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SPH5030 is a selective and irreversible HER2 inhibitor. SPH5030 inhibits HER2WT and EGFRWT with IC50s of 3.51 and 8.13 nM, respectively. SPH5030 shows excellent activities against HER2 mutants. SPH5030 can be used for the research of cancer.

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

SPH5030 Chemical Structure

SPH5030 Chemical Structure

CAS No. : 2364326-23-6

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1 mg USD 625 In-stock
5 mg USD 1875 In-stock
10 mg USD 3180 In-stock
25 mg USD 5800 In-stock
50 mg USD 8700 In-stock
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Based on 1 publication(s) in Google Scholar

SPH5030 Related Antibodies

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Description

SPH5030 is a selective and irreversible HER2 inhibitor. SPH5030 inhibits HER2WT and EGFRWT with IC50s of 3.51 and 8.13 nM, respectively. SPH5030 shows excellent activities against HER2 mutants. SPH5030 can be used for the research of cancer[1].

IC50 & Target

IC50: 3.51 nM (HER2WT), 0.42 nM (HER2D769H), 0.43 nM (HER2D769Y), 0.16 nM (HER2V777L), 0.56 nM (HER2R896C), 8.13 nM (EGFRWT)[1]
In Vitro

SPH5030 (0-10 μM; 72 h) shows anti-proliferation activities against tumor cell lines[1].

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

SPH5030 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: NCI-N87, BT-474, SK-BR-3 with HER2 overexpression, MDA-MB-468 with EGFR overexpression, NCI-H441, Es-2, MFE-280, NUGC-4, COLO678, KM12-luc and BaF3 cell lines
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Effectively inhibited NCI-N87, BT-474, SK-BR-3 with HER2 overexpression and BaF3 cells with IC50s of 1.09, 2.01, 20.09 and 6.3 nM, respectively. Poorly inhibited MDA-MB-468 with EGFR overexpression, NCI-H441, Es-2, MFE-280, NUGC-4, COLO678 and KM12-luc cells with IC50s of 2980, 4257, 2716, 3967, 1218, 6065 and 3597 nM, respectively.
In Vivo

SPH5030 (5-40 mg/kg; p.o. once per day for 13 or 21 days) shows in vivo antitumor efficacy in mice with xenograft tumor models[1].
1.19 Pharmacokinetic Properties of SPH5030 in Mice and Rats[1].

Mice
IV 3 mg/kg		 Mice
PO 10 mg/kg		 Rats
IV 3 mg/kg		 Rats
PO 6 mg/kg
CL (L/kg·h) 0.70±0.20 0.78±0.13
t1/2 (h) 3.76±0.15 3.60±0.59 4.56±0.20 4.38±0.35
Vss (L/kg) 2.96±0.96 3.55±0.64
Cmax (μg/mL) 1.90±0.14 0.76±0.33
tmax (h) 2.67±1.15 3.33±1.15
AUC0-t (h·μg/mL) 13.07±0.48 5.47±2.82
F (%) 87.66 71.35

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

Animal Model: BALB/c nude mouse with NCI-N87 and BT474 xenografts, and NPSG mouse with BAF3 HER2 A775_G776insYVMA xenografts[1]
Dosage: 5, 10, 20 and 40 mg/kg
Administration: Oral gavage; 5-40 mg/kg once per day; for 13 or 21 days
Result: Dose-dependently inhibited tumor growth in NCI-N87, BT474 and BAF3 HER2 A775_G776insYVMA xenograft mouse models, and showed an equivalent or better activity of tumor inhibition compared with neratinib and pyrotinib at a dose of 20 mg/kg. Showed no mortality or significant loss of body weight in xenograft mouse models.
Clinical Trial
Molecular Weight

582.63

Formula

C31H31FN8O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CCOC1=C(C=C2C(N=CN=C2NC3=CC(C)=C(C=C3)OC4=CC5=NC=NN5C=C4)=C1)NC(/C(F)=C/[C@H]6CCCN6C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (171.64 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 1.7164 mL 8.5818 mL 17.1636 mL
5 mM 0.3433 mL 1.7164 mL 3.4327 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, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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
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, stored under nitrogen). 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 1.7164 mL 8.5818 mL 17.1636 mL 42.9089 mL
5 mM 0.3433 mL 1.7164 mL 3.4327 mL 8.5818 mL
10 mM 0.1716 mL 0.8582 mL 1.7164 mL 4.2909 mL
15 mM 0.1144 mL 0.5721 mL 1.1442 mL 2.8606 mL
20 mM 0.0858 mL 0.4291 mL 0.8582 mL 2.1454 mL
25 mM 0.0687 mL 0.3433 mL 0.6865 mL 1.7164 mL
30 mM 0.0572 mL 0.2861 mL 0.5721 mL 1.4303 mL
40 mM 0.0429 mL 0.2145 mL 0.4291 mL 1.0727 mL
50 mM 0.0343 mL 0.1716 mL 0.3433 mL 0.8582 mL
60 mM 0.0286 mL 0.1430 mL 0.2861 mL 0.7151 mL
80 mM 0.0215 mL 0.1073 mL 0.2145 mL 0.5364 mL
100 mM 0.0172 mL 0.0858 mL 0.1716 mL 0.4291 mL
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SPH5030 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:

SPH50302364326-23-6SPH 5030SPH-5030OthersNCI-N87irreversibleanti-tumormutantneratinibpyrotinibInhibitorinhibitorinhibit

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