PHGDH-IN-3 - ≥98% , CAS No.2893778-31-7

CAS: 2893778-31-7 Cat. No.: P647846 분자식: C₂₄H₁₈FN₃O₄S₂ 분자량: 495.55

GRADE & PURITY ≥98%

Storage

Protected from light,Store at -80°C

Shipped In

Dry ice packs + Cold packs

개요

PHGDH-IN-3 is an orally active phosphoglycerate dehydrogenase (PHGDH) inhibitor. PHGDH-IN-3 inhibits PHGDH with an IC 50 value of 2.8 μM. PHGDH-IN-3 can be used for the research of cancer

In Vitro

PHGDH-IN-3 (compound D8) has good enzymatic inhibitory activity with an IC 50 value of 2.8 μM. PHGDH-IN-3 has high binding affinity for the PHGDH protein with a K d value of 2.33 μM. PHGDH-IN-3 has sensitivity to the cell lines with the PHGDH gene amplification or overexpression. PHGDH-IN-3 can restrict the de novo serine synthesis from glucose within MDA-MB-468 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PHGDH-IN-3 (compound D8) (p.o., i.v.; 1, 3 mg/kg) exhibits excellent in vivo pharmacokinetic properties . PHGDH-IN-3 (i.p.; 12.5, 25, 50 mg/kg; once daily for consecutive 31 days) exertes evident antitumor efficacy in the PC9 xenograft mouse model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: ICR mice Dosage: 1, 3 mg/kg Administration: Oral (p.o.) and intravenous (i.v.) administration Result: PK parameters i.v. (1 mg/kg) p.o. (3 mg/kg) AUC (h•ng/mL) 38,358 ± 14,768 94,386 ± 23,416 T 1/2 (h) 4.94 ± 0.38 4.74 ± 0.30 T max (h) 3.33 ± 1.15 CL _obs (mL/min/kg) 0.48 ± 0.23 C max (ng/mL) 8842 ± 1755 F (%) 82.0 Animal Model: Balb/c nude mice Dosage: 12.5, 25, 50 mg/kg Administration: Intraperitoneal (i.p.); once daily for consecutive 31 days Result: Exhibited an in vivo anti-tumor effect and significantly delayed the tumor growth. Significantly abated the tumor weights of mice at 25 mg/ kg.

Form:Solid

IC50& Target:IC50: 2.8 μM (PHGDH),Kd: 2.33 μM (PHGDH)

Specifications

사양 및 순도

≥98%

생화학 및 생리적 메커니즘

PHGDH-IN-3 is an orally active phosphoglycerate dehydrogenase (PHGDH) inhibitor. PHGDH-IN-3 inhibits PHGDH with an IC 50 value of 2.8 μM. PHGDH-IN-3 can be used for the research of cancer.

보관 조건

Protected from light,Store at -80°C

배송

Dry ice packs + Cold packs

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작업 유형

INHIBITOR

순수함

≥98%

이름과 식별자

분자량

495.55

화학 및 물리적 특성

• 용해성: DMSO : 100 mg/mL (201.80 mM; ultrasonic and warming and heat to 70°C)

자주 묻는 질문

What is the purity of this product?

This product is supplied at ≥98% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?80 °C, protected from light. The material is light-sensitive — keep it in its original opaque or amber container.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2893778-31-7, the molecular formula is C24H18FN3O4S2, and the molecular weight is 495.55 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.