SPH5030

Name: SPH5030
Brand: MedChemExpress
SKU: HY-143319
Rating: 4.5 (1 reviews)

Cat. No.: HY-143319 Purity: 99.40%: FAQs
Data Sheet SDS COA Handling Instructions

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SPH5030 is a selective and irreversible HER2 inhibitor. SPH5030 inhibits HER2^WT and EGFR^WT 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

CAS No. : 2364326-23-6

Size	Price	Stock	Quantity
5 mg	USD 870	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1400	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 2850	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 4600	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 3.51 nM (HER2^WT), 0.42 nM (HER2^D769H), 0.43 nM (HER2^D769Y), 0.16 nM (HER2^V777L), 0.56 nM (HER2^R896C), 8.13 nM (EGFR^WT)^[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.

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
t_1/2 (h)	3.76±0.15	3.60±0.59	4.56±0.20	4.38±0.35
V_ss (L/kg)	2.96±0.96		3.55±0.64
C_max (μg/mL)		1.90±0.14		0.76±0.33
t_max (h)		2.67±1.15		3.33±1.15
AUC_0-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.

2364326-23-6

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
10 mM	0.1716 mL	0.8582 mL	1.7164 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.

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 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.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.40%

Select Batch:

Data Sheet (276 KB) SDS (252 KB)

COA (249 KB) HNMR (278 KB) RP-HPLC (226 KB) LCMS (224 KB)

Handling Instructions (2659 KB)

References

[1]. Li D,et al. Discovery of SPH5030, a Selective, Potent, and Irreversible Tyrosine Kinase Inhibitor for HER2-Amplified and HER2-Mutant Cancer Treatment. J Med Chem. 2022 Apr 14;65(7):5334-5354. [Content Brief]

Complete Stock Solution Preparation Table

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

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-5030EGFREpidermal growth factor receptorErbB-1HER1NCI-N87irreversibleanti-tumormutantneratinibpyrotinibInhibitorinhibitorinhibit

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SPH5030

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SPH5030 Related Antibodies

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Complete Stock Solution Preparation Table

SPH5030 Related Classifications

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