2. Cell Cycle/DNA Damage Others Apoptosis
  3. Topoisomerase Drug Derivative MDM-2/p53
  4. Silatecan

Silatecan (AR-67) is a blood-brain barrier-permeable derivative of Camptothecin (HY-16560), DNA topoisomerase I inhibitor, an anticancer agent, and a radiosensitizer. Silatecan potently radiosensitizes wild-type p53 gliomas. Silatecan can be used in research related to glioma, leukemia, non-small cell lung cancer, colon cancer, ovarian cancer, renal cancer, prostate cancer, breast cancer, cervical cancer, gastric cancer, nasopharyngeal cancer, and uterine cancer.

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

Silatecan

Silatecan Chemical Structure

CAS No. : 220913-32-6

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Silatecan Related Antibodies

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Topoisomerase Topo I Topo II DNA gyrase

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Description

Silatecan (AR-67) is a blood-brain barrier-permeable derivative of Camptothecin (HY-16560), DNA topoisomerase I inhibitor, an anticancer agent, and a radiosensitizer. Silatecan potently radiosensitizes wild-type p53 gliomas. Silatecan can be used in research related to glioma, leukemia, non-small cell lung cancer, colon cancer, ovarian cancer, renal cancer, prostate cancer, breast cancer, cervical cancer, gastric cancer, nasopharyngeal cancer, and uterine cancer[1][2][3].

IC50 & Target[1]

Topoisomerase I

 

Cellular Effect
Cell Line Type Value Description References
MDA-MB-435 IC50
14 nM
Compound: 14
Inhibition against MDA-MB-435 S human breast cancer cells in the absence of albumin
Inhibition against MDA-MB-435 S human breast cancer cells in the absence of albumin
[PMID: 11052802]
Tumor Cell line GI50
21 nM
Compound: 14
Mean GI50 against variety of human tumor cell lines
Mean GI50 against variety of human tumor cell lines
[PMID: 11052802]
In Vitro

Silatecan (10 μg/mL; 0-6 h) exhibits better lactone stability in BALB/c mouse plasma than CPT-11 (HY-16562), Topotecan (HY-13768) and CPT (HY-16560), with a 50% degradation time of 30 min, and 20% of its lactone form remains after 6 h of incubation[2].
Silatecan (at various concentrations; 72 h) potently inhibits the growth of multiple cancer cell lines, including drug-resistant sublines (e.g., gastric cancer MKN45, nasopharyngeal carcinoma TW-039)[2].
Silatecan (0.001-10 μg/mL; 96 h) inhibits the proliferation of colorectal cancer SW480 cells, gastric cancer MKN45 cells, nasopharyngeal carcinoma TW039 cells, uterine cancer MES-SA cells, and Doxorubicin (HY-15142A)-resistant MES-SA/Dx5 cells in vitro tissue culture in a concentration-dependent manner, with IC50 values ranging from 0.03 μM (TW039) to 2.21 μM (SW480)[2].
Silatecan (0.1-1.0 μM; 30 min) potently radiosensitizes wild-type p53 glioma D54-MG cells by eliminating the shoulder region of radiation survival curves; its SER reaches 1.4 at concentrations of 0.1 or 0.2 μM[3].
Silatecan (0.1 μM; 30 min) mildly radiosensitizes glioma T98G cells carrying mutant p53, with an SER of 1.2 at the concentration of 0.1 μM, but its sensitizing effect is weaker than that on D54-MG cells carrying wild-type p53[3].
Silatecan (30 min) is a potent cytotoxic agent in wild-type TOP1 Chinese hamster lung fibroblast DC3F cells (LD50 = 0.05 μM)[3].

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

Silatecan Related Antibodies

Cell Cytotoxicity Assay[2]

Cell Line: human cervical KB, Topo I-overexpressed KB-100, P-gp170/MDR-overexpressed vinblastine-resistant KB-VIN10, P-gp170/MDR-overexpressed paclitaxel-resistant KB-TAX50, gastric MKN45, colorectal SW480, breast MCF-7, hepatic HepG2, nasopharyngeal TW-039, uterine MES-SA, doxorubicin-resistant uterine MES-SA/Dx5
Concentration: Various concentrations
Incubation Time: 72 h
Result: Exhibited IC50 values of 35 nM (KB), 750 nM (KB-100), 2271 nM (KB-VIN10), 50 nM (KB-TAX50).

Western Blot Analysis[3]

Cell Line: human glioma D54-MG cells
Concentration: 5 μM, 10 μM
Incubation Time: 30 min
Result: Depleted free cellular TOP1 in a dose-dependent manner, indicating stimulation of covalent TOP1-DNA complex formation.
Was 10-fold more potent than camptothecin for this effect, as 5 μM induced greater TOP1 depletion than 50 μM camptothecin.
Left TOP2 and β-actin levels unaffected, demonstrating specificity for TOP1.
Parmacokinetics
Species Dose Route T1/2 (Distribution) T1/2β CL Vdss
Mice[2] 8 mg/kg i.v. 8 min 33 min 37 mL/min/kg 0.7 L/kg
In Vivo

Silatecan (DB-67) (3-30 mg/kg/day; daily; 5 days to four 21-day cycles) dose-dependently inhibits subcutaneous U87 glioma xenograft growth in nude mice, with 30 mg/kg/day inducing complete tumor regression and no overt toxicity[1].
Silatecan (3-10 mg/kg; i.v.; daily; two 5-consecutive-day cycles) exerts dose-dependent in vivo antitumor activity against subcutaneous human colorectal SW480 xenografts in male BALB/c nude mice, with significant tumor growth inhibition observed at 3 mg/kg and 10 mg/kg intravenous doses[2].
Silatecan (3.3-10 mg/kg; i.v.; daily; two 5-consecutive-day cycles) exerts dose-dependent in vivo antitumor activity against subcutaneous gastric MKN45 xenografts in male BALB/c nude mice, with significant tumor growth inhibition observed at 3.3 mg/kg and 10 mg/kg intravenous doses[2].

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

Animal Model: Nude mice[1]
Dosage: 3 mg/kg/day; 10 mg/kg/day; 30 mg/kg/day
Administration: daily; 5 days (3 mg/kg, 10 mg/kg); daily; four 21-day cycles (10 mg/kg); daily; two cycles (30 mg/kg)
Result: Achieved 61% tumor growth inhibition at day 28 post-implantation.
Achieved 73% tumor growth inhibition at day 28 post-implantation.
Kept mice progression-free for over 90 days before tumor regrowth after treatment cessation.
Induced complete tumor regression in all animals, even when initiated after large tumors had developed.
Caused no overt toxicity in any treated animals.
Animal Model: BALB/c nude (male, adult, human colorectal SW480 cancer cells implanted subcutaneously)[2]
Dosage: 3 mg/kg; 10 mg/kg
Administration: i.v.; daily; two 5-consecutive-day cycles (days 1-5 and days 22-26)
Result: Dose-dependently suppressed the growth of human colorectal SW480 tumor xenografts, with significant differences in tumor size compared to the vehicle control group (p < 0.05) by day 60 post-dosing.
Animal Model: BALB/c nude (male, adult, human gastric MKN45 cancer cells implanted subcutaneously)[2]
Dosage: 3.3 mg/kg; 10 mg/kg
Administration: i.v.; daily; two 5-consecutive-day cycles (days 1-5 and days 22-26)
Result: Dose-dependently suppressed the growth of human gastric MKN45 tumor xenografts, with significant differences in tumor size compared to the vehicle control group (p < 0.05) by day 40 post-dosing.
Clinical Trial
Molecular Weight

478.61

Formula

C26H30N2O5Si
CAS No.
Appearance

Solid

Color

Yellow to brown

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture and light

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (208.94 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0894 mL 10.4469 mL 20.8938 mL
5 mM 0.4179 mL 2.0894 mL 4.1788 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 and 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

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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: ≥ 2.5 mg/mL (5.22 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.

    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: 2.5 mg/mL (5.22 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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 and light)

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
References

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 and light). 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 2.0894 mL 10.4469 mL 20.8938 mL 52.2346 mL
5 mM 0.4179 mL 2.0894 mL 4.1788 mL 10.4469 mL
10 mM 0.2089 mL 1.0447 mL 2.0894 mL 5.2235 mL
15 mM 0.1393 mL 0.6965 mL 1.3929 mL 3.4823 mL
20 mM 0.1045 mL 0.5223 mL 1.0447 mL 2.6117 mL
25 mM 0.0836 mL 0.4179 mL 0.8358 mL 2.0894 mL
30 mM 0.0696 mL 0.3482 mL 0.6965 mL 1.7412 mL
40 mM 0.0522 mL 0.2612 mL 0.5223 mL 1.3059 mL
50 mM 0.0418 mL 0.2089 mL 0.4179 mL 1.0447 mL
60 mM 0.0348 mL 0.1741 mL 0.3482 mL 0.8706 mL
80 mM 0.0261 mL 0.1306 mL 0.2612 mL 0.6529 mL
100 mM 0.0209 mL 0.1045 mL 0.2089 mL 0.5223 mL
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Silatecan 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:

Silatecan220913-32-6AR-67 DB 67AR67AR 67DB67DB 67DB-67TopoisomeraseDrug DerivativeMDM-2/p53Drug derivativeovarian cancerrenal cancernon-small cell lung cancerTOP1-DNA cleavable complexesCNS cancermelanomagliomaDNA topoisomerase Icolon cancerleukemiaInhibitorinhibitorinhibit

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