2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. HSP
  4. CH5138303

CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model.

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

CH5138303 Chemical Structure

CH5138303 Chemical Structure

CAS No. : 959763-06-5

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1 mg USD 280 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model[1][2].

IC50 & Target

HSP90α

0.52 nM (Kd)

In Vitro

When used in combination with FLC, CH5138303 shows antifungal activitiy against azole-resistant C. albicans, with a FICI (fractional inhibitory concentration index) of 0.500[2].

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

CH5138303 Related Antibodies
In Vivo

CH5138303 (SCID mice bearing NCI-N87 cells, 0-50 mg/kg, Orally, once daily for 11 days) shows potent antitumor efficacy with TGI (tumor growth inhibition) of 136% and a median effective dose (ED50) of 3.9 mg/kg without significant loss of body weight[1].

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

415.90

Formula

C19H18ClN5O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N)CCCSC1=NC(N)=NC(C2=C(Cl)C=C3C4=C2C=CC=C4COC3)=N1
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 : ≥ 33 mg/mL (79.35 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 2.4044 mL 12.0221 mL 24.0442 mL
5 mM 0.4809 mL 2.4044 mL 4.8088 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 (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

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.05%

COA (251 KB) HNMR (211 KB) RP-HPLC (230 KB)

Handling Instructions (2659 KB)
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 (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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4044 mL 12.0221 mL 24.0442 mL 60.1106 mL
5 mM 0.4809 mL 2.4044 mL 4.8088 mL 12.0221 mL
10 mM 0.2404 mL 1.2022 mL 2.4044 mL 6.0111 mL
15 mM 0.1603 mL 0.8015 mL 1.6029 mL 4.0074 mL
20 mM 0.1202 mL 0.6011 mL 1.2022 mL 3.0055 mL
25 mM 0.0962 mL 0.4809 mL 0.9618 mL 2.4044 mL
30 mM 0.0801 mL 0.4007 mL 0.8015 mL 2.0037 mL
40 mM 0.0601 mL 0.3006 mL 0.6011 mL 1.5028 mL
50 mM 0.0481 mL 0.2404 mL 0.4809 mL 1.2022 mL
60 mM 0.0401 mL 0.2004 mL 0.4007 mL 1.0018 mL
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CH5138303 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:

CH5138303959763-06-5CH 5138303CH-5138303HSPHeat shock proteinsorally activeantitumor agentHsp90 inhibitorHCT116NCI-N87gastric cancerInhibitorinhibitorinhibit

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