Cat. No.: HY-77554

Cephalomannine

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Cephalomannine is a Paclitaxel (HY-B0015) alkaloidal analog that can be isolated from most Cephalotaxus species. Cephalomannine is an orally active anti-tumor agent and can be used as a chemotherapy agent for cancer research.

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

Purity: 99.04%
CAS No.: 71610-00-9
Formula: C₄₅H₅₃NO₁₄
Molecular Weight:831.90

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Cephalomannine Chemical Structure

CAS No.: 71610-00-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

HIF-1α

All HIF/HIF Prolyl-Hydroxylase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.1 μM Compound: 1	Cytotoxicity against human A2780 cells by MTT assay Cytotoxicity against human A2780 cells by MTT assay	[PMID: 18001087]
A2780	IC₅₀	0.013 μM Compound: 4	Antiproliferative activity against human A2780 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay Antiproliferative activity against human A2780 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 25682561]
A549	IC₅₀	0.1 μM Compound: 1	Cytotoxicity against human A549 cells by MTT assay Cytotoxicity against human A549 cells by MTT assay	[PMID: 18001087]
A549	IC₅₀	0.005 μM Compound: 4	Antiproliferative activity against human A549/CDDP cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay Antiproliferative activity against human A549/CDDP cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 25682561]
A549	IC₅₀	0.008 μM Compound: 4	Antiproliferative activity against human A549 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay Antiproliferative activity against human A549 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 25682561]
Bel-7402	IC₅₀	0.92 μM Compound: 1	Cytotoxicity against human Bel7402 cells by MTT assay Cytotoxicity against human Bel7402 cells by MTT assay	[PMID: 18001087]
BGC-823	IC₅₀	0.1 μM Compound: 1	Cytotoxicity against human BGC823 cells by MTT assay Cytotoxicity against human BGC823 cells by MTT assay	[PMID: 18001087]
HCT-8	IC₅₀	0.31 μM Compound: 1	Cytotoxicity against human HCT8 cells by MTT assay Cytotoxicity against human HCT8 cells by MTT assay	[PMID: 18001087]
HCT-8	IC₅₀	>25 μM Compound: 4	Antiproliferative activity against human HCT8 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay Antiproliferative activity against human HCT8 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 25682561]
HepG2	IC₅₀	0.02 μM Compound: 4	Antiproliferative activity against human HepG2 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay Antiproliferative activity against human HepG2 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 25682561]
IGROV-1	IC₅₀	0.3 μM Compound: 4	Antiproliferative activity against human IGROV1 cells assessed as growth inhibition after 72 hrs by Coulter counting analysis Antiproliferative activity against human IGROV1 cells assessed as growth inhibition after 72 hrs by Coulter counting analysis	[PMID: 19833515]
KB	IC₅₀	0.0015 μg/mL Compound: 55	Cytotoxicity against human KB cells Cytotoxicity against human KB cells	[PMID: 14987066]
KB	ED₅₀	3.8 ng/mL Compound: 2	Cytotoxicity against human KB cells Cytotoxicity against human KB cells	[PMID: 19209890]
KB	ED₅₀	3.8 x 10^-3 μg/mL Compound: 2	Cytotoxicity against human KB cells Cytotoxicity against human KB cells	[PMID: 19209890]
KB	ED₅₀	3.8 ng/mL Compound: 2	Cytotoxicity against human KB cells Cytotoxicity against human KB cells	[PMID: 7264680]
KB	ED₅₀	3.8 x 10^-3 μg/mL Compound: 2	Cytotoxicity against human KB cells Cytotoxicity against human KB cells	[PMID: 7264680]
MCF7	IC₅₀	6 nM Compound: cephalomannine	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 11325226]
MCF7	IC₅₀	0.004 μM Compound: 4	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 25682561]
NIH3T3	IC₅₀	0.6 μM Compound: 4	Antiproliferative activity against mouse NIH/3T3 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay Antiproliferative activity against mouse NIH/3T3 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 25682561]
SW480	IC₅₀	0.033 μM Compound: 4	Antiproliferative activity against human SW480 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay Antiproliferative activity against human SW480 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 25682561]

In Vitro

Cephalomannine significantly inhibits the proliferation of H460, A549 and H1299 cells under normal oxygen conditions, with IC₅₀ values of 0.18, 0.20 and 0.37 μM, respectively. Cephalomannine shows obvious inhibitory effect on cell viability under hypoxia^[3].
Cephalomannine (0, 0.025, 0.05, 0.1 μM; 0, 12, 24h) inhibiting the interaction of APEX1/HIF-1α can also significantly inhibit the cell viability, ROS production, intracellular pH, migration of hypoxic lung cancer cells, and angiogenesis of hypoxic human umbilical vein endothelial cells (HUVECs)^[3].
Cephalomannine dose-dependently inhibits UBE2S expression and thus suppresses prostate cancer (PCa) growth and metastasis^[4].

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

Cell Line:
Concentration:
Incubation Time:
Result:

RT-PCR^[3]

Cell Line:

H460 and A549 cell lines
Concentration:

0, 0.025, 0.05, 0.1 μM
Incubation Time:

0, 12, 24h
Result:

After 24 h, the relative expression of APEX1 and HIF-1α was significantly inhibited.

Immunofluorescence^[3]

Cell Line:

H460 and A549 cell lines
Concentration:

0, 0.025, 0.05, 0.1 μM
Incubation Time:

0, 12, 24h
Result:

HIF-1α levels were increased in hypoxic lung cancer cells.

Western Blot Analysis^[3]

Cell Line:

H460 and A549 cell lines
Concentration:

0, 0.025, 0.05, 0.1 μM
Incubation Time:

0, 12, 24h
Result:

The expression of APEX1 and HIF-1α was decreased.

In Vivo

Cephalomannine (0.4 mg/kg, intraperitoneal injection, 10 days) could significantly inhibit the growth of lung cancer cells in nude mice xenograft model, with no obvious side effects^[3].
Cephalomannine can interrupt the interaction between APEX1 and HIF-1α by competitive binding with APEX1^[3].

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

Animal Model:

BALB/C nude mice xenograft model^[3]
Dosage:

0.4 mg/kg
Administration:

Intraperitoneal injection (i.p.)
Result:

Reduced the volume and weight of H460 xenograft tumors.

Animal Model:

BALB/c nude mice bone metastasis xenograft model^[4]
Dosage:

10 mg/kg, 20 mg/kg
Administration:

Intraperitoneal injection (i.p.)
Result:

Decreased bone destruction, reduced bioluminescence intensity and number of bone metastases, significantly extended time to endpoint events, decreased UBE2S expression and number of osteoclasts, and did not produce significant toxicity to the heart, liver, or kidney of nude mice.

Chemical Information

CAS No. 71610-00-9
Appearance Solid
Molecular Weight 831.90
Formula C₄₅H₅₃NO₁₄
Color White to off-white
SMILES

O=C(/C(C)=C/C)N[C@@H](C1=CC=CC=C1)[C@H](C(O[C@@H]2C(C)=C([C@@H](OC(C)=O)C([C@@]3(C)[C@]([C@](OC(C)=O)(CO4)[C@H]4C[C@@H]3O)([H])[C@@H]5OC(C6=CC=CC=C6)=O)=O)C(C)(C)[C@@]5(O)C2)=O)O
Structure Classification
- Terpenoids
- Diterpenoids
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (120.21 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

1.2021 mL

6.0103 mL

12.0207 mL

5 mM

0.2404 mL

1.2021 mL

2.4041 mL

10 mM

0.1202 mL

0.6010 mL

1.2021 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (3.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (3.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, 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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (555 KB)
- English - EN (555 KB)
- Français - FR (555 KB)
- Deutsch - DE (555 KB)
- Norwegian - NO (555 KB)
- Español - ES (555 KB)
- Swedish - SV (555 KB)
- Italian - IT (555 KB)
- Korean - KR (555 KB)
- Portuguese - PT (555 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]. Feng Gao, et al. Synthesis, isolation, stereostructure and cytotoxicity of paclitaxel analogs from cephalomannine.Fitoterapia. 2013 Oct;90:79-84. [Content Brief]

[2]. Jianhua Li, et al. Microbial transformation of cephalomannine by Luteibacter sp. J Nat Prod. 2007 Dec;70(12):1846-9. [Content Brief]

[3]. Ullah, Asmat et al. Cephalomannine inhibits hypoxia-induced cellular function via the suppression of APEX1/HIF-1α interaction in lung cancer. Cell death & disease vol. 2021;12(5):490. [Content Brief]

[4]. Peng S, et al. UBE2S as a novel ubiquitinated regulator of p16 and β-catenin to promote bone metastasis of prostate cancer. Int J Biol Sci. 2022 May 16;18(8):3528-3543.

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.2021 mL	6.0103 mL	12.0207 mL	30.0517 mL
	5 mM	0.2404 mL	1.2021 mL	2.4041 mL	6.0103 mL
	10 mM	0.1202 mL	0.6010 mL	1.2021 mL	3.0052 mL
	15 mM	0.0801 mL	0.4007 mL	0.8014 mL	2.0034 mL
	20 mM	0.0601 mL	0.3005 mL	0.6010 mL	1.5026 mL
	25 mM	0.0481 mL	0.2404 mL	0.4808 mL	1.2021 mL
	30 mM	0.0401 mL	0.2003 mL	0.4007 mL	1.0017 mL
	40 mM	0.0301 mL	0.1503 mL	0.3005 mL	0.7513 mL
	50 mM	0.0240 mL	0.1202 mL	0.2404 mL	0.6010 mL
	60 mM	0.0200 mL	0.1002 mL	0.2003 mL	0.5009 mL
	80 mM	0.0150 mL	0.0751 mL	0.1503 mL	0.3756 mL
	100 mM	0.0120 mL	0.0601 mL	0.1202 mL	0.3005 mL

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Cephalomannine

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All HIF/HIF Prolyl-Hydroxylase Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Cephalomannine Related Classifications

HY-77554 Related Classifications