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BKM120 (NVP-BKM120, Buparlisib)

Catalog No.S2247

BKM120 (NVP-BKM120, Buparlisib) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Phase 2.

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BKM120 (NVP-BKM120, Buparlisib) Chemical Structure
Molecular Weight: 410.39

Validation & Quality Control

Cited by 34 publications：

3 customer reviews : in vivo invitation

Quality Control & MSDS

Related Compound Libraries

BKM120 (NVP-BKM120, Buparlisib) is available in the following compound libraries:

Inhibitor Library Kinase Inhibitor Library Bioactive Compound Library Cambridge Cancer Compound Library

PI3K Inhibitors with Unique Features

Selective PI3K Inhibitors

CAL-101 (Idelalisib, GS-1101) p110δ-selective, IC50=2.5 nM. TGX-221 p110β-specific, IC50=5 nM.
Most Potent PI3K Inhibitor

BEZ235 (NVP-BEZ235, Dactolisib) p110α/γ/δ/β, IC50=4 nM/5 nM/7 nM/75 nM.
FDA-approved PI3K Inhibitor

CAL-101 (Idelalisib, GS-1101) Approved by FDA for Relapsed Chronic Lymphocytic Leukemia, Follicular Lymphoma and Small Lymphocytic Lymphoma.
Newest PI3K Inhibitor

VS-5584 (SB2343) Potent and selective dual PI3K/mTOR inhibitor for mTOR, PI3Kα/β/δ/γ with IC50 of 3.4 nM and 2.6-21 nM, respectively.

Product Information

Compare PI3K Products

Research Area
Research Area
Inhibition Profile
Inhibition Profile
BKM120 (NVP-BKM120, Buparlisib) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Phase 2.
Matthew T. Burger, et al. ACS Med. Chem. Lett., 2011, 2(10), 774–779
BKM120 (NVP-BKM120, Buparlisib) Mechanism
BKM120 (NVP-BKM120, Buparlisib) Mechanism
The receptor-regulated class I PI3K are heterodimeric enzymes, consisting of a 110-kDa catalytic subunit and a regulatory subunit. Different from p110α, -β, and -δ isoforms, the p110γ isoform tightly binds to the p101 regulatory subunit. The p101 structure indicates that an N-terminal domain mediates heterodimerization with the p110γ subunit, and a C-terminal interaction domain mediates the binding to Gβγ complexes. ^[1] The ATP binding site of PI3K-gamma catalytic domain is located in a cleft between the N- and the C-terminal lobes of the catalytic domain.
BKM120 is a 2,6-dimorpholino pyrimidine derivative. The crystal structure indicates that BKM120 binds in the ATP-binding site of PI3K-gamma kinase domain. Specifically, 2-morpholino group makes an interaction via the hydrogen bond from the morpholine oxygenoxygen to the backbone amino group of Val882. The exocyclic nitrogen in the 6-position pyridyl substituent as a donor also forms two bonds to Asp841 and Asp964 in the catalytic region. In addition, a water molecule makes a hydrogen bond bridge between Tyr836 and Asp810, which acts as a hydrogen bond acceptor to interact with the 6-pyridyl endocyclic nitrogen. The binding mode results in greater affinity of PI3K enzyme for BKM120 than ATP. ^[2]
References
[1] Voigt P, et al. J Biol Chem. 2005, 280(6), 5121-5127.
[2] Maira SM, et al. Mol Cancer Ther. 2012, 11(2), 317-328.

Cat.No.	Product Name	Solubility (25°C)
S1009	BEZ235 (NVP-BEZ235, Dactolisib)	<1 mg/mL	0.01 mg/mL	<1 mg/mL
S1065	Pictilisib (GDC-0941)	<1 mg/mL	44 mg/mL	<1 mg/mL
S1105	LY294002	<1 mg/mL	36 mg/mL	21 mg/mL
S2226	CAL-101 (Idelalisib, GS-1101)	<1 mg/mL	83 mg/mL	23 mg/mL
S2247	BKM120 (NVP-BKM120, Buparlisib)	<1 mg/mL	82 mg/mL	2 mg/mL
S1038	PI-103	<1 mg/mL	24 mg/mL	<1 mg/mL
S2638	NU7441 (KU-57788)	<1 mg/mL	3 mg/mL	<1 mg/mL
S1169	TGX-221	<1 mg/mL	12 mg/mL	<1 mg/mL
S1268	IC-87114	<1 mg/mL	0.66 mg/mL	<1 mg/mL
S2758	Wortmannin	<1 mg/mL	85 mg/mL	<1 mg/mL
S1118	XL147 analogue	<1 mg/mL	3 mg/mL	<1 mg/mL
S1072	ZSTK474	<1 mg/mL	21 mg/mL	<1 mg/mL
S2814	Alpelisib (BYL719)	<1 mg/mL	88 mg/mL	2 mg/mL
S1410	AS-605240	<1 mg/mL	0.4 mg/mL	<1 mg/mL
S1205	PIK-75	<1 mg/mL	3 mg/mL	<1 mg/mL
S2767	3-Methyladenine (3-MA)	20 mg/mL	3 mg/mL	4 mg/mL
S2636	A66	<1 mg/mL	79 mg/mL	1 mg/mL
S1523	Voxtalisib (SAR245409, XL765) Analogue	<1 mg/mL	12 mg/mL	<1 mg/mL
S1489	PIK-93	<1 mg/mL	78 mg/mL	<1 mg/mL
S2658	Omipalisib (GSK2126458, GSK458)	<1 mg/mL	100 mg/mL	<1 mg/mL
S1187	PIK-90	<1 mg/mL	0.28 mg/mL	<1 mg/mL
S2743	PF-04691502	<1 mg/mL	14 mg/mL	<1 mg/mL
S1462	AZD6482	<1 mg/mL	82 mg/mL	10 mg/mL
S2696	Apitolisib (GDC-0980, RG7422)	<1 mg/mL	20 mg/mL	<1 mg/mL
S1360	GSK1059615	<1 mg/mL	2 mg/mL	<1 mg/mL
S7028	Duvelisib (IPI-145, INK1197)	<1 mg/mL	83 mg/mL	<1 mg/mL
S2628	Gedatolisib (PF-05212384, PKI-587)	<1 mg/mL	2 mg/mL	<1 mg/mL
S1352	TG100-115	<1 mg/mL	9 mg/mL	<1 mg/mL
S2671	AS-252424	<1 mg/mL	61 mg/mL	<1 mg/mL
S2749	BGT226 (NVP-BGT226)	<1 mg/mL	30 mg/mL	<1 mg/mL
S2759	CUDC-907	<1 mg/mL	102 mg/mL	<1 mg/mL
S2227	PIK-294	<1 mg/mL	98 mg/mL	<1 mg/mL
S2681	AS-604850	<1 mg/mL	57 mg/mL	5 mg/mL
S8002	GSK2636771	<1 mg/mL	28 mg/mL	<1 mg/mL
S2802	BAY 80-6946 (Copanlisib)	0.002 mg/mL	0.002 mg/mL	0.01 mg/mL
S1219	YM201636	<1 mg/mL	35 mg/mL	<1 mg/mL
S2699	CH5132799	<1 mg/mL	12 mg/mL	<1 mg/mL
S2682	CAY10505	<1 mg/mL	58 mg/mL	<1 mg/mL
S2207	PIK-293	<1 mg/mL	80 mg/mL	<1 mg/mL
S2739	PKI-402	<1 mg/mL	0.4 mg/mL	<1 mg/mL
S2870	TG100713	<1 mg/mL	2 mg/mL	<1 mg/mL
S7016	VS-5584 (SB2343)	<1 mg/mL	71 mg/mL	3 mg/mL
S7103	GDC-0032	<1 mg/mL	70 mg/mL	<1 mg/mL
S7018	CZC24832	<1 mg/mL	5 mg/mL	<1 mg/mL
S7798	GNE-317	<1 mg/mL	47 mg/mL	<1 mg/mL
S7356	HS-173	<1 mg/mL	84 mg/mL	<1 mg/mL
S7623	PI-3065	<1 mg/mL	50 mg/mL	<1 mg/mL
S7645	Pilaralisib (XL147)	<1 mg/mL	100 mg/mL	<1 mg/mL
S7675	PF-4989216	<1 mg/mL	76 mg/mL	7 mg/mL
S7694	AZD8186	<1 mg/mL	91 mg/mL	35 mg/mL
S7813	AMG319	<1 mg/mL	77 mg/mL	77 mg/mL
S7646	Voxtalisib (XL765, SAR245409)	<1 mg/mL	54 mg/mL	<1 mg/mL

Product Description

Biological Activity Protocol Clinical Trial Information Chemical Information FAQ Tech Support

Biological Activity

Description

Targets

p110α ^[1]
(Cell-free assay)

p110δ ^[1]
(Cell-free assay)

p110β ^[1]
(Cell-free assay)

p110γ ^[1]
(Cell-free assay)

IC50

52 nM

116 nM

166 nM

262 nM

In vitro

BKM120 is not sensitive to Class III and Class IV PI3K's or PI4K. NVP-BKM120 shows great antiproliferation activity to PI3K deregulated cell lines including A2780, U87MG, MCF7 and DU145 with GI50 of 0.1-0.7 nM. ^[1] BKM120 induces multiple myeloma cells (ARP1, ARK, MM.1S, MM1.R and U266) apoptosis, which results in increased G1-phase cells and decreased S-phase cells. BKM120 induced CD138+ primary MM cell apoptosis and has significant lower cytotoxicity toward CD138− stromal cells. BKM120 exposure could cause upregulation of BimS and downregulation of XIAP. ^[2] BKM120 demonstrates antiproliferative activity in human gastric cancer cell lines by decreasing mTOR downstream signaling. BKM120 could increase either p-ERK or p-STAT3 in KRAS mutant gastric cancer cells. Combination with STAT3 blockade, BKM120 shows a synergism in cells harboring mutated KRAS by inducing apoptosis, but not in KRAS wild-type cells. ^[3] A recent study shows that BKM120 shows differential forms of cell death on the basis of p53 status of the cells with p53 wild-type cells undergoing apoptotic cell death and p53 mutant/deleted cells having a mitotic catastrophe cell death. BKM120 mediates mitotic catastrophe mainly through Aurora B kinase. ^[4]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
MCF7	Mo\tR5l1d3SxeHnjJGF{e2G7		MlTuO\|IhcA>?	NXfmZYRvTE2VTx?=	NHO4RYREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGW6cILld5NqdmdiUFmzT4FteGijIFW1OFVMKG23dHHueEB4cXSqIFfJOVAhd2ZiMD6wNFAyPThizszN	NUjKN3BVOjR7MECyOlY>
DU145	MlvrR5l1d3SxeHnjJGF{e2G7		NFPmd204OiCq	MmDrSG1UVw>?	Mn3JR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSHUyPDViY3XscJMh\XiycnXzd4lv\yCOS1KxJI12fGGwdDD3bZRpKEeLNUCgc4YhOC5yMEC0N\|Uh\|ryP	NUfPelZ3OjR7MECyOlY>
A2780	NFLxe\|hEgXSxdH;4bYMhSXO\|YYm=		MmfLO\|IhcA>?	MWTEUXNQ	MX;DfZRwfG:6aXPpeJkh[WejaX7zeEBRXEWQLXTl[olkcWWwdDDoeY1idiCDMke4NEBk\WyuczD3bZRpKEeLNUCgc4YhOC5yMEC2N\|Uh\|ryP	NF3NdngzPDlyMEK2Oi=>
U87MG	M3zBVWN6fG:2b4jpZ{BCe3OjeR?=		NYf6VohyPzJiaB?=	MmPiSG1UVw>?	NIe2W\|ZEgXSxdH;4bYNqfHliYXfhbY5{fCCSVFXOMYRm\mmlaXXueEBpfW2jbjDVPFdOTyClZXzsd{B4cXSqIFfJOVAhd2ZiMD6wNFA3QThizszN	NVrSTpZHOjR7MECyOlY>
A2780	NVu1e3Z6TnWwY4Tpc44hSXO\|YYm=		MX:xJIg>	NVHkVlBQTE2VTx?=	Mmm1TY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O\|MheGixc4Doc5J6dGG2aX;uJJdqfGhiRVO1NEBw\iByLkC1OUDPxE1?	MV2yOFkxODJ4Nh?=
DU145	NH[yPYJHfW6ldHnvckBCe3OjeR?=		NFfzR\|IyKGh?	M3n5c2ROW09?	NF;xPGJKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hTFVzNEWgZ4VtdHNiaHHyZo9zcW6pIFzLRlEhdXW2YYTpc44hf2m2aDDFR\|UxKG:oIECuNFc{KM7:TR?=	MkTnNlQ6ODB{Nk[=
A2780	NWnTN3dbTnWwY4Tpc44hSXO\|YYm=		MWixJIg>	M1XRVWROW09?	MmGyTY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O\|MheGixc4Doc5J6dGG2aX;uJIlvKFCWRV6t[IVncWOrZX70JIh2dWGwIFGyO\|gxKGOnbHzzJJdqfGhiRVO1NEBw\iByLkC3OEDPxE1?	NGfwZmszPDlyMEK2Oi=>
MCF7	MYLGeY5kfGmxbjDBd5NigQ>?		MWOxJIg>	MlL2SG1UVw>?	M2WzcmlvcGmkaYTpc44hd2ZiUFmzT4FteGijIFW1OFVMKG23dHHueE1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckB4cXSqIFXDOVAhd2ZiMD6xJO69VQ>?	M{fHV\|I1QTByMk[2
U87MG	M2TQWWZ2dmO2aX;uJGF{e2G7		M1niTlEhcA>?	NEG1SJFFVVOR	NUj4eZo5UW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIGDUSW4u\GWoaXPp[Y51KGi3bXHuJHU5P02JIHPlcIx{KHerdHigSWM2OCCxZjCwMlE{KM7:TR?=	NUHQPIVJOjR7MECyOlY>
A2780	MnOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MkT0O\|IhcA>?	NFG5WGdFVVOR	MmXTSWM2OD1yLkWyJO69VQ>?	NF7OS2EzPDlyMEK2Oi=>
SKMES-1	NWnFcY85S3m2b4TvfIlkKEG\|c3H5	MlLxNUDPxE1?	MXi3NkBp		MlTxTY5lfWOnczDj[YxtKGSnYYTo	NXHnTJY3OjZyMUOzNVg>
H596	NFzuW\|RHfW6ldHnvckBCe3OjeR?=	NI\1O2EyKM7:TR?=			NIfYW4pKdXCjaYLzJINmdGxibXnndoF1cW:w	NXLDW\|NTOjZyMUOzNVg>
HCC2450	NIDzSnpHfW6ldHnvckBCe3OjeR?=	MlqwNUDPxE1?			NFmwR3BKdXCjaYLzJINmdGxiaX72ZZNqd25?	M4HxelI3ODF\|M{G4
A549	M3;0XWZ2dmO2aX;uJGF{e2G7	NVHWdpl3PTByIH7N	MmP3OFghcA>?	NIe2S2NFVVOR	MXjJcohq[mm2czDBb5Qh[WO2aY\heIlwdg>?	NG[1cXMzPTl\|N{K5PS=>
A549	Mke2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NE\RWVQyKM7:TR?=	NH\6bY84OiCq	NXfVd5F2TE2VTx?=	NHXPWmVKdmirYnn0d{Bk\WyuIHfyc5d1cA>?	NGPu[3MzPTl\|N{K5PS=>
H522	NF3KcopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NXG3e\|cyOSEQvF2=	NHTQNIs4OiCq	MVPEUXNQ	M{S5e2lvcGmkaYTzJINmdGxiZ4Lve5Rp	MlLJNlU6Ozd{OUm=
LNCaP	NHP4fWFHfW6ldHnvckBCe3OjeR?=	NVfHW\|FJOSEQvF2=			NYq0e\|N{W3WycILld5NmeyCyLVHLWEBt\X[nbIO=	M{jBbFI2OzZyN{m5
LNCaP95	NH;EUoxHfW6ldHnvckBCe3OjeR?=	NGP0TIYyKM7:TR?=			NVO1fIhFW3WycILld5NmeyCyLVHLWEBt\X[nbIO=	NILtbZkzPTN4MEe5PS=>
HCT-15	NWnMT3NLSXCxdH;zbZMhSXO\|YYm=	MVmxNEDPxE1?	MYm0PEBp	MWPEUXNQ	MVvJcoR2[2W\|IHHwc5B1d3OrczDpckBJS1RvMUWgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>?	MkHCNlUyPTJ{NEW=
HCT-116	NGHjTHhCeG:2b4Ppd{BCe3OjeR?=	MXOxNEDPxE1?	NH[zc4w1QCCq	M3i4e2ROW09?	Mn;rTY5lfWOnczDhdI9xfG:\|aYOgbY4hUEOWLUGxOkBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w	MYqyOVE2OjJ2NR?=
NCI-H460	MoHvRZBwfG:\|aYOgRZN{[Xl?	M3Lob\|ExKM7:TR?=	MUm0PEBp	NEPXVItFVVOR	NHTjPFJKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCQQ1mtTFQ3OCClZXzsd{Bp[XKkb4XybY5oKFCLS{PDRUBpd3S\|cH;0JI12fGG2aX;u	NGnLOnQzPTF3MkK0OS=>
SKOV-3	NXflfGpsSXCxdH;zbZMhSXO\|YYm=	NGflcGsyOCEQvF2=	NXrJfIFjPDhiaB?=	MkfzSG1UVw>?	MYLJcoR2[2W\|IHHwc5B1d3OrczDpckBUU0:YLUOgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>?	NGP4fY8zPTF3MkK0OS=>
BSY-1	NXexV5VXSXCxdH;zbZMhSXO\|YYm=	MoeyNVAh\|ryP	MVK0PEBp	MYnEUXNQ	MXvJcoR2[2W\|IHHwc5B1d3OrczDpckBDW1lvMTDj[YxteyCqYYLic5VzcW6pIGDJT\|NESSCqb4TzdI91KG23dHH0bY9v	MkjWNlUyPTJ{NEW=
MKN-1	MX;BdI91d3OrczDBd5NigQ>?	MWmxNEDPxE1?	MUm0PEBp	MlnnSG1UVw>?	M4S3RWlv\HWlZYOgZZBweHSxc3nzJIlvKE2NTj2xJINmdGy\|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25?	NV3mTpNzOjVzNUKyOFU>
NCI-H522	NVfYUZhmSXCxdH;zbZMhSXO\|YYm=	MWqxNEDPxE1?	MVe0PEBp	NXrubJQ4TE2VTx?=	MV3JcoR2[2W\|IHHwc5B1d3Orcx?=	MYmyOVE2OjJ2NR?=
OVCAR-3	NELCVYtCeG:2b4Ppd{BCe3OjeR?=	NFj1SXcyOCEQvF2=	NHP6SHE1QCCq	MVPEUXNQ	NU\QPHYzUW6mdXPld{BieG:ydH;zbZM>	Mn:2NlUyPTJ{NEW=
HBC-5	NFLRPFBCeG:2b4Ppd{BCe3OjeR?=	NV;3SGs3OTBizszN	NUTMXJhKPDhiaB?=	NXzUZoNHTE2VTx?=	NEO1VVlKdmS3Y3XzJIFxd3C2b4Ppdy=>	MWOyOVE2OjJ2NR?=
RXF-631L	NWXKZmtLSXCxdH;zbZMhSXO\|YYm=	M3rlcVExKM7:TR?=	NGKzVHQ1QCCq	M{T4dmROW09?	MYLJcoR2[2W\|IHHwc5B1d3Orcx?=	NVHaPJloOjVzNUKyOFU>
MKN-45	M1vqU2Fxd3Sxc3nzJGF{e2G7	MVOxNEDPxE1?	MVy0PEBp	NVXI[GFiTE2VTx?=	NWXGd4pCUW6mdXPld{BieG:ydH;zbZM>	MoiwNlUyPTJ{NEW=
BON-1	NVz4TmdoT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NEKwc2s2ODBibl2=	MnrONVAh\A>?	MlL5SG1UVw>?	NFTjfnBKdmirYnn0d{Bk\WyuIHfyc5d1cA>?	M{nCfVI2ODJ4Mkmy
BON-1	NVPGbVhlTnWwY4Tpc44hSXO\|YYm=	M2PzelUxOCCwTR?=	MV[0JIg>	NEPvfG1FVVOR	NV;zOo9PUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBVcHJ\|MEigZY5lKFOnckS3Ny=>	M3PxfFI2ODJ4Mkmy
QGP-1	NIXjNnhHfW6ldHnvckBCe3OjeR?=	M1:zUlUxOCCwTR?=	MXO0JIg>	MmTYSG1UVw>?	MmLwTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDUbJI{ODhiYX7kJHNmejR5Mx?=	M{PxWlI2ODJ4Mkmy
Huh7	MV;GeY5kfGmxbjDBd5NigQ>?	NVz0T2RqOSEQvF2=	NEXHflgyKGh?	NUHRNVhGTE2VTx?=	MonYTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDT[ZI1PzR?	NHTXRmYzPTByNESwNy=>
BNL	MVXGeY5kfGmxbjDBd5NigQ>?	NFGzO5YyKM7:TR?=	NH:xRWQyKGh?	MnLoSG1UVw>?	NIPNU2FKdmirYnn0d{BxcG:\|cHjvdplt[XSrb36gc4YhWzZ?	Ml3jNlUxODR2MEO=
MDA-MB-175	NWfrVWRCT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NH\iSY4yKM7:TR?=	MX21JIQ>	NX3nWGh5TE2VTx?=	Mm\YTWM2ODxzIN88US=>	M{X5NlI1QDd7N{m2
MDA-MB-134	MmiwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NFHoRWUyKM7:TR?=	MWO1JIQ>	MnX5SG1UVw>?	MWDJR\|UxRDFizszN	MVOyOFg4QTd7Nh?=
HCC1500	NIXqU5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MnfCNUDPxE1?	M{eyPVUh\A>?	NF30bpFFVVOR	Mlu0TWM2ODxzIN88US=>	NYqzNI5SOjR6N{m3PVY>
EFM-19	NETVUIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NGPVO2cyKM7:TR?=	NUXweYt2PSCm	M4Pmc2ROW09?	MYXJR\|UxRDFizszN	NX\RPWFROjR6N{m3PVY>
ZR-75-30	MmXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NIDyOmcyKM7:TR?=	M2nSWFUh\A>?	NXnsS3BTTE2VTx?=	NWPCU5dSUUN3MEyxJO69VQ>?	MYqyOFg4QTd7Nh?=
MDA-MB-361	M4[5XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M4TTfFEh\|ryP	MmPJOUBl	NW\FV\|dRTE2VTx?=	M3TI[mlEPTB:MTFOwG0>	M{HUflI1QDd7N{m2
T-47D	M{DMeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NGjxRXYyKM7:TR?=	NH\peXI2KGR?	M{fZWWROW09?	Mmm2TWM2ODxzIN88US=>	NETrTGYzPDh5OUe5Oi=>
SK-BR-3	NIXpRnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MnvUNUDPxE1?	M4nDcVUh\A>?	MkfaSG1UVw>?	MoWzTWM2ODxzIN88US=>	NWH4VJNlOjR6N{m3PVY>
UACC-732	MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M1XvPFEh\|ryP	NETIVJg2KGR?	M2D1NWROW09?	MlnTTWM2ODxzIN88US=>	M3qyXlI1QDd7N{m2
BT-474	M1G3W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NY\TbHAzOSEQvF2=	M1XGZVUh\A>?	NXnu[VFsTE2VTx?=	NVXNVZFmUUN3MEyxJO69VQ>?	MV:yOFg4QTd7Nh?=
HCC202	MoPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MlnINUDPxE1?	NGf3dJk2KGR?	MYLEUXNQ	NWq2UphVUUN3MEyxJO69VQ>?	NIi3OpYzPDh5OUe5Oi=>
MCF7	MlfYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1mwXlEh\|ryP	MYm1JIQ>	NHrMd\|BFVVOR	MVnJR\|UxRDFizszN	NX\VVndTOjR6N{m3PVY>
MDA-MB-415	MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M1;tflEh\|ryP	NHfxU2s2KGR?	NUjkSpFkTE2VTx?=	NIPDSnNKSzVyPEGg{txO	MkHyNlQ5Pzl5OU[=
MDA-MB-453	MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MnHxNUDPxE1?	NIPTZ\|A2KGR?	M3zUW2ROW09?	M3LZ[GlEPTB:MTFOwG0>	M4L5WlI1QDd7N{m2
ZR-75-1	MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NVTrXVg4OSEQvF2=	NGnUPYY2KGR?	MnfJSG1UVw>?	MUPJR\|UxRDFizszN	M1\pT\|I1QDd7N{m2
HCC38	M1\6S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M17YeVEh\|ryP	NUGzVXJIPSCm	MnHRSG1UVw>?	M3nWNmlEPTB:MTFOwG0>	MmDnNlQ5Pzl5OU[=
HCC1419	MnW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NGHmN\|YyKM7:TR?=	Mnn2OUBl	MYXEUXNQ	NIrjWHVKSzVyPEGg{txO	MlnsNlQ5Pzl5OU[=
UACC-812	M2LoU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MWixJO69VQ>?	MkfjOUBl	NUWwN2VpTE2VTx?=	Moj5TWM2ODxzIN88US=>	NWD2fYxIOjR6N{m3PVY>
HCC1187	NFjvWldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYCyS\|FwOSEQvF2=	M{LTZVUh\A>?	M4i5[2ROW09?	NUPQZot1UUN3MEyxJO69VQ>?	NFvtb44zPDh5OUe5Oi=>
KPL-1	MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NXrr[mtXOSEQvF2=	NIS3dVM2KGR?	M1jEc2ROW09?	NVi0ToVqUUN3MEyxJO69VQ>?	Mm\WNlQ5Pzl5OU[=
SUM-225	M3LWfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MkXMNUDPxE1?	M3\4[lUh\A>?	M1jjN2ROW09?	Mof3TWM2ODxzIN88US=>	MViyOFg4QTd7Nh?=
EFM-192A	NGjZemhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MlnkNUDPxE1?	NUfkcHZ6PSCm	NVzwOGY1TE2VTx?=	MWPJR\|UxRDFizszN	M2HlcFI1QDd7N{m2
JIMT-1	MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M2Xqb\|Eh\|ryP	NF\Uc\|g2KGR?	M1\RPWROW09?	NF;CR\|lKSzVyPEGg{txO	NFq2UYgzPDh5OUe5Oi=>
HCC1143	M{DYZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mn21NUDPxE1?	NWiwdlE5PSCm	MoruSG1UVw>?	NFPL[IFKSzVyPEGg{txO	NEXZTWMzPDh5OUe5Oi=>
HCC2218	MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NHK4[FYyKM7:TR?=	M2LYWFUh\A>?	NV74R2Q3TE2VTx?=	NV;DPHluUUN3MEyxJO69VQ>?	MVKyOFg4QTd7Nh?=
MDA-MB-468	MoPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Ml;xNUDPxE1?	MV[1JIQ>	NYnuPYtyTE2VTx?=	MXfJR\|UxRDFizszN	MYOyOFg4QTd7Nh?=
BT-20	NYjhNWVoT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3HwcFEh\|ryP	NETRe482KGR?	NW[zc2ZHTE2VTx?=	MkD6TWM2ODxzIN88US=>	M3\RU\|I1QDd7N{m2
MDA-MB-435	Ml;lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MnrNNUDPxE1?	MYi1JIQ>	MUnEUXNQ	MkXGTWM2ODxzIN88US=>	Mm[2NlQ5Pzl5OU[=
BT-549	MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NWC0TJZYOSEQvF2=	MljNOUBl	Mo\aSG1UVw>?	MVjJR\|UxRDFizszN	MV2yOFg4QTd7Nh?=
HCC1806	MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MV6xJO69VQ>?	NEHGXGY2KGR?	NWroZ5FZTE2VTx?=	NIPLbpZKSzVyPEGg{txO	MmHjNlQ5Pzl5OU[=
HCC1937	NETsRVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NXntSIZDOSEQvF2=	MoThOUBl	MU\EUXNQ	MYjJR\|UxRDFizszN	MoPHNlQ5Pzl5OU[=
Hs578T	NGnLXG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NITsSZYyKM7:TR?=	M1HmSFUh\A>?	NFfM[npFVVOR	MVvJR\|UxRDFizszN	Mnv6NlQ5Pzl5OU[=
LN18	MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MnTRNlAh\|ryP	NEH0bok4OiCq	MmLaSG1UVw>?	MVHJR\|UxRDVizszN	M4PVcVI1PzRzMEe0
LN229	NV31OINWT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MYqyNEDPxE1?	M{XocFczKGh?	NUHifHNOTE2VTx?=	MULJR\|UxRDVizszN	NULSWIpNOjR5NEGwO\|Q>
LNZ308	M2r6dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NGjIWpAzOCEQvF2=	MlzVO\|IhcA>?	NHzDfHpFVVOR	M2nNVGlEPTB:NTFOwG0>	MoG0NlQ4PDFyN{S=
T98G	M1rUSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NWPHVJZsOjBizszN	NF\o[HY4OiCq	NFWyTnFFVVOR	Mm\LTWM2ODx3IN88US=>	NV3Bd2RJOjR5NEGwO\|Q>
U87	NXPuRWxmT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MVeyNEDPxE1?	NXLpXHc2PzJiaB?=	MVPEUXNQ	Mnz0TWM2ODx3IN88US=>	MVeyOFc1OTB5NB?=
LN18	M1rPcWZ2dmO2aX;uJGF{e2G7	NHPu[3Y2KM7:TR?=	M1jXXVI1KGh?	M2PaT2ROW09?	M3XtOWlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1R?	NHTIfI4zPDd2MUC3OC=>
LNZ308	M1vvSGZ2dmO2aX;uJGF{e2G7	NFnXZ5k2KM7:TR?=	NGHpclQzPCCq	NV[3TGVRTE2VTx?=	MkCxTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXA>?	NUXG[XV{OjR5NEGwO\|Q>
Saos-2	NH6yWFJHfW6ldHnvckBCe3OjeR?=	NXG3[oZqPTBizszN	M33yfFQ5KGh?		MV\Jcohq[mm2czDj[YxtKGmwdnHzbY9v	NUTWUWxYOjR5Mke2OlA>
MG-63	NXPSSZZyTnWwY4Tpc44hSXO\|YYm=	NIPzdHY2OCEQvF2=	MW[0PEBp		Mlv4TY5pcWKrdIOgZ4VtdCCrbo\hd4lwdg>?	NV\5fG1YOjR5Mke2OlA>
SJSA-1	M1PkWGZ2dmO2aX;uJGF{e2G7	NHfCN5Y2OCEQvF2=	MYK0PEBp		MkPkTY5pcWKrdIOgZ4VtdCCrbo\hd4lwdg>?	MnL4NlQ4Ojd4NkC=
Saos-2	NHTUdFlHfW6ldHnvckBCe3OjeR?=	NWDWOnhDPTBizszN	M{XjU\|Q5KGh?		MVjJcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO\|aX;u	NXjvSWVUOjR5Mke2OlA>
MG-63	NEewSGxHfW6ldHnvckBCe3OjeR?=	MX:1NEDPxE1?	MVK0PEBp		NGXheZhKdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9v	NHqxTpMzPDd{N{[2NC=>
SJSA-1	MYfGeY5kfGmxbjDBd5NigQ>?	NVGxcoZIPTBizszN	M1f1RlQ5KGh?		NFewd2tKdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9v	MoTzNlQ4Ojd4NkC=
Saos-2	NWXjR3N2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MXG1NEDPxE1?	Mlf4OFghcA>?		NWPNVJdkUW6qaXLpeJMh[2WubDD2bYFjcWyrdIm=	NUnxeXA6OjR5Mke2OlA>
MG-63	NWS5cXp1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M2q2WVUxKM7:TR?=	MlryOFghcA>?		NFf0cmhKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?=	MVGyOFczPzZ4MB?=
SJSA-1	Mn;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MYq1NEDPxE1?	Ml7xOFghcA>?		M1zCe2lvcGmkaYTzJINmdGxidnnhZoltcXS7	MXWyOFczPzZ4MB?=
FaDu	NWPPVpY3TnWwY4Tpc44hSXO\|YYm=	NULnSJdGPSEQvF2=	MWKyOEBp	NV\0OWE3TE2VTx?=	M3LiOXJm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u	MVmyOFY{OTF2Nx?=
EMT6	NI\ScWJHfW6ldHnvckBCe3OjeR?=	NH7wPIE2KM7:TR?=	MWWyOEBp	M1;QUGROW09?	MX;S[YR2[2W\|IH;4fYdmdiClb37zeY1xfGmxbh?=	NVPDeG1IOjR4M{GxOFc>
HCT116	MV7GeY5kfGmxbjDBd5NigQ>?	MnvBOUDPxE1?	MVWyOEBp	MorsSG1UVw>?	M3rVbnJm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u	M33pbFI1PjNzMUS3
U87	M1PTOWZ2dmO2aX;uJGF{e2G7	NVGxUZBjPSEQvF2=	MnrRNlQhcA>?	Mon5SG1UVw>?	M3;2c3Jm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u	MnyzNlQ3OzFzNEe=
GBM	MVjBdI9xfG:\|aYOgRZN{[Xl?	NWXNb41KOs7:TR?=	M2XCU\|Q5cA>?	M{\mRmROW09?	NWmyUmc2cW6mdXPl[EBpcWeqZYKgcIV3\Wy\|IH;mJIFxd3C2b4Ppd{wh[W6mIHTlZ5Jm[XOnZDDj[YxtKH[rYXLpcIl1gQ>?	MUWyOFUxODR7Mh?=
BON	NVTYRnNoT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M2DjRVEuPc7:TR?=	MUC3Nog>		NY\uPJVW\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>?	M3raZVI1PDR\|NUKz
BON	NV;CfVZZSXCxcITvd4l{KEG\|c3H5	Ml\XNU02\|ryP	MmXmNlRp		NHfROW1qdmO{ZXHz[ZMh[XCxcITvd4l{	M3fHW\|I1PDR\|NUKz
H1975	NHrCeo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M1LHNVAvOy17LkdOwG0>	MlXYO\|Jp	MXTEUXNQ	NILoXnpKSzVyPUGuN\|g2\|ryP	Mn;RNlQ{Ozd6NE[=
H1975	M13q[mFxd3C2b4Ppd{BCe3OjeR?=	M1nRcVLPxE1?	M3Ll[lI1cA>?	M{Pq[mROW09?	NFS5NlRqdmO{ZXHz[ZMh[XCxcITvd4l{KHKjdHWgd4lodmmoaXPhcpRtgQ>?	MoC2NlQ{Ozd6NE[=
T-ALL	NXLqVIt4SXCxcITvd4l{KEG\|c3H5	NGT5cHJj\XS5ZXXuJFEvPCCjbnSgOU4{KG2PIHH0JFI1cCCjbnSgNE46KGGwZDC1MlUhdU1iYYSgOFhpKGmwIHTp[oZmemWwdDDj[YxtKGyrbnW=	M2\WZ\|I1KG:{IES4bC=>	MkOwSG1UVw>?	M4H3VoFn\mWldIOgeIhmKFCLM1ugdIF1cHejeTDpckBVNUGOTDDj[YxtKGyrbnXz	MXyyOFMyODd\|Nh?=
BCR-ABL	MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MX6wMlI2NTFyzszN	NVT1VHBGPGR?		M{fGdpNq\26rZnnjZY51dHliaX7obYJqfCClZXzsJJBzd2yrZnXyZZRqd25?	MV6yOFI1PDZzMh?=
LC-1/SQSF	NIrTdWZHfW6ldHnvckBCe3OjeR?=	NXuxO4dWO87:TR?=	NG\Rc4YzPGh?	Mo\hSG1UVw>?	M365OIRm[3KnYYPlJG5TTjJicILveIVqdiCuZY\lcC=>	Mm\BNlM6QDByOUO=
Primary CLL cells	M{nNT2Fxd3C2b4Ppd{BCe3OjeR?=	NEexd5kyNTFyzszN	NGr2VWQ1QGh?		NWTNRZVzcW6mdXPld{BieG:ydH;zbZMhcW5iQ1zMJINmdGy\|IHnu[IVx\W6mZX70JI9nKHC{b3fuc5N1cWNibXHyb4Vzew>?	NXW0OYdLOjN6NUC4NFc>
Primary CLL cells	MkHrT4lv[XOnIFHzd4F6	M2OyNVLPxE1?	M3i3fVMxdWmw		MUjk[YNz\WG\|ZXSgVGk{UyCjY4Tpeol1gQ>?	MkPBNlM5PTB6MEe=
Primary CLL cells	MlPUR5l1d3SxeHnjJGF{e2G7	M1[5dFLPxE1?	M2LpUVI1cA>?		M1jVSolv\HWlZYOgZ4VtdCCleYTveI95cWOrdIm=	NGKye5IzOzh3MEiwOy=>
human NSCLC cell lines	M3jFZWFxd3C2b4Ppd{BCe3OjeR?=	MYqwMlEzPS12zszN	NXmxZW06OjSq	MmX3SG1UVw>?	MWfJR\|UxeyC{YX7n[ZMh\nKxbTCwMlQuOs7:TR?=	M3rzPVI{PTZ{NEey
human HCC cell lines	Mmq2R4VtdCC4aXHibYxqfHliYYPzZZk>	M4SwfVAvODB3LUJOwG0>	MVu0PIg>		MWnJR\|UxRTIQvF2=	M2nFcVI{PDh7OUm5
Huh7	NHzQVmJMcW6jc3WgRZN{[Xl?	M17mSFHPxE1?	Mkf4OFhp		NF7PRnp{cWewaf-shYNidnSueTDy[YR2[2W\|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q>	MVWyN\|Q5QTl7OR?=
SK-HEP1	MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MX[xMVIx\|ryP	MmTUO\|Jp	NXj1bFF{TE2VTx?=	M{jyb2lEPTExvKyx{txO	NUCxXVZUOjN2N{mxN\|Y>
786-0	NYjtcG57T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NHLU[5YyNTJyzszN	NFvie\|I4Omh?	M{XOUGROW09?	M3fFcWlEPTExvKyx{txO	NF3WTlIzOzR5OUGzOi=>
JVM2	NUj0S5NkS3m2b4TvfIlkcXS7IHHzd4F6	MmXqNE4zNTJyzszN	NX\s[ZF1PzKq	NIHyRpVFVVOR	M{jqTmlEPTB;MD65{txO	NIT6NVkzOzJ\|OE[zPS=>
EHEB	NWXMd\|V5S3m2b4TvfIlkcXS7IHHzd4F6	M3HGfVAvOi1{MN88US=>	NV3JfItTPzKq	NYH1cZBXTE2VTx?=	Mnu0TWM2OD1yLkhOwG0>	Mo\uNlMzOzh4M{m=
MEC2	NUG5R20xS3m2b4TvfIlkcXS7IHHzd4F6	M3:wc\|AvOi1{MN88US=>	NVqzUZRCPzKq	NF;JPGxFVVOR	M{P5W2lEPTB;MD63{txO	MXWyN\|I{QDZ\|OR?=
primary B-CLL lymphocytes	MWrBdI9xfG:\|aYOgRZN{[Xl?	NUDZOZZnUUN3MDDmc5Ih\WGlaDDwdolu[XK7IHPlcIwhdGmwZR?=	NHjIOIQzPGh?	NFTrdpdFVVOR	NWjw[ZRpUUN3MP-8oFPPxE1iZn;yJIFtdCCyYYTp[Y51ew>?	MYCyN\|I{QDZ\|OR?=
primary B-CLL lymphocytes	MW\LbY5ie2ViQYPzZZk>	NHrtSI5KSzVyIH\vdkBm[WOqIIDybY1ienliY3XscEBtcW6n	Mor6NlRp		Mlm3bY5pcWKrdIOgdFcxWz[NID[gOGUuSlBzIHX4dJJme3Orb36=	NFKzbJUzOzJ\|OE[zPS=>
human NSCLC	Mo\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUSwMlUuOs7:TR?=	NEPDbY44Omh?		MnjmTWM2OD1zzszN	NF3X[mszOjd6MUO5Ny=>
human NSCLC	M4XmUWtqdmG\|ZTDBd5NigQ>?	M4HMOFHPxE1?	NH3Q[4EzPGh?		NFPLU\|FqdmirYnn0d{B1cGViQXv0M41VV1Jic3nncoFtcW6pIIDheIh4[XliYYSgN4gh[W[2ZYKgeJJm[XSvZX70	M1Hod\|IzPzhzM{mz
Y1 cell line	NUD5UWI1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MkP2NE4y\|ryPL{JOwG0>	M2nQbFI1cA>?	NYryVFFWTE2VTx?=	MoXjbY5pcWKrdIOgOlDwxIViY3XscEB3cWGkaXzpeJkhcW5iTYnjMXNkfHJvdILhcpNn\WO2ZXSgZ4VtdHN?	MlvvNlI3QTJ7MES=
PIK3CA-mutant MCF7	NXO4WY1OT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MmHLS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1?	MoL0O\|Jp		MkX2S2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1?	NFzCOXYzOjZ3M{m2Oy=>
PIK3CA-mutant MCF7	NEflepZMcW6jc3WgRZN{[Xl?	NYnMfpNUUUN3ME2xNVTDuTOwTR?=	MWO3Nog>		NUTrWGFvUUN3ME2xNVTDuTOwTTDpckBz\WS3Y3nu[{BCc3RicHjvd5Bpd3K7bHH0bY9vKGyndnXsdy=>	NYHMNWM2OjJ4NUO5Olc>
MCF7-myr-Akt	MlrwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NFfiZ2NIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?=	MlPuO\|Jp		MmnyS2k2OD1{OUpCtVY5dk4xvJzMSFUx97zgMUCsNFAxdk1?	NGjBWo8zOjZ3M{m2Oy=>
colon cancer cell lines	MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NIXQWowxNTFyzszN	MYi3Nog>	MkfQSG1UVw>?	NEPR[HRKSzVyPUJOwG0>	M2nKSVIzPTR\|OEW3
gastric cancer cell lines	NUTudnJMT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MUmwMVEx\|ryP	M2rmPFczcA>?	NV\L[5hOTE2VTx?=	NWDzWpV4UUN3ME2yMVXPxE1?	M1n5SVIzPTR\|OEW3
HCT-116/HT-29/MKN-45	NWX6TYYySXCxcITvd4l{KEG\|c3H5	M1j0cVLPxE1?	Mn\WOFhp		MonGd4hq\nRiaX6gS\|IheGijc3W=	MUGyNlU1Ozh3Nx?=
HT-29 and HCT-116	Ml;YR4F{eGG\|ZTDhd5NigQ>?	MlnnOe69VQ>?	M1zad\|I1cA>?		NVfqUHg4cW6mdXPld{Bk[XOyYYPlJIFkfGm4aYT5	M3PrRlIzPTR\|OEW3
MM cell lines	MoGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M2T1S\|Ex\|ryP	NYLGRlV{OjSq	M2jh[GROW09?	MYDJR\|UxKH[jcnnld{BidW:wZzDkbYZn\XKnboSgZ4VtdCCuaX7ld{BqdiC2aX3lJIFv\CCmb4PlJIRmeGWwZHXuZ4U>	NXLjSlI5OjJ{MEe0PFU>
ARP-1	MWTBdI9xfG:\|aYOgRZN{[Xl?	MoLFNVDPxE1?	NF3HVVgzPGh?	MkDuSG1UVw>?	M2XXR4lv\HWlZYOgUW0h[2WubDDhdI9xfG:\|aYOgeIhzd3WpaDDjZZNx[XOnIHHjeIl3[XSrb36=	MluwNlIzODd2OEW=
SNU-601	NXy2VYdMT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NHyySI04Omh?	M1nv[2ROW09?	MlzVTWM2OD1yLkixOuKyOC5yNkROwG0>	MX6yNlE2QThzNB?=
SNU-1	NXXEeFA1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M3Pw[lczcA>?	MorISG1UVw>?	MmTtTWM2OD1zLkC4NuKyOC5yMklOwG0>	M1HTW\|IzOTV7OEG0
SNU-668	MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NYCz[3hiPzKq	NF:4SWFFVVOR	MYXJR\|UxRTFwNUe5xtExNjB5NN88US=>	M{Dh[lIzOTV7OEG0
AGS	MoTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MUO3Nog>	Mle5SG1UVw>?	MWXJR\|UxRTFwN{G0xtExNjFzN988US=>	MX[yNlE2QThzNB?=
SNU-216	NF7lSlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		M3fPWFczcA>?	MVHEUXNQ	MnXlTWM2OD1{Lk[5NuKyOC5yOENOwG0>	MkPvNlIyPTl6MUS=
SNU-5	M4nKXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NFLUVms4Omh?	MorySG1UVw>?	MkjjTWM2OD1zLkO1NeKyOC5yOUJOwG0>	NWeweHpnOjJzNUm4NVQ>
SNU-638	MkTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MU[3Nog>	NFr2dW9FVVOR	NUfDT2ZXUUN3ME2yMlI5OsLzMD6wOVPPxE1?	M4[2VFIzOTV7OEG0
SNU-16	M1TIWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MX:3Nog>	MUfEUXNQ	MXPJR\|UxRTFwNUezxtExNjByMd88US=>	M3;aNlIzOTV7OEG0
SNU-484	M3nFbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		Mlz6O\|Jp	NIPNclRFVVOR	MkPWTWM2OD1zLkeyPOKyOC5yNEZOwG0>	NUHCeYt[OjJzNUm4NVQ>
SNU-620	NVq0eJV1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NUTaU2pvPzKq	M1fnSmROW09?	M1vlVGlEPTB;Mj65N\|nDuTBwMECx{txO	NIPw[5kzOjF3OUixOC=>
SNU-719	NET2Z4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MYm3Nog>	MXjEUXNQ	NXzTNmRKUUN3ME2zMlA{P8LzMD6wN\|LPxE1?	NUPkZ\|Z1OjJzNUm4NVQ>
glioma cell lines	NVLTW4t7T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MXO3Nog>		NWn4cJhyUUN3ME2xMVLPxE1?	NFjyb4YzOjB4NUC4NC=>
U87	NUDGSGtwSXCxcITvd4l{KEG\|c3H5	NFOxe\|kz\|ryP	M330cVczcA>?		MUnpcoR2[2W\|IHPlcIwh[XCxcITvd4l{KGGwZDDjcIVifmWmIGDBVnAh[W6mIHPhd5Bie2VvMx?=	MX6yNlA3PTB6MB?=

... Click to View More Cell Line Experimental Data

In vivo

BKM120 completely inhibits pAktser473 in A2780 xenograft tumors at doses of 30, 60, or 100 mg/kg, respectively. BKM120 also shows antitumor activity against U87MG glioma model at doses of 30 and 60 mg/kg. ^[1] BKM120 treatment results in significantly reduced tumor volume and level of circulating human kappa chain at 5 μM/kg/day−1in ARP1 SCID mouse model, with prolonged survival. ^[2]

Features

Protocol(Only for Reference)

Kinase Assay: ^[1]

PI3K biochemical assay (ATP depletion assay)	BKM120 is dissolved in DMSO and directly distributed into a black 384-well plate at 1.25 µL per well. To start the reaction, 25 µL of 10 nM PI3 kinase and 5 µg/mL 1-α-phosphatidylinositol (PI) in assay buffer (10 mM Tris pH 7.5, 5 mM MgCl₂, 20 mM NaCl, 1 mM DTT and 0.05% CHAPS) are added into each well followed by 25 µL of 2 µM ATP in assay buffer. The reaction is performed until approx 50% of the ATP is depleted and then stopped by the addition of 25 µL of KinaseGlo solution. The stopped reaction is incubated for 5 minutes and the remaining ATP is then detected via luminescence.
PI3K biochemical assay (filter binding assay)	50 µL/well of a 1:1 mixture of 100 µL/mL L-α-phosphatidylinositol and L-α-phosphatidylserine dissolved in chloroform:ethanol (2.2:7.8) is pipetted into 96-well MaxiSorp^TM plates. The solvents are evaporated at room temperature and plates are wa

PI3K biochemical assay (ATP depletion assay)

BKM120 is dissolved in DMSO and directly distributed into a black 384-well plate at 1.25 µL per well. To start the reaction, 25 µL of 10 nM PI3 kinase and 5 µg/mL 1-α-phosphatidylinositol (PI) in assay buffer (10 mM Tris pH 7.5, 5 mM MgCl₂, 20 mM NaCl, 1 mM DTT and 0.05% CHAPS) are added into each well followed by 25 µL of 2 µM ATP in assay buffer. The reaction is performed until approx 50% of the ATP is depleted and then stopped by the addition of 25 µL of KinaseGlo solution. The stopped reaction is incubated for 5 minutes and the remaining ATP is then detected via luminescence.

PI3K biochemical assay (filter binding assay)

50 µL/well of a 1:1 mixture of 100 µL/mL L-α-phosphatidylinositol and L-α-phosphatidylserine dissolved in chloroform:ethanol (2.2:7.8) is pipetted into 96-well MaxiSorp^TM plates. The solvents are evaporated at room temperature and plates are wa

Cell Assay: ^[1]

Cell lines	A2780 cells.
Concentrations	0-6.6 μM
Incubation Time	3 days.
Method	A2780 cells are cultured in DMEM supplemented with 10% FBS, L-glutamine, sodium pyruvate, and antibiotics. Cells are plated in the same medium at a density of 10³ cells per well, 100 μL per well into black-walled-clear-bottom plates and incubated for 3-5 hours. BKM120 supplied in DMSO (20 mM) is diluted. The diluted BKM120 solution (2 μL), is then added to cell medium (500 μL) cell medium (concentration from 0-6.6 μM). Equal volumes of this solution (100 μL) are added to the cells in 96 well plates and incubated at 37 °C for 3 days and developed using Cell Titer Glo. Inhibition of cell proliferation is determined by luminescence read using Trilux.

Animal Study: ^[1]

Animal Models	U87MG and A2780 xenografts are established in female nu/nu mice.
Formulation	In 15% Captisol.
Dosages	~60 mg/kg.
Administration	Dosed orally daily (q.d.).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m²)	0.007	0.025	0.15	0.05	0.02	0.5
K_m factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B K_m
	Animal A K_m

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse K_m(3)	= 11.2 mg/kg
	rat K_m(6)

References

[1] Burger MT, et al. ACS Med Chem Lett, 2011, 2 (10), 774–779.

[2] Zheng Y, et al. J Mol Med (Berl), 2011 Dec 30.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT02756247	Not yet recruiting	Lymphoma\|Mantle Cell Lymphoma\|Follicular Lymphoma\|Diffuse Large B Cell Lymphoma	Memorial Sloan Kettering Cancer Center\|Janssen Scientific ...more	May 2016	Phase 1
NCT02614508	Recruiting	Recurrent Chronic Lymphocytic Leukemia\|Recurrent Small Lymphocytic Lymphoma\|Refractory Chronic Lymphocytic Leukemia\|Refractory Small Lymphocytic Ly ...more	Emory University\|Novartis	January 2016	Phase 1
NCT01613677	Withdrawn	Treatment for Metastatic or Locally Advanced Cervical Cancer	Novartis Pharmaceuticals\|Novartis	November 2015	Phase 2
NCT01971489	Withdrawn	Adult Solid Neoplasm\|Recurrent Non-Small Cell Lung Carcinoma\|Stage IIIA Non-Small Cell Lung Cancer\|Stage IIIB Non-Small Cell Lung Cancer\|Stage IV N ...more	Roswell Park Cancer Institute\|National Cancer Institute ( ...more	September 2015	Phase 1
NCT02452294	Recruiting	Malignant Melanoma\|Metastases	University Hospital Tuebingen\|University Hospital Dresden	July 2015	Phase 2

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Chemical Information

Download BKM120 (NVP-BKM120, Buparlisib) SDF

Molecular Weight (MW)	410.39
Formula	C₁₈H₂₁F₃N₆O₂
CAS No.	944396-07-0

Storage	3 years -20℃powder
Storage	6 months-80℃in solvent
Synonyms	N/A

Solubility (25°C) *	In vitro	DMSO	82 mg/mL (199.8 mM)
		Ethanol	2 mg/mL (4.87 mM)
		Water	<1 mg/mL (<1 mM)
	In vivo	0.5% CMC Na	6 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck 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.

Chemical Name	5-(2,6-dimorpholinopyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine

Molarity Calculator Dilution Calculator Molecular Weight Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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BKM120 (NVP-BKM120, Buparlisib)