XL147 analogue

Catalog No. A10995

XL147 analogue是一种有效的，选择性的，口服可生物利用的I类磷脂酰肌醇3激酶（PI3K）小分子抑制剂，作用于PI3Kα/δ/γ，对PI3Kβ作用效果稍弱。具有潜在的抗肿瘤活性。

Product Citations

Yushi Hayashida, .et al. Invention of a novel photodynamic therapy for tumors using a photosensitizing PI3K inhibitor, Int J Cancer, 2016, Aug 1;139(3):700-11 PMID: 26989815

Technical details

Catalog Num	A10995
M. Wt	448.5
Formula	C21H16N6O2S2
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	956958-53-5
Synonyms	XL-147, SAR245408
SMILES	CC1=CC=C(C=C1)S(=O)(=O)NC2=NC3=CC=CC=C3N=C2NC4=CC5=NSN=C5C=C4

Biological Activity

Targets

Target	Value
PI3Kγ	IC50: 23nM
PI3Kδ	IC50: 36nM
PI3Kα	IC50: 39nM
PI3Kβ	IC50: 383nM
DNA-PK	IC50: 4.75μM
Vps34	IC50: 6.975μM
MEK	IC50: >10μM
B-Raf/C-Raf	IC50: >10μM
mTOR	IC50: >15μM

Solubility *

In vitro (25°C)	DMSO	3 mg/mL (6.68 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	30% PEG400+0.5% Tween80+5% propylene glycol	14 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	22.3 mL	111.48 mL	222.97 mL
0.5 mM	4.46 mL	22.3 mL	44.59 mL
1 mM	2.23 mL	11.15 mL	22.3 mL
5 mM	0.45 mL	2.23 mL	4.46 mL

*The above data is based on the productmolecular weight 448.5 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.