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| SKU | Size | Availability |
Price | Qty |
|---|---|---|---|---|
|
V650429-1mg
|
1mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
$258.90
|
|
|
V650429-5mg
|
5mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
$650.90
|
|
|
V650429-10mg
|
10mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
$1,041.90
|
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| Specifications & Purity | ≥99% |
|---|---|
| Biochemical and Physiological Mechanisms | Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC 50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα , PI3Kβ , PI3Kγ and PI3Kδ , respectively. Antiproliferative and antineoplastic activity. |
| Storage Temp | Store at -20°C |
| Shipped In |
Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available. |
| Product Description |
Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC 50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα , PI3Kβ , PI3Kγ and PI3Kδ , respectively. Antiproliferative and antineoplastic activity In Vitro Vulolisib has antiproliferative activity against PI3Kα-mutant cell lines HCC1954 (H1047R), HGC-27 (E542K) and MKN1 (E545K) with IC 50 s of 21 nM, 60 nM and 40 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Vulolisib (10, 30 and 60 mg/kg; IG; daily for 7days) exhibits better tolerance and exposure than Inavolisib . Vulolisib (10mg/kg; PO; daily for 19 days) inhibits tumor growth with TGI of 132% . Vulolisib (5 mg/kg; IG, single dosage) exhibits favorable pharmacokinetic property . Pharmacokinetic Parameters of Vulolisib in male Balb/c mice . IG (5 mg/kg) t max (h) 0.5 C max (ng/mL) 1057 AUC 0-t (ng/mL·h) 2185 AUC 0-∞ (ng/mL·h) 2274 t 1/2 (h) 1.6 MRT (h) 2.2 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Sprague-Dawley rats Dosage: 10, 30 and 60 mg/kg Administration: IG; daily for 7days Result: Exhibited better tolerance and exposure than Inavolisib. Animal Model: Female BALB/c nude mice (6-8 weeks; injected with HCC1954) Dosage: 10mg/kg Administration: PO; daily for 19 days Result: Inhibited tumor growth with TGI of 132%. Animal Model: Male Balb/c mice Dosage: 5 mg/kg Administration: IG, single dosage (Pharmacokinetic Analysis) Result: Exhibited favorable pharmacokinetic property. Form:Solid IC50& Target:PI3Kα 0.2 nM (IC 50 ) PI3Kβ 168 nM (IC 50 ) PI3Kγ 90 nM (IC 50 ) PI3Kδ 49 nM (IC 50 ) |
| Smiles | C[C@@H](C(=O)N)NC1=CC2=C(C=C1)C3=NC(=CN3CCO2)N4[C@@H](CSC4=O)C(F)F |
|---|---|
| Isomeric SMILES | C[C@@H](C(=O)N)NC1=CC2=C(C=C1)C3=NC(=CN3CCO2)N4[C@@H](CSC4=O)C(F)F |
| PubChem CID | 146267141 |
| Molecular Weight | 423.44 |