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Cat. No.: HY-183741

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VVD-844

VVD-844 is an orally active covalent inhibitor of PI3Kα, which inhibits Pl3Kα/p110α interaction with an IC₅₀ of 4 nM. VVD-844 covalently binds to Cys²⁴² in the RAS binding domain of p110α, blocking RAS-p110α interaction and inhibiting PI3Kα activity. VVD-844 inhibits PI3Kα signaling activation in HER2-overexpressing cells via a RAS-independent mechanism. VVD-844 suppresses tumor growth in mouse. VVD-844 can be used for the research of cancers.

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CAS No.: 3080226-63-4
화학식: C₂₁H₂₂ClFN₄O₃S
분자량:464.94

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

VVD-844 Chemical Structure

CAS No.: 3080226-63-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

PI3Kα

All PI3K Isoforms :

All Akt Isoforms :

In Vitro

VVD-844 (10 nM; 2-24 h) inhibits PI3K/AKT signaling in KPAR (KRAS^G12C) mouse lung cancer cells^[1].
VVD-844 inhibits phosphorylated-Ser⁴⁷³-AKT (pAKT pathway with an lC₅₀ of 11 nM^[1].

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

Western Blot Analysis^[1]

Cell Line:

KPAR (KRASG12C) mouse lung cancer cells
Concentration:

10 nM
Incubation Time:

2; 24 h
Result:

Decreased pAKT (S473) levels.
Decreased pERK1/2 levels when combined with Adagrasib (HY-130149).

In Vivo

VVD-844 (10 mg/kg; p.o.; b.i.d.) inhibits tumor growth in mouse CTG3196 and CR2528 PDX models^[1].

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

Animal Model:

Nu/Nu mice (6-8
weeks) subcutaneously inoculated with CTG3196 tumor^[1]
Dosage:

10 mg/kg
Administration:

p.o.; b.i.d.
Result:

Inhibited tumor growth compared to control.

Animal Model:

Nu/Nu mice (6-8
weeks) subcutaneously inoculated with CR2528 tumor^[1]
Dosage:

10 mg/kg
Administration:

p.o.; b.i.d.
Result:

Inhibited tumor growth compared to control.

Chemical Information

CAS No. 3080226-63-4
분자량 464.94
화학식 C₂₁H₂₂ClFN₄O₃S
SMILES

ClC1=C(C=CC=C1F)[C@@H]2[C@@]3([H])[C@](CN2C4=NC=C(C(N[C@H](C)/C=C/S(C)(=O)=O)=O)N=C4)([H])C3
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[1]. Klebba JE, et al. Covalent inhibitors of the PI3Kα RAS binding domain impair tumor growth driven by RAS and HER2. Science. 2025 Nov 13;390(6774):702-709. [Content Brief]

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

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VVD-844

All PI3K Isoforms

All Akt Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

VVD-844 Related Classifications

HY-183741 Related Classifications