Cladribine (RWJ 26251)

Catalog No.S1199 Synonyms: Leustatin, 2-CdA, 2-chlorodeoxyadenosine, 2-Chloro-2′-deoxyadenosine, CldAdo, Jk 6251, NSC 105014

For research use only.

Cladribine (RWJ 26251, Leustatin, 2-CdA, 2-chlorodeoxyadenosine, 2-Chloro-2′-deoxyadenosine, CldAdo, Jk 6251, NSC 105014) is an adenosine deaminase inhibitor for U266, RPMI8226, and MM1.S cells with IC50 of approximately 2.43 μM, 0.75 μM, and 0.18 μM, respectively.

Cladribine (RWJ 26251) Chemical Structure

CAS No. 4291-63-8

Selleck's Cladribine (RWJ 26251) has been cited by 15 publications

Purity & Quality Control

Choose Selective Adenosine Deaminase Inhibitors

Biological Activity

Description Cladribine (RWJ 26251, Leustatin, 2-CdA, 2-chlorodeoxyadenosine, 2-Chloro-2′-deoxyadenosine, CldAdo, Jk 6251, NSC 105014) is an adenosine deaminase inhibitor for U266, RPMI8226, and MM1.S cells with IC50 of approximately 2.43 μM, 0.75 μM, and 0.18 μM, respectively.
Features Cladribine is primarily active in lymphoid tissues.
Targets
Adenosine deaminase (MM1.S cells) [1] Adenosine deaminase (RPMI8226 cells) [1] Adenosine deaminase (U266 cells) [1]
0.18 μM 0.75 μM 2.43 μM
In vitro

Cladribine exerts remarkable activity in hairy cell leukemia (HCL), a chronic B-cell lymphoproliferative disorder, producing prolonged complete remissions. Cladribine induces accumulation of DNA strand breaks, and subsequently activates the tumor suppressor p53 in lymphocytes. Cladribine may modulate STAT3 activity in MM cells. Cladribine inhibits proliferation/survival of U266, RPMI8226 and MM1.S cells in a dose-dependent manner. While U266 is the least sensitive cell line, MM1.S is the most sensitive one to cladribine. Treatment with cladribine gradually increases the percentage of cells in the G1 phase of the cell cycle and reduces the percentage of cells in S phase. Cladribine appears to increase G2-M phase in U266 cells upon 24 hour-treatment. A dose-dependent increase in apoptosis induced by cladribine is seen in both RPMI8226 and MM1.S cells. Treatment with cladribine at 0.2 μM dramatically induces activation of caspase-3, -8, and -9 and PARP cleavage in a time-dependent manner in MM1.S. Cladribine significantly decreases the phospho-STAT3 (P-STAT3) levels in a dose-dependent manner, but has no effect on the total STAT3 protein levels. [1] Cladribine possesses concentration-dependent apoptosis-inducing potential in the HSB2 cells. [2] Cladribine inhibits growth of primary mast cell (MC) and the MC line HMC-1 in a dose-dependent manner, with lower IC50 values recorded in HMC-1.2 cells harboring KIT D816V compared to HMC-1.1 cells lacking KIT D816V. [3] Cladribine decreases the migratory capacity of CD14+ monocytes, as well as of CD4+ and CD8+ T lymphocytes. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CCRF-CEM cell lines M1HFeWN6fG:2b4jpZ4l1gSCjc4PhfS=> MkPuR49ueG:3bnSge4F{KHSnc4Tl[EBnd3JiY4n0c5RwgGmlaYT5JIFo[Wmwc4SgR2NTTi2FRV2gZ4VtdCCuaX7ld{whUUN3ME2wMlAxOyEQvF2= NYOxOJVERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUezNlU2Pid-MUezNlU2PjxxYU6=
HEp-2 cell lines NHXWVWpEgXSxdH;4bYNqfHliYYPzZZk> NI\RRmJEd22yb4Xu[EB4[XNidHXzeIVlKG[xcjDjfZRwfG:6aXPpeJkh[WejaX7zeEBJTXBvMjDj[YxtKGyrbnXzMEBKSzVyPUCuNFMh|ryP M{T3UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{K1OVYoRjF5M{K1OVY9N2F-
L1210 cell lines M3zPeGN6fG:2b4jpZ4l1gSCjc4PhfS=> NHTaTYxEd22yb4Xu[EB4[XNidHXzeIVlKG[xcjDjfZRwfG:6aXPpeJkh[WejaX7zeEBNOTJzMDDj[YxtKGyrbnXzMEBKSzVyPUCuNFch|pyv Moi3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|MkW1Okc,OTd|MkW1Olww[T5?
CCRF-CEM cells M4jUN2N6fG:2b4jpZ4l1gSCjc4PhfS=> Mme4O|IhcA>? M3Hwd2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNEWkZvQ1XNJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC5yMEC1JO69VQ>? M3HySlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOESwO|IzLz5{MUi0NFczOjxxYU6=
human Raji cells NYP2ZlZPS3m2b4TvfIlkcXS7IHHzd4F6 NEHjd2Y4OiCq M4LKe2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHJicmliY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlAxQSEQvF2= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTh2MEeyNkc,OjF6NEC3NlI9N2F-
human HuH7 cells MXvDfZRwfG:6aXPpeJkh[XO|YYm= NF7GXpM4OiCq NUizWoI1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUHWKNzDj[YxteyCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVEvQCEQvF2= NH3xUG09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS2NlI4Pyd-MkW0OlIzPzd:L3G+
human T47D cells NESwXoVEgXSxdH;4bYNqfHliYYPzZZk> MYq3NkBp MlfWR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWFQ4TCClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuO{DPxE1? MmfrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2NkKyO|coRjJ3NE[yNlc4RC:jPh?=
human HCT116 cells M3rifGN6fG:2b4jpZ4l1gSCjc4PhfS=> Mn2yO|IhcA>? NHjUXJBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjNizszN M2T4WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NE[yNlc4Lz5{NUS2NlI4PzxxYU6=
human K562 cells MnLpVJJwdGmoZYLheIlwdiCjc4PhfS=> MUK0PEBp NIq0SpdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFu1OlIh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTFyIN88US=> NVXPXJo3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5OlA{OjNpPkK1PVYxOzJ|PD;hQi=>
human SKHEP1 cells NWHpfIpkWHKxbHnm[ZJifGmxbjDhd5NigQ>? MlTnOFghcA>? NUHmNJBKSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT2hGWDFiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUSg{txO MmDLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7NkCzNlMoRjJ3OU[wN|I{RC:jPh?=
human MOLT3 cells NYK3eYJ6WHKxbHnm[ZJifGmxbjDhd5NigQ>? NFnTTGk1QCCq MUnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2RTGSzJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0zNjNizszN MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl4MEOyN{c,OjV7NkCzNlM9N2F-
human KG1 cells NFToTlZRem:uaX\ldoF1cW:wIHHzd4F6 MVi0PEBp M{G3S2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1exJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjJizszN M4HGdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OU[wN|I{Lz5{NUm2NFMzOzxxYU6=
human RPMI8226 cells M3vUTnBzd2yrZnXyZZRqd25iYYPzZZk> M2nmdVQ5KGh? M4DDNWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUmDNTVgzOjZiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPU[g{txO NFO1UJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm2NFMzOyd-MkW5OlA{OjN:L3G+
human MCF7 cells Mk\6VJJwdGmoZYLheIlwdiCjc4PhfS=> NF7pPZo1QCCq M3HURmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PDVizszN NYDRbVZMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5OlA{OjNpPkK1PVYxOzJ|PD;hQi=>
human SK-UT-1B cells NVjHO4dDWHKxbHnm[ZJifGmxbjDhd5NigQ>? NUfwd2l{PDhiaB?= NFvVXoZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMXVVNTGEIHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xJO69VQ>? NFHzWnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm2NFMzOyd-MkW5OlA{OjN:L3G+
L1210 cell lines MoPtSpVv[3Srb36gZZN{[Xl? MWXJckB3cXS{bzDpcohq[mm2b4L5JIVn\mWldDD3ZZMhfGW|dHXkJIZweiCleYTvd5RifGmlIHHjeIl3cXS7IH;uJJRp\SCpcn;3eIghd2ZibYXybY5mKGyndXvlcYlkKExzMkGwJINmdGxibHnu[ZMtKEmGNUC9NE4xOyEQvF2= NF3qdnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUm1OlY3Lz5{OUm1OlY3RC:jPh?=
P388 leukemic cell lines MWHGeY5kfGmxbjDhd5NigQ>? M1W3eGlvKH[rdILvJIlvcGmkaYTvdpkh\W[oZXP0JJdieyC2ZYP0[YQh\m:{IHP5eI9{fGG2aXOgZYN1cX[rdImgc44hfGinIHfyc5d1cCCxZjDsfY1xcG:rZDDu[Y9xdGG|bTDQN|g5KGyndXvlcYlkKGOnbHygcIlv\XNuIFnEOVA:OC5yMzFOwG0> M2S4dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OUW2OlYoRjJ7OUW2OlY9N2F-
BV173 NFG0NXFEgXSxdH;4bYNqfHliYYPzZZk> M4XQSlMh\GG7cx?= MmjmR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRnYyPzNiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlAxODkQvF2= MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTdzMUC1OEc,OjF5MUGwOVQ9N2F-
BT549 NITjT25EgXSxdH;4bYNqfHliYYPzZZk> NUToVYpmOyCmYYnz M3\iW2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJVPTR7IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9NE4yOjQQvF2= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTdzMUC1OEc,OjF5MUGwOVQ9N2F-
CT26 M2DJbGN6fG:2b4jpZ4l1gSCjc4PhfS=> M{nIS|Mh\GG7cx?= NVLmdohTS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhS1R{NjDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvOTNzzszN M2LDfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{GxNFU1Lz5{MUexNVA2PDxxYU6=
MES-SA M1\j[WN6fG:2b4jpZ4l1gSCjc4PhfS=> MVmzJIRigXN? MXLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSXMuW0FiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlE3Pc7:TR?= M4S1dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{GxNFU1Lz5{MUexNVA2PDxxYU6=
K562 M1vSd2N6fG:2b4jpZ4l1gSCjc4PhfS=> MmDKN{Bl[Xm| M4fkd2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJJBi[2yrdHH4[YwhemW|aYP0ZY51KEt3NkKgZ4VtdHNiYX\0[ZIhOyCmYYnzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjF5zszN NW[5cZdHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG3NVExPTRpPkKxO|EyODV2PD;hQi=>
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CEM-DNR-bulk NUDkRmE1S3m2b4TvfIlkcXS7IHHzd4F6 NYn3T4g2OyCmYYnz MWDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDSW0uTE6ULXL1cIsh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UWEBie3OjeTygTWM2OD1yLkO1Nu69VQ>? MkLKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF5MUGwOVQoRjJzN{GxNFU1RC:jPh?=
L1210 MnTLR5l1d3SxeHnjbZR6KGG|c3H5 NW\pO4J5OyCmYYnz Ml;NR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgUFEzOTBiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlM6O87:TR?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTdzMUC1OEc,OjF5MUGwOVQ9N2F-
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MCF7 M{DvWmN6fG:2b4jpZ4l1gSCjc4PhfS=> MUezJIRigXN? MUnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHQh[XO|YYmsJGlEPTB;Mj6zOe69VQ>? MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTdzMUC1OEc,OjF5MUGwOVQ9N2F-
K562 NHvOS5JEgXSxdH;4bYNqfHliYYPzZZk> M324VFMh\GG7cx?= MVLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHQh[XO|YYmsJGlEPTB;Nz62Pe69VQ>? NYPyW4dRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG3NVExPTRpPkKxO|EyODV2PD;hQi=>
PC3 M3vMdGN6fG:2b4jpZ4l1gSCjc4PhfS=> Mn;TN{Bl[Xm| M4\ad2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBEOyClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUiuNljPxE1? MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTdzMUC1OEc,OjF5MUGwOVQ9N2F-
C6 NXz2bXk3S3m2b4TvfIlkcXS7IHHzd4F6 NWr1d5pnOyCmYYnz M1v0UWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KHKjdDDDOkBk\WyuczDh[pRmeiB|IHThfZMh[nliTWTUJIF{e2G7LDDJR|UxRTlwMEhOwG0> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTdzMUC1OEc,OjF5MUGwOVQ9N2F-
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HCT116 M3judmN6fG:2b4jpZ4l1gSCjc4PhfS=> MW[3NkBpenN? NF;5WY1EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IGPSRkBie3OjeTygTWM2OD1yLkROwG0> M37IOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkG5NFQ3Lz5{OEKxPVA1PjxxYU6=
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MCF7 MkO5R5l1d3SxeHnjbZR6KGG|c3H5 MnzLO|IhcHK| M4jxWWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0z|ryP MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJzOUC0Okc,Ojh{MUmwOFY9N2F-
TC32 MVLxTHRUKGG|c3H5 MmjldWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFSFM{KgZ4VtdHN? M3;mVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SJ-GBM2 MoWzdWhVWyCjc4PhfS=> M{XKOpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSj3HRm0zKGOnbHzz MonGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
A673 NFXBRnpyUFSVIHHzd4F6 MofwdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN? M2[zUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC MVvxTHRUKGG|c3H5 NWHm[JY4eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> NV3ibGJbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-37 NYTBZ2w5eUiWUzDhd5NigQ>? MlPtdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUO3JINmdGy| NVHVeHpRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 MUTxTHRUKGG|c3H5 MljldWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?= MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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OHS-50 M{\zNpFJXFNiYYPzZZk> NXzRNplIeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=> MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MG 63 (6-TG R) MWnxTHRUKGG|c3H5 MnnqdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE2JIE[zJEg3NVSJIGKpJINmdGy| MoS3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB1643 MWHxTHRUKGG|c3H5 M2PlVZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJG5DOTZ2MzDj[Yxtew>? M1;K[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
A673 NXPwTHFseUiWUzDhd5NigQ>? MUHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDBOlc{KGOnbHzzLS=> MkDzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC NFKzVlZyUFSVIHHzd4F6 M4PVS5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vTVOgZ4VtdHN? NWW3WZR5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-37 M4n3VJFJXFNiYYPzZZk> MVHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDCWE0{PyClZXzsdy=> MkfDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
TC32 MoDBdWhVWyCjc4PhfS=> MWrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDUR|MzKGOnbHzz MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MG 63 (6-TG R) M1zPTZFJXFNiYYPzZZk> MVnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDNS{A3OyBqNj3US{BTMSClZXzsdy=> NYHHdHBbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
In vivo Cladribine (0.7-3.5 mM) and/or diltiazem (2.4 mM), is injected intraperitoneally into adult zebrafish and red blood cell (RBC) lysates are assayed by HPLC for levels of purine nucleotides (e.g. ATP), potential biomarkers of cardiovascular health. Diltiazem increased RBC ATP concentrations, which are inhibited by co-injection of cladribine. [5] Plasma concentrations of Cladribine decreases rapidly following a biphasic decline after both ia and s.c. administrations. The AUC and t 1/2 beta after a single 1 mg/kg ia and 2 mg/kg s.c. injection of Cladribine are 0.66 vs 1.2 μg × h/mL and 3.5 vs 4.5 hours, respectively. [6]

Protocol (from reference)

Cell Research:[1]
  • Cell lines: U266, RPMI8226 and MM1.S
  • Concentrations: 0 μM - 32 μM
  • Incubation Time: 72 hours
  • Method: The non-radioactive cell proliferation kit is used to determine cell viability. In brief, Human MM cell line U266, RPMI8226 and MM1.S are seeded onto 96-well plates with either 0.1 mL complete medium (5% FBS) as control, or 0.1 mL of the same medium containing a series of doses of cladribine, and incubated for 72 hours. After reading all wells at 490 nm with a micro-plate reader, the percentages of surviving cells from each group relative to controls, defined as 100% survival, are determined by reduction of MTS.
Animal Research:[5]
  • Animal Models: Adult wild-type (AB) zebrafish
  • Dosages: 0.7 mM - 3.5 mM
  • Administration: Administered via i.p.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+1% Tween 80+H2O
For best results, use promptly after mixing.

10mg/mL

Chemical Information

Molecular Weight 285.69
Formula

C10H12ClN5O3

CAS No. 4291-63-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1C(C(OC1N2C=NC3=C(N=C(N=C32)Cl)N)CO)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04997148 Recruiting -- Relapsing-Remitting Multiple Sclerosis Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany|Merck Serono Limited an affiliate of Merck KGaA Darmstadt Germany August 11 2021 --
NCT04821596 Recruiting Other: biological collection Multiple Sclerosis University Hospital Rouen July 13 2020 Not Applicable
NCT04121065 Not yet recruiting Procedure: Blood withdrawal Relapsing Multiple Sclerosis Neuromed IRCCS January 2020 --

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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