^[2]
Dosage:	36 mg/kg
Administration:	i.p.; daily; 7 weeks
Result:	Delayed tumor growth, resulting in an approximately 2-fold reduction in tumor volume at the end of the 7-week treatment period. Showed statistical significance at 35 days (P = .048) and 49 days (P = .032) post-treatment initiation.

Animal Model:	NOD/SCID (sublethally irradiated with 3.5 Gy)^[2]
Dosage:	10 mg/kg
Administration:	i.p.; daily; 10 days
Result:	Decreased cyclin D2 protein expression in xenografted LP-1 tumors compared to vehicle control tumors, as detected by immunoblotting.

Animal Model:	NOD/SCID (sublethally irradiated with 3.5 Gy)^[2]
Dosage:	10 mg/kg
Administration:	i.p.; daily; 5 days
Result:	Decreased cyclin D2 and cyclin D3 protein expression in xenografted MDAY-D2 tumors compared to vehicle control tumors, as detected by immunoblotting.

Animal Model:	DBA2^[2]
Dosage:	40 mg/kg
Administration:	i.p.; daily; 7 days
Result:	Completely abolished formation of malignant ascites; no measurable ascites volume or malignant cell count was detected in treated mice, compared to vehicle control mice with median ascites volume of ~3 mL and median ascites cell count of ~1×10⁸ cells.

Molecular Weight

350.88

Formula

C₂₁H₂₁N.3/2H₂O.HCl

CAS No.

41354-29-4

Appearance

Solid

Color

White to off-white

SMILES

CN1CC/C(CC1)=C2C3=CC=CC=C3C=CC4=CC=CC=C/24.[H]Cl.O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (94.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 0.67 mg/mL (1.91 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8500 mL	14.2499 mL	28.4998 mL
5 mM	0.5700 mL	2.8500 mL	5.7000 mL
10 mM	0.2850 mL	1.4250 mL	2.8500 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (8.55 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (8.55 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 3 mg/mL (8.55 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 99.74%

Select Batch:

Data Sheet (283 KB) SDS (394 KB)

COA (253 KB) LCMS (103 KB)

Handling Instructions (2659 KB)

References

[1]. Feng YM, et al. Cyproheptadine, an antihistaminic drug, inhibits proliferation of hepatocellular carcinoma cells by blocking cell cycle progression through the activation of P38 MAP kinase. BMC Cancer. 2015;15:134. Published 2015 Mar 17. [Content Brief]

[2]. Mao X, et al. Cyproheptadine displays preclinical activity in myeloma and leukemia. Blood. 2008;112(3):760-769. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.8500 mL	14.2499 mL	28.4998 mL	71.2494 mL
DMSO	5 mM	0.5700 mL	2.8500 mL	5.7000 mL	14.2499 mL
	10 mM	0.2850 mL	1.4250 mL	2.8500 mL	7.1249 mL
	15 mM	0.1900 mL	0.9500 mL	1.9000 mL	4.7500 mL
	20 mM	0.1425 mL	0.7125 mL	1.4250 mL	3.5625 mL
	25 mM	0.1140 mL	0.5700 mL	1.1400 mL	2.8500 mL
	30 mM	0.0950 mL	0.4750 mL	0.9500 mL	2.3750 mL
	40 mM	0.0712 mL	0.3562 mL	0.7125 mL	1.7812 mL
	50 mM	0.0570 mL	0.2850 mL	0.5700 mL	1.4250 mL
	60 mM	0.0475 mL	0.2375 mL	0.4750 mL	1.1875 mL
	80 mM	0.0356 mL	0.1781 mL	0.3562 mL	0.8906 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.